m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT00205
 [1], [2], [3]
m6A modification ADAR1 ADAR1 METTL3 Methylation : m6A sites Direct Enhancement RNA modification CDK4 CDK4 ADAR Methylation : modification sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
 Regulator Info 
m6A Target Interferon-inducible protein 4 (ADAR1)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type RNA modification (RNAMod)  >> Adenosine-to-Inosine editing (A-to-I)
Epigenetic Regulator Interferon-inducible protein 4 (ADAR1) WRITER View Details
Regulated Target Cyclin-dependent kinase 4 (CDK4) View Details
Crosstalk Relationship m6A  →  A-to-I Enhancement
Crosstalk Mechanism m6A modification directly impacts RNA modification through modulating the expression level of RNA modification regulator
Crosstalk Summary METTL3 methylates Interferon-inducible protein 4 (ADAR1) mRNA, thereby enhancing its protein expression, which subsequently promotes ADAR mediated A-to-I RNA editing of the Cyclin-dependent kinase 4 (CDK4) transcript.
Responsed Drug Palbociclib
 Drug Info 
Pathway Response mRNA surveillance pathway hsa03015
RNA degradation hsa03018
Cell Process RNA stability
In-vitro Model
 MGG8 Glioblastoma Homo sapiens CVCL_D1H4
U-87MG ATCC Glioblastoma Homo sapiens CVCL_0022
U-118MG Astrocytoma Homo sapiens CVCL_0633
CFPAC-1 Cystic fibrosis Homo sapiens CVCL_1119
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Cyclin-dependent kinase 4 (CDK4) 62 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Palbociclib Approved [4]
Synonyms
571190-30-2; PD0332991; PD-0332991; Ibrance; PD 0332991; UNII-G9ZF61LE7G; Palbociclib(PD0332991); 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(piperazin-1-yl)pyridin-2-yl]amino]-8H-pyrido[2,3-d]pyrimidin-7-one; 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one; G9ZF61LE7G; PD 332991; 6-ACETYL-8-CYCLOPENTYL-5-METHYL-2-[(5-PIPERAZIN-1-YLPYRIDIN-2-YL)AMINO]PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE; LQQ; PD 332991, PD 0332991, PD0332991; 6-Acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-ylpyridin-2-ylamino)-8H-pyrido(2,3-d)pyrimidin-7-one; 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one; HMR-2934
    Click to Show/Hide
MOA Modulator
Activity IC50 = 9 nM
External Link
CID: 5330286
TTD: D00UZR
DrugBank: DB09073
 Compound Name Ribociclib Succinate Approved [5]
Synonyms
1374639-75-4; LEE011 succinate; LEE011 (succinate); UNII-BG7HLX2919; LEE011-BBA; Ribociclib succinate [USAN]; BG7HLX2919; Kisqali (TN); Ribociclib succinate (USAN); LEE-011 succinate; SCHEMBL2684999; EX-A1586; HY-15777B; 1374639-75-4 (succinate); AKOS030526460; CS-2277; ACN-040739
    Click to Show/Hide
MOA Modulator
External Link
CID: 57334219
TTD: D01HVT
 Compound Name LY2835219 Approved [6]
Synonyms
Abemaciclib; 1231929-97-7; Verzenio; LY-2835219; UNII-60UAB198HK; LY2835219 (free base);
    Click to Show/Hide
MOA Modulator
Activity IC50 = 2 nM
External Link
CID: 46220502
TTD: D05SBO
DrugBank: DB12001
 Compound Name Trilaciclib Approved [7]
Synonyms
