Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03296
[1], [2]
Histone modification H3K27ac EZH2 METTL3 Direct Enhancement m6A modification SRSF11 SRSF11 METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
m6A Target Serine/arginine-rich splicing factor 11 (SRSF11)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Histone modification (HistMod)
Epigenetic Regulator Histone-lysine N-methyltransferase EZH2 (EZH2) WRITER View Details
Regulated Target Histone H3 lysine 27 acetylation (H3K27ac) View Details
Downstream Gene METTL3 View Details
Crosstalk Relationship Histone modification  →  m6A Enhancement
Crosstalk Mechanism histone modification directly impacts m6A modification through modulating the level of m6A regulator
Crosstalk Summary METTL3 is required to maintain the features of GBM stem cells. When combined with TMZ, METTL3 silencing suppressed orthotopic TMZ-resistant xenograft growth in a cooperative manner. Mechanistically, TMZ induced a SOX4-mediated increase in chromatin accessibility at the METTL3 locus by promoting Histone H3 lysine 27 acetylation (H3K27ac) levels and recruiting RNA polymerase II. Moreover, METTL3 depletion affected the deposition of m6A on histone modification-related gene transcripts, such as EZH2, leading to nonsense-mediated mRNA decay. Silencing METTL3 or overexpressing dominant-negative mutant METTL3 suppressed the growth and self-renewal of Glioblastoma cells. Integrated transcriptome and MeRIP-seq analyses revealed that downregulating the expression of METTL3 decreased m6A modification levels of Serine/arginine-rich splicing factor 11 (SRSF11), which led to YTHDC1-dependent NMD of SRSF transcripts and decreased SRSF protein expression.
Responsed Disease Brain cancer ICD-11: 2A00
Pathway Response RNA degradation hsa03018
Cell Process mRNA decay
In-vitro Model
U-251MG Astrocytoma Homo sapiens CVCL_0021
U-87MG ATCC Glioblastoma Homo sapiens CVCL_0022
In-vivo Model Six-week-old female BALB/c nude mice were purchased from the Model Animal Research Center of Nanjing University and housed in individually ventilated micro-isolator cages under a 12 h dark/light cycle. Nude mice were divided into four groups of six mice each. After deep anesthesia, a 27-gauge needle was used to drill a burrhole into the skull 0.5 mm anterior and 2 mm lateral to the bregma. A 10 μ L gas-tight syringe (Hamilton) was then used to inject 10 μ L of the U87 MG-TMZ_R-luc cell suspension in the striatum at a depth of 3 mm from the dural surface. One week after the injection of the tumor cells, 40 mg/kg/day of TMZ in saline was administered for over 2 weeks by intraperitoneal injection. During TMZ treatment, a Xenogen IVIS Spectrum system was used to monitor the tumor growth. At the end point, brain tissues were dissected from the mice models and measured the length (a) and width (b) of the tumors. Tumor volume was calculated by the formula V = ab2/2.
