Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03359
[1], [2]
Histone modification H3K27ac HDAC2 ALKBH5 Direct Inhibition m6A modification SPRY2 SPRY2 ALKBH5 Demethylation : m6A sites
m6A Modification:
m6A Regulator RNA demethylase ALKBH5 (ALKBH5) ERASER
m6A Target Protein sprouty homolog 2 (SPRY2)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Histone modification (HistMod)
Epigenetic Regulator Histone deacetylase 2 (HDAC2) ERASER View Details
Regulated Target Histone H3 lysine 27 acetylation (H3K27ac) View Details
Downstream Gene ALKBH5 View Details
Crosstalk Relationship Histone modification  →  m6A Inhibition
Crosstalk Mechanism histone modification directly impacts m6A modification through modulating the level of m6A regulator
Crosstalk Summary Mechanically, HDAC2-reduced Histone H3 lysine 27 acetylation (H3K27ac) inhibits ALKBH5 transcription in CRC, whereas ectopic ALKBH5 expression decreases tumorigenesis of CRC cells and protects mice from colitis-associated tumor development.METTL14/ALKBH5/IGF2BPs combine to modulate JMJD8 stability in an m6A-dependent manner, which increases glycolysis and accelerates the development of CRC by enhancing the enzymatic activity of PKM2. ALKBH5 plays an antitumor role in colorectal cancer by modulating the FOXO3/miR-21/Protein sprouty homolog 2 (SPRY2) axis, which not only suggests a regulatory effect between ALKBH5 and FOXO3, but also provides a new therapeutic direction for colorectal cancer.
Responsed Disease Colorectal cancer ICD-11: 2B91
Pathway Response FoxO signaling pathway hsa04068
In-vitro Model
HCT 116 Colon carcinoma Homo sapiens CVCL_0291
Caco-2 Colon adenocarcinoma Homo sapiens CVCL_0025
SW480 Colon adenocarcinoma Homo sapiens CVCL_0546
SW620 Colon adenocarcinoma Homo sapiens CVCL_0547
FHC Normal Homo sapiens CVCL_3688
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Histone deacetylase 2 (HDAC2) 113 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name CHR-3996 Phase 1/2 [3]
Synonyms
CCT-075453; CHR-2504; HDAC inhibitors, Chroma Therapeutics; Histone deacetylase inhibitors, Chroma
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4 nM
External Link
 Compound Name PMID29671355-Compound-74 Patented [4]
MOA Inhibitor
Activity IC50 = 119 nM
External Link
 Compound Name PMID29671355-Compound-59 Patented [4]
MOA Inhibitor
Activity IC50 = 10 nM
External Link
 Compound Name PMID29671355-Compound-55 Patented [4]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID29671355-Compound-11 Patented [4]
MOA Inhibitor
Activity IC50 = 24 nM
External Link
 Compound Name PMID29671355-Compound-9 Patented [4]
MOA Inhibitor
Activity IC50 = 128 nM
External Link
 Compound Name PMID29671355-Compound-8 Patented [4]
MOA Inhibitor
Activity IC50 = 123000 nM
External Link
 Compound Name PMID29671355-Compound-61 Patented [4]
MOA Inhibitor
Activity IC50 = 45.9 nM
External Link
 Compound Name PMID29671355-Compound-23 Patented [4]
MOA Inhibitor
Activity IC50 = 7450 nM
External Link
 Compound Name PMID29671355-Compound-44 Patented [4]
MOA Inhibitor
Activity IC50 < 150 nM
External Link
 Compound Name PMID29671355-Compound-56 Patented [4]
MOA Inhibitor
Activity IC50 = 54.4 nM
External Link
 Compound Name PMID29671355-Compound-67 Patented [4]
MOA Inhibitor
Activity IC50 > 50000 nM
External Link
 Compound Name PMID29671355-Compound-31 Patented [4]
MOA Inhibitor
Activity IC50 = 2 nM
External Link
 Compound Name PMID29671355-Compound-21 Patented [4]
MOA Inhibitor
Activity IC50 = 4880 nM
External Link
 Compound Name PMID29671355-Compound-62 Patented [4]
MOA Inhibitor
Activity IC50 = 100 to 500 nM
External Link
 Compound Name PMID29671355-Compound-43 Patented [4]
MOA Inhibitor
Activity IC50 = 124 nM
External Link
 Compound Name PMID29671355-Compound-25 Patented [4]
MOA Inhibitor
Activity IC50 = 5400 nM