G1T28; 1374743-00-6; Trilaciclib [USAN]; G1T28(Trilaciclib); GTPL9626; CHEMBL3894860; SCHEMBL10082028; BDBM253928; US9464092, T; HY-101467; CS-0021431; 2'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'H-spiro(cyclohexane-1,9'-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one; Spiro(cyclohexane-1,9'(6'H)-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one, 7',8'-dihydro-2'-((5-(4-methyl-1-piperazinyl)-2-pyridinyl)amino)-; 2-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]spiro[7,8-dihydropyra
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 68029831
TTD: D0AP9E
DrugBank: DB15442
 Compound Name Apremilast Approved [8]
Synonyms
Apremilast (USAN); CC-10004; N-[2-[1-(3-ethoxy-4-methoxy-phenyl)-2-methylsulfonyl-ethyl]-1,3-dioxo-isoindol-4-yl]acetamide
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 11561674
TTD: D07ESC
DrugBank: DB05676
 Compound Name LEE011 Phase 3 [9]
Synonyms
Ribociclib; 1211441-98-3; LEE-011; Kisqali; Ribociclib(LEE011); UNII-TK8ERE8P56; LEE 011; 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide; TK8ERE8P56; Ribociclib (LEE011); AK174906; 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide; 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo [2,3-d]pyrimidine-6-carboxylic acid dimethylamide; Ribociclib [USAN:INN]; LEE011A; Tube013
    Click to Show/Hide
MOA Modulator
Activity IC50 = 2 nM
External Link
CID: 44631912
TTD: D08MXP
DrugBank: DB11730
 Compound Name P-276 Phase 2 [10]
Synonyms
CDK4 inhibitor (cancer), Nicholas Piramal; P-664-02; CDK4 inhibitor (iv, cancer), Piramal Life Sciences; CDK4 inhibitor(iv, cancer), NPIL Research & Development
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 23643976
TTD: D0W8IY
 Compound Name G1T38 Phase 2 [11]
Synonyms
YPJRHEKCFKOVRT-UHFFFAOYSA-N; SCHEMBL16036885; CHEMBL3904602; BDBM253941; US9464092, GG; 1628256-23-4
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 86269224
TTD: D0WU1O
 Compound Name Ro 31-7453 Phase 2 [12]
Synonyms
Bisindolylmaleimide deriv. 44; MKC-1; Ro-31-7453; 3-(1-methylindol-3-yl)-4-(1-methyl-6-nitroindol-3-yl)pyrrole-2,5-dione
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 5327686
TTD: D01UMT
DrugBank: DB05608
 Compound Name P276-00 Phase 2 [13]
Synonyms
CHEMBL2312181; SCHEMBL1180418
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 23643975
TTD: D05IRT
 Compound Name GLR2007 Phase 1/2 [14]
MOA Inhibitor
External Link
TTD: D4IS0G
 Compound Name FCN-437 Phase 1/2 [15]
MOA Inhibitor
External Link
TTD: D8ZV2Q
 Compound Name NUV-422 Phase 1/2 [16]
MOA Inhibitor
External Link
TTD: D70HZT
 Compound Name P1446A-05 Phase 1 [13]
MOA Inhibitor
Activity IC50 < 100 nM
External Link
CID: 67409219
TTD: D0DX4J
DrugBank: DB15157
 Compound Name PF-07220060 Phase 1 [17]
MOA Inhibitor
External Link
TTD: DZJ3D5
 Compound Name G1T28-1 Phase 1 [6]
MOA Modulator
External Link
TTD: D01XZG
 Compound Name AG-024322 Phase 1 [13]
Synonyms
AG-24322; N-[[5-[(3E)-3-(4,6-difluorobenzimidazol-2-ylidene)-1,2-dihydroindazol-5-yl]-4-methylpyridin-3-yl]methyl]ethanamine
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 135413565
TTD: D0IX4B
DrugBank: DB13035
 Compound Name PHA-793887 Phase 1 [10]
Synonyms
Cyclin-dependent kinase inhibitor (cancer), Nerviano
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 46191454
TTD: D0P1CV
DrugBank: DB12686
 Compound Name RGT-419B Phase 1 [18]
MOA Inhibitor
External Link