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Histone-lysine N-methyltransferase EZH2 (EZH2) 74 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Tazemetostat Approved [3]
Synonyms
EPZ-6438; 1403254-99-8; EPZ6438; UNII-Q40W93WPE1; N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide; Q40W93WPE1; EPZ 6438; E7438; (1,1'-Biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2.5 nM
External Link
 Compound Name DS-3201b Phase 2 [4]
Synonyms
Valemetostat; 1809336-39-7; UNII-60RD0234VE; 60RD0234VE; 1809336-39-7 (free base); DS-3201; (2R)-7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide; Valemetostat 2HCl; Valemetostat [INN]; Valemetostat (DS-3201); CHEMBL4597193; EZH1/2 inhibitor DS-3201; SCHEMBL18393626; SCHEMBL18393627; SCHEMBL18639210; EX-A3423; DS3201; NSC813381; s8926; NSC-813381; HY-109108; CS-0039740; D11551
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CPI-1205 Phase 1/2 [5]
Synonyms
HPODOLXTMDHLLC-QGZVFWFLSA-N; 1621862-70-1; UNII-455J2479FY; CPI1205; CPI 1205; 455J2479FY; (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide; GTPL9115; SCHEMBL17329268; MolPort-044-560-382; KS-000006BA; EX-A1068; s8353; AKOS030628484; ZINC220982768; CS-7648; compound 13 [PMID: 27739677]; HY-100021; J3.556.402K; N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-1-[(1R)-1-[1-(2,2,2-trifluoroethyl)piperidin-4-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name SHR2554 Phase 1/2 [6]
MOA Inhibitor
External Link
 Compound Name CPI-0209 Phase 1/2 [7]
MOA Inhibitor
External Link
 Compound Name GSK2816126 Phase 1 [8]
Synonyms
GSK 126; GSK-126
    Click to Show/Hide
MOA Modulator
Activity Ki = 0.5 nM
External Link
 Compound Name PF-06821497 Phase 1 [9]
Synonyms
UNII-S4L4MM20B6; S4L4MM20B6; CHEMBL4080228; PF06821497; 1844849-10-0; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one; SCHEMBL17330426; GTPL10516; BDBM50246967; NSC800019; DB14799; HY-101571A; NSC-800019; compound 23a [PMID: 29211475]; CS-0092626; Q29209799; 1(2H)-Isoquinolinone, 5,8-dichloro-2-((1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl)-3,4-dihydro-7-((R)-methoxy-3-oxetanylmethyl)-; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one; CJD
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name DS-3201 Phase 1 [5]
Synonyms
QTGYNKYZRZATJB-UHFFFAOYSA-N; 701899-63-0; 2-(2-(2-Methyl-1H-imidazol-5-yl)ethyl)isoindoline-1,3-dione; 2-(2-(2-Methyl-1H-imidazol-5-yl)-ethyl)isoindoline-1,3-dione; SCHEMBL7743461; MolPort-035-945-474; MolPort-035-690-353; ZINC98086069; AKOS024459002; AKOS024262663; MCULE-2708350770; FCH4077443; AK158834; AX8292467; ST2403812; 2-[2-(2-methyl-1H-imidazol-5-yl)ethyl]-2,3-dihydro-1H-isoindole-1,3-dione
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name HH2853 Phase 1 [10]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-33 Patented [11]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
 Compound Name PMID28394193-Compound-Figure3bI Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-35 Patented [11]
MOA Inhibitor
Activity IC50 = 10 nM
External Link
 Compound Name PMID28394193-Compound-54 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-24 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-27 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-25 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-50 Patented [11]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
 Compound Name PMID28394193-Compound-47 Patented [11]
MOA Inhibitor
Activity IC50 = 2 nM; Ki < 1 nM
External Link
 Compound Name PMID28394193-Compound-21 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-41 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-53 Patented [11]