External Link
 Compound Name N8-hydroxy-2-methoxy-N1-phenyloctanediamide Investigative [5]
Synonyms
CHEMBL251010; SCHEMBL8158442
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name N-(4'-acetyl-4-aminobiphenyl-3-yl)benzamide Investigative [6]
Synonyms
CHEMBL1099078; BDBM50317997
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3800 nM
External Link
 Compound Name N-Hydroxy-E-3-(4'-chlorobiphenyl-4-yl)-acrylamide Investigative [7]
Synonyms
CHEMBL557066; SCHEMBL3292989; SCHEMBL3292983; BDBM50293365
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1860 nM
External Link
 Compound Name N7-hydroxy-2-methoxy-N1-phenylheptanediamide Investigative [5]
Synonyms
CHEMBL251206; SCHEMBL8143763
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name N7-hydroxy-N1-phenyl-2-propoxyheptanediamide Investigative [5]
Synonyms
CHEMBL251406; SCHEMBL8144856
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name N-(4-amino-4'-vinylbiphenyl-3-yl)benzamide Investigative [6]
Synonyms
CHEMBL1096397; BDBM50318002
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 800 nM
External Link
 Compound Name N-(4-amino-3'-methoxybiphenyl-3-yl)benzamide Investigative [6]
Synonyms
CHEMBL1097747; BDBM50317991
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1300 nM
External Link
 Compound Name KAR-1880 Investigative [8]
Synonyms
Anti-inflammatory OS-HDI; OS-HDI-2; HDAC 2 inhibitors (topical, dermatitis/psoriasis), Karus
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-(2-amino-5-(pyridin-4-yl)phenyl)benzamide Investigative [6]
Synonyms
CHEMBL1095096
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3900 nM
External Link
 Compound Name N-(4-amino-3'-methylbiphenyl-3-yl)benzamide Investigative [6]
Synonyms
CHEMBL1094108; BDBM50317995
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MOA Inhibitor
Activity IC50 = 3100 nM
External Link
 Compound Name N-(3'-acetyl-4-aminobiphenyl-3-yl)benzamide Investigative [6]
Synonyms
CHEMBL1097746; BDBM50317992
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 13000 nM
External Link
 Compound Name N-(4-amino-4'-fluorobiphenyl-3-yl)benzamide Investigative [6]
Synonyms
CHEMBL1098337; SCHEMBL15398027; BDBM50317988
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1400 nM
External Link
 Compound Name N8,2-dihydroxy-N1-phenyloctanediamide Investigative [5]
Synonyms
CHEMBL251009; SCHEMBL8144564
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name N-(2-amino-5-(furan-3-yl)phenyl)benzamide Investigative [6]
Synonyms
CHEMBL1095095; Benzamide, N-[2-amino-5-(3-furanyl)phenyl]-; BDBM50318000
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 39 nM
External Link
 Compound Name N-Hydroxy-E-3-(biphenyl-4-yl)-acrylamide Investigative [7]
Synonyms
CHEMBL556532; SCHEMBL3292226; SCHEMBL3290139
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 820 nM
External Link
 Compound Name 2-(allyloxy)-N8-hydroxy-N1-phenyloctanediamide Investigative [5]
Synonyms
CHEMBL402719; SCHEMBL8150833
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name 2-(benzyloxy)-N7-hydroxy-N1-phenylheptanediamide Investigative [5]
Synonyms
CHEMBL402718; SCHEMBL8152458
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name N-(4-amino-4'-bromobiphenyl-3-yl)benzamide Investigative [6]
Synonyms
CHEMBL1097748; BDBM50317990
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 600 nM
External Link
 Compound Name N-(2-amino-5-(furan-2-yl)phenyl)benzamide Investigative [6]
Synonyms
CHEMBL1097651
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 43 nM
External Link
 Compound Name 5-(Biphenyl-4-yl)-pentanoic acid N-hydroxyamide Investigative [7]
Synonyms
CHEMBL541239; SCHEMBL7045815
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 720 nM
External Link
 Compound Name N-(4-aminobiphenyl-3-yl)benzamide Investigative [6]