TTD: DYH94Z
 Compound Name FN-1501 Phase 1 [19]
Synonyms
1429515-59-2; CHEMBL4077071; UNII-6MC966B505; TQR1001; BDBM50270304; NSC781143; 6MC966B505; NSC-781143; HY-111361; CS-0039834; 4((7HPyrrolo[2,3d]pyrimidin-4-yl)amino)N(4-((4-methylpiperazin-1-yl)methyl)phenyl)1Hpyrazole-3-carboxamide; 4-((7H-Pyrrolo (2,3-d)pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide; 4-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-5-carboxamide; 4a?(7Ha'Pyrrolo[2,3a'd]pyrimidin-4-yl)amino)a'Na?4-((4-methylpiperazin-1-yl)methyl)phenyl)a?Ha'pyrazole-3-carboxamide; N-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamide
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 72195175
TTD: DKCU40
 Compound Name RGB-286638 Phase 1 [10]
Synonyms
GPC-286199; RGB-286199; RGB-344064; Non-selective CDK inhibitors, Agennix; Non-selective CDK inhibitors, GPC Biotech; Non-selective cyclin dependent kinase inhibitors, Agennix; Non-selective cyclin dependent kinase inhibitors, GPC Biotech
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 11285001
TTD: D03DKV
 Compound Name Imidazo pyridine derivative 3 Patented [20]
Synonyms
PMID26161698-Compound-22
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3 nM
External Link
CID: 46937330
TTD: D0WT7D
 Compound Name Palbociclib/ribociclib analog 1 Patented [20]
Synonyms
PMID26161698-Compound-4
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 89798202
TTD: D03HED
 Compound Name Pyrrolo[2,3-d]pyrimidine derivative 10 Patented [20]
Synonyms
PMID26161698-Compound-2
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3 nM
External Link
CID: 53378895
TTD: D04AKA
 Compound Name PMID26161698-Compound-17 Patented [20]
MOA Inhibitor
External Link
CID: 739323
TTD: D0FQ6V
 Compound Name Pyrrolo[2,3-d]pyrimidine derivative 9 Patented [20]
Synonyms
PMID26161698-Compound-1
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 1 nM
External Link
CID: 44818950
TTD: D08KKC
 Compound Name PMID25726713-Compound-49 Patented [21]
MOA Inhibitor
Activity IC50 < 50 nM
External Link
TTD: D07TVO
 Compound Name PMID25726713-Compound-51 Patented [21]
MOA Inhibitor
Activity IC50 < 50 nM
External Link
TTD: D0KH7Q
 Compound Name Indole-based analog 13 Patented [20]
Synonyms
PMID26161698-Compound-20
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 73293
TTD: D0LX6X
 Compound Name Isoquinoline 1,3-dione derivative 1 Patented [20]
Synonyms
PMID26161698-Compound-49
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4 nM
External Link
TTD: D0W4MN
 Compound Name PMID25726713-Compound-48 Patented [21]
MOA Inhibitor
Activity IC50 < 50 nM
External Link
TTD: D0WJ3W
 Compound Name PMID25726713-Compound-47 Patented [21]
MOA Inhibitor
Activity IC50 < 50 nM
External Link
TTD: D0X5VI
 Compound Name PMID25726713-Compound-50 Patented [21]
MOA Inhibitor
Activity IC50 < 50 nM
External Link
TTD: D0Y8JF
 Compound Name PMID25991433-Compound-A1 Patented [22]
MOA Inhibitor
Activity IC50 = 910 nM
External Link
TTD: D0H4HD
 Compound Name Oxazolyl methylthiothiazole derivative 1 Patented [20]
Synonyms
PMID26161698-Compound-52
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 100 nM
External Link
CID: 25195503
TTD: D0M5DX
 Compound Name BAY 10-00394 Discontinued in Phase 2 [10]