MOA Inhibitor
Activity IC50 = 80 nM
External Link
 Compound Name PMID28394193-Compound-Figure5aVIII Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-38 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-51 Patented [11]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
 Compound Name PMID28394193-Compound-31 Patented [11]
MOA Inhibitor
Activity IC50 = 20 nM
External Link
 Compound Name PMID28394193-Compound-42 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-15 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-52 Patented [11]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
 Compound Name PMID28394193-Compound-32 Patented [11]
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name PMID28394193-Compound-23 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-29 Patented [11]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
 Compound Name PMID28394193-Compound-30 Patented [11]
MOA Inhibitor
Activity IC50 = 16 nM
External Link
 Compound Name PMID28394193-Compound-39 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-49 Patented [11]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
 Compound Name PMID28394193-Compound-43 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-40 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-Figure3bIII Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-36 Patented [11]
MOA Inhibitor
Activity IC50 = 316 nM
External Link
 Compound Name PMID28394193-Compound-28 Patented [11]
MOA Inhibitor
Activity IC50 = 32 nM
External Link
 Compound Name PMID28394193-Compound-22 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-18 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-16 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-44 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-20 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-19 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-37 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-Figure3bII Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-26 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-17 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-34 Patented [11]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
 Compound Name PMID28394193-Compound-56 Patented [11]
MOA Inhibitor
Activity IC50 = 0.93 nM
External Link
 Compound Name PMID28394193-Compound-46 Patented [11]
MOA Inhibitor
Activity IC50 = 5 nM
External Link
 Compound Name PMID28394193-Compound-57 Patented [11]
MOA Inhibitor
Activity IC50 = 6.45 nM
External Link
 Compound Name PMID28394193-Compound-14 Patented [11]
MOA Inhibitor
Activity IC50 = 21900 nM
External Link
 Compound Name PMID28394193-Compound-12 Patented [11]
MOA Inhibitor
Activity IC50 < 10 nM
External Link
 Compound Name PMID26882240-Compound-1 Patented [12]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-55 Patented [11]
MOA Inhibitor
Activity IC50 = 8.13 nM
External Link
 Compound Name PMID28394193-Compound-45 Patented [11]
MOA Inhibitor
Activity IC50 = 168000 nM
External Link
 Compound Name PMID28394193-Compound-13 Patented [11]
MOA Inhibitor
Activity IC50 = 1470 nM
External Link
 Compound Name EPZ005687 Investigative [13]
Synonyms
EPZ-005687; EPZ 005687
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name EI1 Investigative [14]
Synonyms
KB-145943
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name UNC1999 Investigative [15]
Synonyms
UNC 1999; UNC-1999
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MS1943 Investigative [6]
Synonyms
2225938-17-8; SCHEMBL21271666; EX-A3962; s8918; HY-133129; CS-0112146; 6-(6-(4-(2-(2-((3r,5r,7r)-adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide; 6-(6-(4-(2-(2-(Adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide
    Click to Show/Hide
MOA Degrader
External Link
 Compound Name GSK343 Investigative [16]
Synonyms
compound 6 [PMID 24900432]; GSK 343
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 174 nM
External Link
 Compound Name PMID28394193-Compound-11 Patented [17]
External Link
 Compound Name PMID28394193-Compound-10 Patented [17]
External Link
 Compound Name PMID28394193-Compound-14 Patented [11]
MOA Inhibitor
Activity IC50 = 21900 nM
External Link
 Compound Name PMID28394193-Compound-12 Patented [11]
MOA Inhibitor
Activity IC50 < 10 nM
External Link
 Compound Name PMID28394193-Compound-13 Patented [11]
MOA Inhibitor
Activity IC50 = 1470 nM
External Link
 Compound Name PMID28394193-Compound-56 Patented [11]
MOA Inhibitor
Activity IC50 = 0.93 nM
External Link
 Compound Name PMID28394193-Compound-46 Patented [11]
MOA Inhibitor
Activity IC50 = 5 nM
External Link
 Compound Name PMID28394193-Compound-57 Patented [11]
MOA Inhibitor
Activity IC50 = 6.45 nM
External Link
 Compound Name PMID28394193-Compound-55 Patented [11]
MOA Inhibitor
Activity IC50 = 8.13 nM
External Link
 Compound Name PMID28394193-Compound-45 Patented [11]
MOA Inhibitor
Activity IC50 = 168000 nM
External Link
2A00: Brain cancer 53 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Zinostatin stimalamer Approved [18]
Synonyms
Smancs (TN)
    Click to Show/Hide
External Link
 Compound Name Motexafin gadolinium Approved [19]
Synonyms
Xcytrin; Gadolinium texaphyrin; GdT2B2; GD-Tex; Motexafin gadolinium (USAN); PCI-0120; Xcytrin (TN)
    Click to Show/Hide
External Link
 Compound Name Lomustine Approved [20]
Synonyms
Belustine; CCNU; CINU; Cecenu; CeeNU; Chloroethylcyclohexylnitrosourea; Lomustina; Lomustinum; Bristol Myers Squibb Brand of Lomustine; CCNU [Chloroethyl nitrosoureas]; Cyclohexyl chloroethyl nitrosourea; Lomustine medac Brand; Medac Brand of Lomustine; Rhone Poulenc Rorer Brand of Lomustine; OR5087; RB 1509; SRI 2200; Bristol-Myers Squibb Brand of Lomustine; CeeNU (TN); Lomustina [INN-Spanish]; Lomustinum [INN-Latin]; NPFAPI-06; Rhone-Poulenc Rorer Brand of Lomustine; CeeNU, CCNU, Lomustine; Lomustine (USAN/INN); Lomustine [USAN:BAN:INN]; N-(2-Chloroethyl)-N'-cyclohexyl-N-nitrosourea; (Chloro-2-ethyl)-1-cyclohexyl-3-nitrosourea; (Cloro-2-etil)-1-cicloesil-3-nitrosourea; (Cloro-2-etil)-1-cicloesil-3-nitrosourea [Italian];1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea; 1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea [Chloroethyl nitrosoureas]; 1-(2-Chloroethyl)-3-cyclohexylnitrosourea
    Click to Show/Hide
External Link
 Compound Name Borocaptate sodium B 10 Approved [18]
External Link
 Compound Name DTI-015 Approved [21]
Synonyms
Carmustine; 154-93-8; 1,3-Bis(2-chloroethyl)-1-nitrosourea; BCNU; Carmustin; Nitrumon; Carmubris; Gliadel; BiCNU; Bi CNU; Carmustinum; Bischlorethylnitrosurea; Bischlorethylnitrosourea; Carmustina; Becenun; Becenum; Bischloroethyl nitrosourea; N,N'-BIS(2-CHLOROETHYL)-N-NITROSOUREA; Bis(2-chloroethyl)nitrosourea; Urea, N,N'-bis(2-chloroethyl)-N-nitroso-; Gliadel Wafer; FDA 0345; Bischloroethylnitrosourea; SRI 1720; 1,3-Bis(2-chloroethyl)nitrosourea; BiCNU (TN); Carmustinum [INN-Latin]; Carmustina [INN-Spanish]; DTI 015; NCI-C04773; SK; Injectable carmustine, Direct Therapeutics
    Click to Show/Hide
External Link
 Compound Name Prinomastat Approved [22]
Synonyms
AG-3354; AG-3362; Prinomastat (USAN/INN); (3S)-N-hydroxy-2,2-dimethyl-4-(4-pyridin-4-yloxyphenyl)sulfonylthiomorpholine-3-carboxamide
    Click to Show/Hide
External Link
 Compound Name INO-1001 Phase 3 [23]