Synonyms
CHEMBL271741; 3max; SCHEMBL16380794; BDBM50232053; N-(4-amino-biphenyl-3-yl)-benzamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 27 nM
External Link
 Compound Name N-(2-amino-5-(benzofuran-2-yl)phenyl)benzamide Investigative [6]
Synonyms
CHEMBL1097063
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10000 nM
External Link
 Compound Name N-(2-aminophenyl)benzamide Investigative [6]
Synonyms
2'-AMINOBENZANILIDE; 721-47-1; CHEMBL405072; AC1LFSYX; AC1Q5NOK; ACMC-1AE0C; Oprea1_478192; MLS000084661; SCHEMBL407834; N-(2-amino-phenyl)-benzamide; AC1Q514U; Benzamide, N-(2-aminophenyl)-; CTK2H2825; DTXSID60353948; RFDVMOUXHKTCDO-UHFFFAOYSA-N; MolPort-001-783-352; ZINC225957; HMS2355D18; STL497474; BDBM50232046; AKOS000133162; MCULE-5545982713; NE17312; SMR000019009; TC-170926; KB-298435; ST51030142; EN300-31745; SR-01000389415; AE-641/00785046
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3100 nM
External Link
 Compound Name N-(4-amino-4'-methoxybiphenyl-3-yl)benzamide Investigative [6]
Synonyms
CHEMBL1095412; BDBM50317998
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 140 nM
External Link
 Compound Name N-Hydroxy-E-3-(4'-cyanobiphenyl-4-yl)-acrylamide Investigative [7]
Synonyms
CHEMBL538710; SCHEMBL3292721; SCHEMBL3292715; BDBM50293355
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 330 nM
External Link
 Compound Name N-(2-amino-5-(thiazol-2-yl)phenyl)benzamide Investigative [6]
Synonyms
CHEMBL1097278
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 390 nM
External Link
 Compound Name N-(2-aminophenyl)quinoxaline-6-carboxamide Investigative [9]
Synonyms
benzamide-type inhibitor, 20; CHEMBL236060; BDBM19424
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2000 nM
External Link
 Compound Name 7-Biphenyl-4-yl-heptanoic acid hydroxyamide Investigative [10]
Synonyms
CHEMBL125098; BDBM50222335; 7-(4-Biphenylyl)heptanehydroximic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid Investigative [11]
Synonyms
CHEMBL115049; 436150-72-0; SCHEMBL7368556; CTK1D2674; DTXSID40658342; BDBM50221807; 8-[([1,1'-Biphenyl]-4-yl)oxy]-2-oxooctanoic acid; Octanoic acid, 8-([1,1'-biphenyl]-4-yloxy)-2-oxo-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 1,1,1-Trifluoro-8-phenoxy-octan-2-one Investigative [12]
Synonyms
CHEMBL114796; BDBM50217940
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 7-(Biphenyl-4-yloxy)-heptanoic acid hydroxyamide Investigative [11]
Synonyms
CHEMBL114184; SCHEMBL3383144
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 7-Phenoxy-heptanoic acid hydroxyamide Investigative [10]
Synonyms
CHEMBL124322; N-hydroxy-7-phenoxyheptanamide; 7-Phenoxyheptanehydroximic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one Investigative [12]
Synonyms
CHEMBL117916; SCHEMBL7366611; BDBM50217945
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-(4-hydroxybiphenyl-3-yl)benzamide Investigative [13]
Synonyms
CHEMBL269935; SCHEMBL5724398; BDBM50232005
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 200 nM
External Link
 Compound Name 8-Phenyl-octanoic acid hydroxyamide Investigative [10]
Synonyms
CHEMBL123624; N-Hydroxy-8-phenyloctanamide; SCHEMBL5807174
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one Investigative [12]
Synonyms
CHEMBL116023; SCHEMBL7368359; BDBM50218558
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-(2-aminophenyl)nicotinamide Investigative [13]
Synonyms
N-(2-Amino-phenyl)-nicotinamide; 436089-31-5; N-(2-aminophenyl)pyridine-3-carboxamide; CHEMBL236678; AC1LMN6K; SCHEMBL18086514; CTK4I7538; DTXSID50360661; CHEBI:125506; ZINC873967; BDBM50220259; 3463AE; AKOS000129725; RTR-042156; MCULE-7933541910; N-(2-aminophenyl)-3-pyridylcarboxamide; ZB014940; ACM436089315; ST086607; ASN 01337807; KB-298440; TR-042156; BC4148434; SR-01000329900; SR-01000329900-1; BRD-K20880473-001-04-6