Synonyms
roniciclib; BAY 1000394; KB-145902; 1223498-69-8; Tube010; SCHEMBL875845; GTPL7874
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 45380979
TTD: D0NV9O
 Compound Name R547 Discontinued in Phase 1 [13]
Synonyms
LIA; R-547; [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 6918852
TTD: D04FHB
DrugBank: DB08094
 Compound Name ZK 304709 Discontinued in Phase 1 [13]
Synonyms
1010440-84-2; ZK CDK; UNII-87GI98VT0I; SCHEMBL955299; 87GI98VT0I; DTXSID20143701
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 59733314
TTD: D00VBT
 Compound Name INOC-005 Preclinical [10]
Synonyms
Capridine beta (prostate cancer), Prostagenics
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D07ZJC
 Compound Name CYC-103 Terminated [10]
Synonyms
Cyclin groove inhibitors, Cyclacel; CYC-103 (Pimetics series); CYC-103 cyclin groove inhibitors, Cyclacel; CYC-103 program, Cyclacel
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0Y6HA
 Compound Name PD-0183812 Terminated [23]
Synonyms
PETCVZZPKYJZAU-UHFFFAOYSA-N; PD183812; AC1NS8PJ; CHEMBL139653; SCHEMBL5268115; BDBM6280; PD 0183812; N8 Pyrido[2,3-d]pyrimidin-7-one deriv 72; 8-{bicyclo[221]heptan-2-yl}-2-({4-[4-(3-hydroxypropyl)piperidin-1-yl]phenyl}amino)-7H,8H-pyrido[2,3-d]pyrimidin-7-one; 8-(3-bicyclo[221]heptanyl)-2-[4-[4-(3-hydroxypropyl)piperidin-1-yl]anilino]pyrido[2,3-d]pyrimidin-7-one; PD0183813
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 20 nM
External Link
CID: 5330258
TTD: D0Z0KD
 Compound Name N-(2-(1H-Indol-3-yl)ethyl)biphenyl-4-carboxamide Investigative [24]
Synonyms
CHEMBL521733; N-[2-(1H-indol-3-yl)ethyl]biphenyl-4-carboxamide; AC1LG1FS; Oprea1_829316; Oprea1_192683; MolPort-001-987-537; ZINC285233; STK129364; BDBM50272836; AKOS000554028; MCULE-1062167425; NCGC00304458-01; BAS 03049800; ST45172084; AB01300868-01; N-[2-(1H-indol-3-yl)ethyl]-4-phenylbenzamide; N-(2-indol-3-ylethyl)(4-phenylphenyl)carboxamide; Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-amide
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 787236
TTD: D03VDM
 Compound Name 1-(1H-Indazol-6-yl)-3-pyridin-2-yl-urea Investigative [25]
Synonyms
Diarylurea deriv. 14a; AC1NS9HT; BDBM6656; CHEMBL143759; ZINC13471116; AKOS027814075; 3-1H-indazol-6-yl-1-pyridin-2-ylurea; 1-(1H-indazol-6-yl)-3-pyridin-2-ylurea; N-(1H-Indazol-6-yl)-N -pyridin-2-ylurea
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 5330597
TTD: D0G4JS
 Compound Name 1-(7-Hydroxy-naphthalen-1-yl)-3-pyridin-2-yl-urea Investigative [25]
Synonyms
Diarylurea deriv. 14; AC1NS9HN; CHEMBL140624; BDBM6654; ZINC13471112; 1-(7-Hydroxy-1-naphthyl)-3-(2-pyridyl)urea; N-(7-Hydroxy-1-naphthyl)-N -pyridin-2-ylurea; 1-(7-hydroxynaphthalen-1-yl)-3-pyridin-2-ylurea
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 5330595
TTD: D0M8CO
 Compound Name 1-Pyridin-2-yl-3-quinolin-5-yl-urea Investigative [25]
Synonyms
Diarylurea deriv. 14b; AC1NS9HW; BDBM6657; CHEMBL143704; ZINC13471117; 1-pyridin-2-yl-3-quinolin-5-ylurea; 3-pyridin-2-yl-1-quinolin-5-ylurea; 1-(5-Quinolyl)-3-(2-pyridyl)urea; N-Pyridin-2-yl-N -quinolin-5-ylurea
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 5330598
TTD: D0T2VG