Synonyms
Hypoxanthine arabinoside; LT00454797; 9-[(3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-3H-purin-6-one
    Click to Show/Hide
External Link
 Compound Name GliAtak Phase 3 [24]
Synonyms
GliAtak (TN)
    Click to Show/Hide
External Link
 Compound Name SOT-107 Phase 3 [25]
Synonyms
TransMID
    Click to Show/Hide
External Link
 Compound Name ICT-107 Phase 3 [26]
External Link
 Compound Name Cintredekin besudotox Phase 3 [27]
External Link
 Compound Name Rindopepimut Phase 3 [28]
External Link
 Compound Name DCVax-Ovarian Phase 3 [29]
Synonyms
DCVax-L; Dendritic cell-based immunotherapy (ovarian cancer), Northwest Biotherapeutics
    Click to Show/Hide
External Link
 Compound Name DCVax-Brain Phase 3 [30]
Synonyms
Dendritic cell-based immunotherapy (brain cancer), Northwest Biotherapeutics
    Click to Show/Hide
External Link
 Compound Name TVI-Brain-1 Phase 2/3 [31]
External Link
 Compound Name NLG8189 Phase 2/3 [5]
Synonyms
1-Methyl-D-tryptophan; Indoximod; 110117-83-4; D-Tryptophan, 1-methyl-; D-1MT; Indoximod (NLG-8189); D-1-methyltryptophan; UNII-TX5CYN1KMZ; D-(+)-1-Methyltryptophan; TX5CYN1KMZ; (R)-2-amino-3-(1-methyl-1H-indol-3-yl)propanoic acid; (2R)-2-amino-3-(1-methylindol-3-yl)propanoic acid; NSC-721782; (2R)-2-amino-3-(1-methyl-3-indolyl)propanoic acid; 1-MT; (2R)-2-azanyl-3-(1-methylindol-3-yl)propanoic acid; (2R)-2-amino-3-(1-methyl-1H-indol-3-yl)propanoic acid; D-l-Methyltryptophan; Indoximod [USAN:INN]; NLG-8189; NLG 8189
    Click to Show/Hide
External Link
 Compound Name Synthetic survivin peptide vaccine Phase 2 [32]
External Link
 Compound Name Fresolimumab Phase 2 [33]
Synonyms
GC-1008
    Click to Show/Hide
External Link
 Compound Name DNX-2401 Phase 2 [34]
Synonyms
Tasadenoturev
    Click to Show/Hide
External Link
 Compound Name TVI-Brain-1 cancer vaccine Phase 2 [35]
External Link
 Compound Name PDT with Photofrin Phase 2 [5]
External Link
 Compound Name F18-ML-10 Phase 2 [36]
External Link
 Compound Name PT2385 Phase 2 [37]
Synonyms
ONBSHRSJOPSEGS-INIZCTEOSA-N; PT-2385; UNII-6O16716DXP; 1672665-49-4; 6O16716DXP; SCHEMBL16555810; ZINC230453533; AKOS030526641; HY-12867; PT2385,1672665-49-4, PT 2385,PT-2385; Benzonitrile, 3-(((1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl)oxy)-5-fluoro-; 3-{[(1s)-2,2-Difluoro-1-Hydroxy-7-(Methylsulfonyl)-2,3-Dihydro-1h-Inden-4-Yl]oxy}-5-Fluorobenzonitrile; 3-(((1S)-2,2-Difluoro-1-hydroxy-7-methanesulfonyl-2,3-dihydro-1hinden-4-yl)oxy)-5-fluorobenzonitrile; 79A
    Click to Show/Hide
External Link
 Compound Name ABT-414 Phase 2 [38]
External Link
 Compound Name CLR1404-I-124 Phase 1/2 [39]
External Link
 Compound Name DM-CHOC-PEN Phase 2 [40]
External Link
 Compound Name L-alanosine Phase 2 [41]
Synonyms
SDX-102
    Click to Show/Hide
External Link
 Compound Name APX005M Phase 2 [5]
External Link
 Compound Name WP-1066 Phase 1/2 [35]
Synonyms
WP1066; 857064-38-1; (S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide; WP 1066; UNII-63V8AIE65T; 63V8AIE65T; AK-99218; C17H14BrN3O; (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide; MLS006010178; SCHEMBL1315826; QCR-16; SCHEMBL1315831; GTPL7972; CHEMBL1923234; EX-A760; AOB1497; DTXSID50235007; MolPort-044-723-708; MolPort-023-219-149; ZINC13983221; AKOS016007983; WP1066/WP-1066; CS-2736; DB12679; 2-Propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-N-((1S)-1-phenylethyl)-, (2E)-; HY-15312
    Click to Show/Hide
External Link
 Compound Name Anti-EGFRvIII CAR transduced PBL Phase 1/2 [42]
External Link
 Compound Name RG6156 Phase 1 [43]
External Link
 Compound Name rhenium-186 Phase 1 [44]
Synonyms