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 6980 nM
External Link
 Compound Name santacruzamate A Investigative [14]
Synonyms
CAY10683
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.112 nM
External Link
 Compound Name N-(4-aminobiphenyl-3-yl)nicotinamide Investigative [13]
Synonyms
CHEMBL255805; BDBM50232035
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 900 nM
External Link
 Compound Name N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide Investigative [13]
Synonyms
CHEMBL256440; SCHEMBL1066609
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 390 nM
External Link
 Compound Name N-(2-aminophenyl)-4-methoxybenzamide Investigative [9]
Synonyms
AC1LFX2W; Cambridge id 5129152; Oprea1_722128; benzamide-type inhibitor, 22; CHEMBL236061; SCHEMBL5226034; BDBM19426; CTK7A1998; MolPort-001-019-504; BDYVCYUXCNZYRW-UHFFFAOYSA-N; ZINC281656; STK156256; AKOS000130378; MCULE-9183453747; N-(2-Amino-phenyl)4-methoxy-benzamide; N-(2-amino-phenyl)-4-methoxy-benzamide; NCGC00240897-01; N1-(4-methoxybenzoyl)-1,2-benzenediamine; N1-(4-methoxy-benzoyl)-1,2-benzenediamine; ST50908739; N-(2-aminophenyl)(4-methoxyphenyl)carboxamide; SR-01000196394
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 900 nM
External Link
 Compound Name 4-Phenylbutyrohydroxamic acid Investigative [15]
Synonyms
N-Hydroxy-4-phenylbutanamide; 32153-46-1; NSC131300; UNII-QX182FOM5S; QX182FOM5S; 4-phenylbutanehydroxamic acid; CHEMBL55895; Benzenebutanamide, N-hydroxy-; NSC 131300; AC1Q7DIW; AC1L5RDX; Phenylbutyrylhydroxamic Acid; AC1Q5QD1; N-Hydroxy-4-phenyl-butyramide; 4-Phenylbutyryl hydroxamic acid; SCHEMBL1350853; CTK4G8310; DTXSID60185943; MolPort-011-492-164; UPHXPXYRKPCXHK-UHFFFAOYSA-N; ZINC4962622; STL301752; BDBM50015142; AKOS009266186; MCULE-9765156954; NSC-131300; NE28489; BCB03_000829; EN300-68596
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 430 nM
External Link
 Compound Name 8-Oxo-8-phenyl-octanoic acid hydroxyamide Investigative [16]
Synonyms
CHEMBL95959; SCHEMBL3383197; N-hydroxy-8-oxo-8-phenyloctanamide
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Octanedioic acid bis-hydroxyamide Investigative [17]
Synonyms
Suberohydroxamic acid
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 29 nM
External Link
 Compound Name ST-2986 Investigative [18]
Synonyms
CHEMBL471041; SCHEMBL3444455; BDBM50278219
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 11000 nM
External Link
 Compound Name 9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide Investigative [12]
Synonyms
9,9,9-Trifluoro-8-Oxo-N-Phenylnonanamide; CHEMBL113537; 2gh6; SCHEMBL2702892; KRCXZGYVOZSCSF-UHFFFAOYSA-N; BDBM50121062; DB07553
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1400 nM
External Link
 Compound Name 7-Mercapto-heptanoic acid phenylamide Investigative [19]
Synonyms
Thiol-SAHA (t-SAHA); CHEMBL325676; SCHEMBL14821761; BDBM152692
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1300 nM
External Link
 Compound Name 6-benzenesulfinylhexanoic acid hydroxamide Investigative [20]
Synonyms
6-(benzenesulfinyl)hexanoic acid hydroxyamide; 875737-03-4
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-(2-Mercapto-ethyl)-N'-phenyl-succinamide Investigative [21]
Synonyms
CHEMBL193959
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 7-Mercapto-heptanoic acid biphenyl-4-ylamide Investigative [19]
Synonyms
CHEMBL112311
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-Hydroxy-4-phenylacetylamino-benzamide Investigative [22]
Synonyms
CHEMBL356824; 656261-23-3; SCHEMBL675578; CTK1J6158; DTXSID40458440; ZINC13533297; AKOS030583151; Benzeneacetamide, N-[4-[(hydroxyamino)carbonyl]phenyl]-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6-(2-Bromo-acetylamino)-hexanoic acid phenylamide Investigative [19]
Synonyms