 Compound Name 1-(9-Oxo-9H-fluoren-4-yl)-3-pyridin-2-yl-urea Investigative [25]
Synonyms
Diarylurea deriv. 15; AC1NS9HQ; BDBM6655; CHEMBL140589; SCHEMBL12856374; ZINC13471114; 1-(9-oxofluoren-4-yl)-3-pyridin-2-ylurea; 3-(9-oxo-9H-fluoren-4-yl)-1-pyridin-2-ylurea; 1-(9-Oxo-9H-fluorene-4-yl)-3-(2-pyridyl)urea; N-(9-Oxo-9H-fluoren-4-yl)-N -pyridin-2-ylurea
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 5330596
TTD: D0X1NW
 Compound Name Cdk4 inhibitor III Investigative [26]
Synonyms
Ryuvidine; 265312-55-8; CHEMBL290904; 2-Methyl-5-[(4-methylphenyl)amino]benzothiazole-4,7-dione; 5-(N-(4-Methylphenyl)amino)-2-methyl-4,7-dioxobenzothiazole; 2-methyl-5-(4-methylanilino)-1,3-benzothiazole-4,7-dione; AC1Q6BBC; AC1LA59T; 2-Methyl-5-p-tolylamino-benzothiazole-4,7-dione; SCHEMBL2169284; GTPL5952; CTK4F8075; CHEBI:92119; AOB6479; MolPort-023-276-509; HMS3269F11; HMS3229E08; ZINC5930916; BDBM50086655; 2-METHYL-5-[(4-METHYLPHENYL)AMINO]-4,7-BENZOTHIAZOLEDIONE; AKOS024457195; CCG-206830
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 6000 nM
External Link
CID: 481747
TTD: D07HPE
 Compound Name Fascaplysin Investigative [23]
Synonyms
Pyrido[1,2-a:3,4-b']diindol-5-ium,12,13-dihydro-13-oxo-, chloride; GNF-PF-1458; ACMC-20bu3v; AC1L2JLY; AC1Q6JA3; SCHEMBL1728912; CHEMBL602937; GTPL5969; BDBM59087; CTK4A8872; CHEBI:93765; ZINC1616841; pyrido[1,2-a:3,4-b']diindol-5-ium, 12,13-dihydro-13-oxo-; HSCI1_000331; NCGC00346951-01; CJ-26101; BRD-K13287209-003-03-2; BRD-K13287209-311-02-1; BRD-K13287209-311-01-3; BRD-K13287209-003-02-4; BRD-K13287209-003-01-6
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 350 nM
External Link
CID: 73292
TTD: D09OAH
 Compound Name Ro-0505124 Investigative [27]
Synonyms
RO0505124
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 9911652
TTD: D09RYV
 Compound Name NSC-625987 Investigative [28]
Synonyms
NSC 625987
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 3004085
TTD: D0VD8B
 Compound Name 10-hydroxy-18-methoxybetaenone Investigative [29]
Synonyms
CHEMBL498247; BDBM50269144
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 10644450
TTD: D0W6CE
 Compound Name PYRAZOLOPYRIDAZINE 1 Investigative [30]
Synonyms
551920-54-8; GW810576X; n-(3-methoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine; pyrazolo[1,5-b]pyridazine deriv. 19; AC1O6ZIQ; CHEMBL187081; BDBM8128; SCHEMBL4489357; CTK1F7320; DTXSID60424889; HMS3305F24; HMS3303K24; ZINC13582569; NCGC00242229-01; DA-42106; FT-0707969; AB01092291-01; 2-Pyrimidinamine, N-(3-methoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-yl-; N-(3-methoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 60 nM
External Link
CID: 6539361
TTD: D02DLC
 Compound Name K00024 Investigative [31]
Synonyms
indolocarbazole deriv. 4(d)
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 5330797
TTD: D0D5HQ
 Compound Name PYRAZOLOPYRIDAZINE 2 Investigative [30]
Synonyms
pyrazolo[1,5-b]pyridazine deriv. 25; AC1O6ZJ2; BDBM8134; CHEMBL186054; N-(3,4-dimethoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 190 nM
External Link
CID: 6539367
TTD: D0O0VP
 Compound Name PMID18986805C9b Investigative [32]
Synonyms
GTPL8160; BDBM50246396; ZINC38224644
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 50 nM