(~186~Re)Rhenium; 14998-63-1; 186Re; DTXSID60933825; Q18882928; RHENIUM (186-RE); Rhenium Re-186; Rhenium, isotope of mass 186; Rhenium-186; RHENIUM-186 [WHO-DD]; UNII-ZU7F1ET6TM; ZU7F1ET6TM
    Click to Show/Hide
External Link
 Compound Name IGV-001 Phase 1 [45]
External Link
 Compound Name DA-3607 Phase 1 [46]
Synonyms
Ad-stTRAIL; TRAIL adenoviral gene therapy (cancer), Dong-A
    Click to Show/Hide
External Link
 Compound Name DC/I540/KLH vaccine Phase 1 [47]
Synonyms
HTERT:540-548; Telomerase: 540-548 peptide vaccine; DC/I540/KLH vaccine (cancer); Dendritic cell/hTERT peptide I540/keyhole limpet hemocyanin vaccine, Dana-Farber; DC/I540/KLH vaccine (cancer), Dana-Farber
    Click to Show/Hide
External Link
 Compound Name KX2-361 Phase 1 [48]
Synonyms
KX-02
    Click to Show/Hide
External Link
 Compound Name MR1-1 Phase 1 [49]
Synonyms
MR1-1KDEL; EGFR-specific immunotoxin, IVAX; Anticancer immunotoxin (EGFR-specific), IVAX
    Click to Show/Hide
External Link
 Compound Name INdoximod + temozolomide Phase 1 [35]
External Link
 Compound Name Anti-CD133-CAR vector-transduced T cells Phase 1 [50]
External Link
 Compound Name 8H9 Phase 1 [51]
External Link
 Compound Name CC-8490 Phase 1 [52]
External Link
 Compound Name Sitimagene ceradenovec Discontinued in Phase 3 [53]
Synonyms
Cerepro; EG-009; HSV thymidine kinase gene therapy, Ark
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External Link
 Compound Name Ranagengliotucel-T Discontinued in Phase 3 [54]
Synonyms
Glionix; Brain tumor vaccine, NovaRx; Antisense (TGFbeta) brain tumor vaccine, NovaRx
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External Link
 Compound Name Oncolysin S Discontinued in Phase 2 [55]
Synonyms
N901-bR
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External Link
 Compound Name Labradimil Discontinued in Phase 2 [56]
Synonyms
Cereport; Lobradimil; Receptor mediated permeabilizer; RMP 7; DRG-0182; RMP-7; N2-((S)-2-(L-Arginyl-L-prolyl-trans-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-L-prolinamido)-3-(p-methoxyphenyl)propyl)-L-arginine; (S-(R*,R*))-L-Arginyl-L-prolyl-trans-4-hydroxy-L-prolyl-3-(2-thienyl)-L-alanylglycyl-L-seryl-N-(2-((4-((aminoiminomethyl)amino)-1-carboxybutyl)amino)-1-((4-methoxyphenyl)methyl)ethyl)-L-prolinamide
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 Compound Name Brain tumor vaccine Discontinued in Phase 1 [57]
Synonyms
Brain cancer vaccine, IRC; Brain tumor vaccine, IRC; IR-850; Established cancer cell line therapy (brain cancer), IRC; GM-CSF vaccine (brain cancer), IRC
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 Compound Name PCNU Terminated [58]
Synonyms
NSC-95466
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 Compound Name 131I-81C6 Terminated [59]
Synonyms
Neuradiab; MAb-81C6; Iodine-131-81C6; Astatine-211-MAb-81C6; Iodine-131-MAb-81C6; Iodine-131-ch-81C6; Iodine-131-ch-81C6-F(ab)2; 211At-MAb-81C6
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 Compound Name NSD-551 Terminated [60]
Synonyms
BK channel activator (cancer), NeuroSearch/TopoTarget
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External Link
 Compound Name AGT-2000 Investigative [61]
Synonyms
Gene therapy (intravenous, brain cancer), ArmaGen
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External Link
 Compound Name NV.XOD.09 Investigative [62]
External Link
 Compound Name EDP-19 Investigative [62]
Synonyms
SiRNA (convection-enhanced delivery, brain tumor), Sheba Medical Center/BioLineRx
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External Link
 Compound Name MIQ-004 Investigative [62]
Synonyms
M-IQ-004
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