CHEMBL344920; 651767-99-6; SCHEMBL3736839; CTK1J8444; DTXSID50432973; HWYLREOMBVUGJQ-UHFFFAOYSA-N; BDBM50222416; ZINC13587789; AKOS030603042; N-Phenyl-6-(bromoacetylamino)hexanamide; Hexanamide, 6-[(bromoacetyl)amino]-N-phenyl-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide Investigative [23]
Synonyms
CHEMBL143674; SCHEMBL673760
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one Investigative [24]
Synonyms
CHEMBL126355; BDBM50222394
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Octanedioic acid hydroxyamide pyridin-4-ylamide Investigative [25]
Synonyms
SCHEMBL8082656; CHEMBL165162; ZINC13472304
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-(6-Mercapto-hexyl)-benzamide Investigative [19]
Synonyms
CHEMBL112364; BDBM50223650
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide Investigative [25]
Synonyms
CHEMBL167455
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Investigative [22]
Synonyms
SCHEMBL675474
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6-benzenesulfonylhexanoic acid hydroxamide Investigative [20]
Synonyms
CHEMBL203207
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one Investigative [12]
Synonyms
SCHEMBL7373122; CHEMBL116578
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Thioacetic acid S-(6-phenylcarbamoyl-hexyl) ester Investigative [19]
Synonyms
CHEMBL111806; SCHEMBL14812153
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-Butyrylamino-N-hydroxy-benzamide Investigative [23]
Synonyms
CHEMBL142254; 656261-22-2; Benzamide, N-hydroxy-4-[(1-oxobutyl)amino]-; SCHEMBL675234; CTK1J6159; DTXSID90461262
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Investigative [24]
Synonyms
CHEMBL127328
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 7-Mercapto-heptanoic acid biphenyl-3-ylamide Investigative [19]
Synonyms
CHEMBL320323
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione Investigative [26]
MOA Inhibitor
External Link
 Compound Name N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide Investigative [22]
Synonyms
SCHEMBL676079
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide Investigative [19]
Synonyms
CHEMBL324126
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 7-Mercapto-heptanoic acid pyridin-3-ylamide Investigative [19]
Synonyms
CHEMBL332246; Heptanamide, 7-mercapto-N-3-pyridinyl-; BDBM50223653
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6-Phenoxy-hexane-1-thiol Investigative [19]
Synonyms
CHEMBL109796; 6-phenoxyhexane-1-thiol; 1-Hexanethiol, 6-phenoxy-; SCHEMBL5679745; MolPort-020-180-823; BDBM50223652; AKOS018584222; MCULE-9521857089
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-Benzoylamino-N-hydroxy-benzamide Investigative [22]
Synonyms
SCHEMBL673678; CHEMBL191227
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide Investigative [16]
Synonyms
CHEMBL143734; NSC718168; AC1L8L82; SCHEMBL13039735; ZINC5579677; BDBM50082664; NSC-718168; NCI60_040737; 6-(4-Chlorobenzoylamino)hexanehydroxamic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Investigative [12]
Synonyms
CHEMBL112148; SCHEMBL7364383; BDBM50218532
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Investigative [24]
Synonyms
CHEMBL127351; SCHEMBL7365180; HWZHDGRMABBYOV-UHFFFAOYSA-N; BDBM50222367; 7-((1,1'-biphenyl)-3-yloxy)-1-(1 ,3-oxazol-2-yl)-1-heptanone
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6-Mercapto-hexanoic acid phenylamide Investigative [19]
Synonyms
CHEMBL109654; Hexanamide, 6-mercapto-N-phenyl-; SCHEMBL14254925; BDBM50027600
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2220 nM
External Link
 Compound Name Cyclostellettamine derivative Investigative [27]
Synonyms
CHEMBL88332
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MOA Inhibitor
External Link
 Compound Name N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide Investigative [16]