External Link
CID: 11675054
TTD: D0P6JS
 Compound Name NU-6102 Investigative [33]
Synonyms
nu6102; 444722-95-6; NU 6102; O6-CYCLOHEXYLMETHOXY-2-(4'-SULPHAMOYLANILINO) PURINE; Cdk1/2 Inhibitor II, NU6102; 6-Cyclohexylmethoxy-2-(4&amp; -sulfamoylanilino)purine; 4-{[6-(cyclohexylmethoxy)-9H-purin-2-yl]amino}benzenesulfonamide; 4SP; 1h1s; 4-[[6-(cyclohexylmethoxy)-7H-purin-2-yl]amino]benzenesulfonamide; 4-{[6-(cyclohexylmethoxy)-7h-purin-2-yl]amino}benzenesulfonamide; 4-[[6-(cyclohexylmethoxy)-9h-purin-2-yl]amino]benzenesulfonamide; 4eor; 4eok; 2iw9; 2c6o; 2iw8; AC1L1IGA; SCHEMBL2170816; CHEMBL319467
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1600 nM
External Link
CID: 4566
TTD: D0Y5RO
DrugBank: DB07126
 Compound Name NU6140 Investigative [34]
Synonyms
Cdk2 Inhibitor IV, NU6140; 444723-13-1; NU 6140; CHEMBL1802728; 4-(6-Cyclohexylmethoxy-9H-purin-2-ylamino)-N,N-diethylbenzamide; 4-{[6-(cyclohexylmethoxy)-7H-purin-2-yl]amino}-N,N-diethylbenzamide; Cdk2 inhibitor IV; SCHEMBL2169233; GTPL5949; CTK8E7940; DTXSID30436732; MolPort-023-276-742; MolPort-044-561-419; HMS3229E18; IN1369; ZINC22309248; BDBM50347924; AKOS024457537; CCG-206836; NCGC00370819-01; NU6140, &gt; RT-011957; 4-(6-cyclohexylmethoxy-9hpurin-2-ylamino)-N,N-diethyl-benzamide
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 10202471
TTD: D04WFN
 Compound Name 3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Investigative [35]
Synonyms
CHEMBL380598; SCHEMBL3148490; HVQJGNALTWNDMX-UHFFFAOYSA-N; BDBM50375058; 2-(1H-Indole-3-yl)-3-phenylmaleimide
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 15422868
TTD: D06AOY
 Compound Name 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Investigative [35]
Synonyms
1H-Pyrrole-2,5-dione, 3,4-bis(4-methoxyphenyl)-; 108774-82-9; ACMC-20mbs9; CHEMBL381099; CTK0G2626; DTXSID90449388
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 10946795
TTD: D00NYT
 Compound Name 3,4-diphenyl-1H-pyrrole-2,5-dione Investigative [35]
Synonyms
2,3-diphenylmaleimide; 1H-Pyrrole-2,5-dione, 3,4-diphenyl-; 31295-36-0; AC1MBL6S; SCHEMBL114611; CHEMBL201949; CTK1B9880; 3,4-diphenylpyrrole-2,5-dione; DTXSID70372903; ZINC3847556
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 2752461
TTD: D0C3WY
 Compound Name 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Investigative [35]
Synonyms
CHEMBL372076; SCHEMBL3822337
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 11572699
TTD: D0EK0G
 Compound Name 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Investigative [36]
MOA Inhibitor
External Link
CID: 9859248
TTD: D0A5RM
References
Ref 1 N?-Methyladenosine Landscape of Glioma Stem-Like Cells: METTL3 Is Essential for the Expression of Actively Transcribed Genes and Sustenance of the Oncogenic Signaling. Genes (Basel). 2019 Feb 13;10(2):141. doi: 10.3390/genes10020141.
Ref 2 ADAR1 is a new target of METTL3 and plays a pro-oncogenic role in glioblastoma by an editing-independent mechanism. Genome Biol. 2021 Jan 28;22(1):51. doi: 10.1186/s13059-021-02271-9.
Ref 3 CircNEIL3 regulatory loop promotes pancreatic ductal adenocarcinoma progression via miRNA sponging and A-to-I RNA-editing. Mol Cancer. 2021 Mar 9;20(1):51. doi: 10.1186/s12943-021-01333-7.