Synonyms
CHEMBL139999; SCHEMBL1232700; BDBM50082661; ZINC13472309
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MOA Inhibitor
External Link
 Compound Name 5-Mercapto-pentanoic acid phenylamide Investigative [19]
Synonyms
N-Phenyl-5-mercaptovaleramide; CHEMBL114344; Pentanamide, 5-mercapto-N-phenyl-
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MOA Inhibitor
External Link
 Compound Name Octanedioic acid hydroxyamide pyridin-2-ylamide Investigative [25]
Synonyms
SCHEMBL8090513; CHEMBL164872; ZINC13472303
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MOA Inhibitor
External Link
 Compound Name N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide Investigative [21]
Synonyms
CHEMBL193979
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MOA Inhibitor
External Link
 Compound Name 2-(methylsulfonylthio)ethyl 2-propylpentanoate Investigative [26]
Synonyms
CHEMBL271677; SCHEMBL4156413
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MOA Inhibitor
External Link
 Compound Name (E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Investigative [24]
Synonyms
CHEMBL126465; SCHEMBL7368197; SCHEMBL7368201
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MOA Inhibitor
External Link
 Compound Name N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Investigative [22]
Synonyms
SCHEMBL676080
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MOA Inhibitor
External Link
 Compound Name N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide Investigative [28]
Synonyms
N-hydroxy-4-(3-phenylpropanamido)benzamide
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MOA Inhibitor
External Link
 Compound Name N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Investigative [22]
Synonyms
SCHEMBL7311087
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MOA Inhibitor
External Link
 Compound Name 8-Oxo-8-phenyl-octanoic acid Investigative [25]
Synonyms
8-Oxo-8-phenyloctanoic acid; 7-Benzoylheptanoic acid; 24314-23-6; Benzeneoctanoic acid, h-oxo-; 7-BENZOYL HEPTANOIC ACID; AC1L6TSB; SCHEMBL3381106; 8-keto-8-phenyl-caprylic acid; CHEMBL162423; 8-Oxo-8-phenyloctanoic acid #; CTK4F3363; DTXSID40305602; UMCSRRHQLAVYRS-UHFFFAOYSA-N; ZINC2168376; 7009f; NSC171230; AKOS016022495; NSC-171230; MCULE-7202530747; ACM24314236; ST50825837
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MOA Inhibitor
External Link
 Compound Name N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide Investigative [22]
Synonyms
CHEMBL143336; 656261-24-4; SCHEMBL674421; CTK1J6157; DTXSID30433908; ZINC13533300; AKOS030583673; n-hydroxy-4-(4-phenylbutyryl-amino)benzamide; Benzenebutanamide, N-[4-[(hydroxyamino)carbonyl]phenyl]-
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MOA Inhibitor
External Link
 Compound Name 6-phenylsulfanylhexanoic acid hydroxamide Investigative [20]
Synonyms
Hexanamide, N-hydroxy-6-(phenylthio)-; CHEMBL203028; SCHEMBL7317658
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MOA Inhibitor
External Link
 Compound Name ST-2987 Investigative [18]
Synonyms
CHEMBL471042; SCHEMBL3444989; SCHEMBL3444984; BDBM50278220
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MOA Inhibitor
Activity IC50 = 2670 nM
External Link
 Compound Name 7-Mercapto-heptanoic acid quinolin-3-ylamide Investigative [19]
Synonyms
CHEMBL112234
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MOA Inhibitor
External Link
 Compound Name 5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide Investigative [29]
Synonyms
CHEMBL84288
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MOA Inhibitor
External Link
 Compound Name 8-Mercapto-octanoic acid phenylamide Investigative [19]
Synonyms
8-mercapto-N-phenyloctanamide; CHEMBL326433; ZINC13609343
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MOA Inhibitor