Ref 4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2017
Ref 5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 6 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics. 2005 Aug;86(2):127-41. doi: 10.1016/j.ygeno.2005.04.008.
Ref 7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
Ref 8 Agreement signed with Prostagenics to develop prostate cancer treatment. Innovate Oncology, Inc. 2005.
Ref 9 Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82. doi: 10.1158/1078-0432.CCR-13-1675. Epub 2013 Sep 17.
Ref 10 Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154. doi: 10.1155/2011/483154. Epub 2010 Dec 27.
Ref 11 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 12 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
Ref 13 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. doi: 10.1038/nrd2907.
Ref 14 Clinical pipeline report, company report or official report of Gan & Lee Pharmaceuticals.
Ref 15 Clinical pipeline report, company report or official report of Fochon Pharmaceuticals.
Ref 16 ClinicalTrials.gov (NCT04541225) Phase 1/2 Dose Escalation, Safety, Pharmacokinetics, and Efficacy Study of NUV-422 in Adults With Recurrent or Refractory High-grade Gliomas and Solid Tumors. U.S.National Institutes of Health.
Ref 17 ClinicalTrials.gov (NCT04557449) Study to Test the Safety and Tolerability of PF-07220060 in Participants With Advance Solid Tumors (CDK4). U.S. National Institutes of Health.
Ref 18 Clinical pipeline report, company report or official report of Regor Therapeutics
Ref 19 Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. J Med Chem. 2018 Feb 22;61(4):1499-1518. doi: 10.1021/acs.jmedchem.7b01261. Epub 2018 Feb 12.
Ref 20 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014). Expert Opin Ther Pat. 2015;25(9):953-70. doi: 10.1517/13543776.2015.1045414. Epub 2015 Jul 13.
Ref 21 Hedgehog inhibitors: a patent review (2013 - present). Expert Opin Ther Pat. 2015 May;25(5):549-65. doi: 10.1517/13543776.2015.1019864. Epub 2015 Mar 1.
Ref 22 c-Jun N-terminal kinase inhibitors: a patent review (2010 - 2014). Expert Opin Ther Pat. 2015;25(8):849-72. doi: 10.1517/13543776.2015.1039984. Epub 2015 May 19.
Ref 23 Pharmacological inhibitors of cyclin-dependent kinases. Trends Pharmacol Sci. 2002 Sep;23(9):417-25. doi: 10.1016/s0165-6147(02)02071-0.
Ref 24 Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4. Bioorg Med Chem. 2008 Aug 15;16(16):7728-39. doi: 10.1016/j.bmc.2008.07.002. Epub 2008 Jul 8.
Ref 25 Structure-based generation of a new class of potent Cdk4 inhibitors: new de novo design strategy and library design. J Med Chem. 2001 Dec 20;44(26):4615-27. doi: 10.1021/jm0103256.
Ref 26 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. Bioorg Med Chem Lett. 2000 Mar 6;10(5):461-4. doi: 10.1016/s0960-894x(00)00014-7.
Ref 27 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1976).
Ref 28 The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4. Clin Cancer Res. 1999 Dec;5(12):4279-86.
Ref 29 Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases. J Nat Prod. 2000 Jun;63(6):739-45. doi: 10.1021/np9905259.
Ref 30 N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy. J Med Chem. 2004 Sep 9;47(19):4716-30. doi: 10.1021/jm040063i.
Ref 31 Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. J Med Chem. 2003 May 22;46(11):2027-30. doi: 10.1021/jm0256169.
Ref 32 Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6486-9. doi: 10.1016/j.bmcl.2008.10.075. Epub 2008 Oct 22.
Ref 33 Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. J Med Chem. 2006 Sep 7;49(18):5470-7. doi: 10.1021/jm060216x.
Ref 34 Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther. 2005 Sep;4(9):1328-37. doi: 10.1158/1535-7163.MCT-05-0022.
Ref 35 Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81. doi: 10.1021/jm0580297.
Ref 36 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9. doi: 10.1021/jm0605740.