Activity IC50 = 754 nM
External Link
 Compound Name N-(6-Hydroxycarbamoyl-hexyl)-benzamide Investigative [25]
Synonyms
CHEMBL57107; 174664-71-2; SCHEMBL573254; CTK0A7470; DTXSID00433435; BDBM50220823; ZINC13490043; 7-(Benzoylamino)heptanehydroxamic acid; AKOS030580013; Benzamide, N-[7-(hydroxyamino)-7-oxoheptyl]-
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MOA Inhibitor
External Link
 Compound Name 7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one Investigative [12]
Synonyms
CHEMBL326529; SCHEMBL7365237; BDBM50217957
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MOA Inhibitor
External Link
 Compound Name 7-Mercapto-heptanoic acid benzothiazol-2-ylamide Investigative [19]
Synonyms
CHEMBL178779
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MOA Inhibitor
External Link
 Compound Name N-Hydroxy-4-(pentanoylamino-methyl)-benzamide Investigative [23]
Synonyms
CHEMBL143102
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MOA Inhibitor
External Link
 Compound Name PSAMMAPLIN A Investigative [16]
Synonyms
110659-91-1; Bisprasin; NSC614495; AC1O46WI; SCHEMBL364511; ZINC150352860; NSC-614495; B723735K022; J-002461; Benzenepropanamide, N,N'-(dithiodi-2,1-ethanediyl)bis(3-bromo-4-hydroxy-alpha-(hydroxyimino)-
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MOA Inhibitor
External Link
2B91: Colorectal cancer 25 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Retifanlimab Approved [30]
Synonyms
INCMGA0012; Retifanlimab
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External Link
 Compound Name Aflibercept Approved [31]
Synonyms
Ziv-Aflibercept; Zaltrap (TN); VEGF Trap; VEGF Trap-Eye
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External Link
 Compound Name Regorafenib Approved [32]
Synonyms
755037-03-7; BAY 73-4506; Regorafenibum; Stivarga; 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide; BAY73-4506; Regorafenib (BAY 73-4506); UNII-24T2A1DOYB; 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide; BAY-73-4506; 24T2A1DOYB; CHEMBL1946170; CHEBI:68647; Stivarga (TN); BAY73-4506 hydrochloride; Regorafenib [USAN:INN]
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External Link
 Compound Name Bevacizumab Approved [33]
Synonyms
Bevacizumab (ophthalmic slow-release tissue tablet)
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External Link
 Compound Name SYM-004 Phase 3 [33]
Synonyms
Chimeric IgG1 antibody 1024 (cancer), Symphogen; Chimeric IgG1 antibody 992 (cancer), Symphogen; Chimeric IgG1 antibodies992 + 1024 (cancer), Symphogen
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External Link
 Compound Name Bevacizumab + Erlotinib Phase 3 [34]
External Link
 Compound Name CPI-613 Phase 3 [33]
Synonyms
95809-78-2; 6,8-bis(benzylthio)octanoic acid; CPI 613; MLS006010202; SCHEMBL1062218; 6,8-Bis(benzylsulfanyl)octanoic acid; Octanoic acid, 6,8-bis((phenylmethyl)thio)-; Octanoic acid, 6,8-bis[(phenylMethyl)thio]-; 6,8-Bis[(phenylmethyl)thio]octanoic acid; CPI613; CHEMBL3186849; QCR-193; AOB1058; MolPort-023-219-128; HMS3656L06; C22H28O2S2; BCP04663; EX-A2043; s2776; AKOS025142095; BCP9000552; DB12109; RL06062; CS-0961; NCGC00344764-01; SMR004701300; AS-16613; BC261916; AK174899; HY-15453; BCP0726000030; KB-293127; AB0035874
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External Link
 Compound Name Bevacizumab Approved [31]
External Link
 Compound Name AlloStim Phase 2/3 [35]
Synonyms
AlloStim (TN)
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External Link
 Compound Name Sibrotuzumab Phase 2 [36]
External Link
 Compound Name CV301 Phase 2 [37]
External Link
 Compound Name Efatutazone Phase 2 [38]
Synonyms
Inolitazone; 223132-37-4; 5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-Thiazolidinedione; Efatutazone [INN]; RS5444; CS-7017; SCHEMBL3246054; CHEMBL3545280; JCYNMRJCUYVDBC-UHFFFAOYSA-N; Efatutazone;CS-7017;RS5444; BCP07478; AKOS030526729; DB11894; CS-0778; KB-77905; DA-07988; HY-14792; QC-10456; 4CA-1384; FT-0737589; 5-[4-[6-(4-amino-3 ,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy]benzyl]thiazolidine-2,4-dione
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External Link
 Compound Name LOR-2040 Phase 2 [39]
External Link
 Compound Name RG7221 Phase 2 [40]
External Link
 Compound Name PEG-SN38 Phase 2 [41]
Synonyms
EZN-2208
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External Link
 Compound Name MEGF0444A Phase 2 [42]
External Link
 Compound Name Encapsulated cell therapy Phase 1/2 [43]
External Link
 Compound Name AB928 Phase 1/2 [44]
External Link
 Compound Name MGD007 Phase 1 [40]
External Link
 Compound Name BNC-101 Phase 1 [45]
External Link
 Compound Name Navicixizumab Phase 1 [33]
External Link
 Compound Name RG7160 Discontinued in Phase 2 [46]
External Link
 Compound Name Nimesulide Terminated [47]
Synonyms
51803-78-2; N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide; Mesulid; Flogovital; Sulidene; Nimed; R-805; 4-NITRO-2-PHENOXYMETHANESULFONANILIDE; Nisulid; Nimesulidum [INN-Latin]; Nimesulida [INN-Spanish]; R 805; UNII-V4TKW1454M; 4-Nitro-2-phenoxy-methanesulfonanilide; 4'-Nitro-2'-phenoxymethanesulfonanilide; Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)-; EINECS 257-431-4; 4'-Nitro-2'-phenoxymethansulfonanilid; BRN 2421175; CHEMBL56367; MLS000069680; V4TKW1454M; Methanesulfonanilide, 4'-nitro-2'-phenoxy-; CHEBI:44445; Dulanermin
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External Link
 Compound Name Saracatinib Phase 2 [48]
External Link
 Compound Name G3139 + Irinotecan Investigative [49]
External Link
References
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Ref 2 m(6)A demethylase ALKBH5 inhibits cell proliferation and the metastasis of colorectal cancer by regulating the FOXO3/miR-21/SPRY2 axis. Am J Transl Res. 2021 Oct 15;13(10):11209-11222. eCollection 2021.
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Ref 18 N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2346-9. doi: 10.1016/j.bmcl.2009.02.029. Epub 2009 Feb 12.
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Ref 28 Design, synthesis and preliminary biological evaluation of N-hydroxy-4-(3-phenylpropanamido)benzamide (HPPB) derivatives as novel histone deacetylase inhibitors. Eur J Med Chem. 2009 Nov;44(11):4470-6. doi: 10.1016/j.ejmech.2009.06.010. Epub 2009 Jun 17.
Ref 29 Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides. Bioorg Med Chem Lett. 2004 May 17;14(10):2477-81. doi: 10.1016/j.bmcl.2004.03.012.
Ref 30 Development of Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Signaling Pathway.J Med Chem. 2019 Feb 28;62(4):1715-1730.
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Ref 33 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 34 ClinicalTrials.gov (NCT00130728) A Study to Evaluate the Efficacy of Bevacizumab in Combination With Tarceva for Advanced Non-Small Cell Lung Cancer
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Ref 36 ClinicalTrials.gov (NCT02198274) Intravenous BIBH 1 in Patients With Metastatic Colorectal Cancer. U.S. National Institutes of Health.
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Ref 45 ClinicalTrials.gov (NCT02726334) A Phase I, Dose Escalation Study of BNC101 in Patients With Metastatic Colorectal Cancer.. U.S. National Institutes of Health.
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Ref 48 Phase II Study of Saracatinib (AZD0530) in Patients With Previously Treated Metastatic Colorectal Cancer. Invest New Drugs. 2015 Aug;33(4):977-84.
Ref 49 Design and development of antisense drugs. Expert Opin. Drug Discov. 2008 3(10):1189-1207.