General Information of the Drug (ID: M6APDG00571)
Name
DS-3201b
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
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Status
Phase 2
Structure
Formula
C26H34ClN3O4
InChI
1S/C26H34ClN3O4/c1-14-11-15(2)29-25(32)20(14)13-28-24(31)19-12-21(27)23-22(16(19)3)33-26(4,34-23)17-7-9-18(10-8-17)30(5)6/h11-12,17-18H,7-10,13H2,1-6H3,(H,28,31)(H,29,32)/t17?,18?,26-/m1/s1
InChIKey
SSDRNUPMYCFXGM-ZZHSESOFSA-N
PubChem CID
126481870
TTD Drug ID
DNM79H
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Enhancer of zeste homolog 2 (EZH2)
Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1)
In total 1 mechanisms lead to this potential drug response
Response Summary Enhancer of zeste homolog 2 (EZH2) is a therapeutic target for DS-3201b. The Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) has potential in affecting the response of DS-3201b through regulating the expression of Enhancer of zeste homolog 2 (EZH2). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Enhancer of zeste homolog 2 (EZH2) is a therapeutic target for DS-3201b. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of DS-3201b through regulating the expression of Enhancer of zeste homolog 2 (EZH2). [2], [3]
References
Ref 1 IGF2BP1 Promotes Proliferation of Neuroendocrine Neoplasms by Post-Transcriptional Enhancement of EZH2. Cancers (Basel). 2022 Apr 24;14(9):2121. doi: 10.3390/cancers14092121.
Ref 2 An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. doi: 10.1021/cb400133j. Epub 2013 Apr 24.
Ref 3 METTL3 Accelerates Breast Cancer Progression via Regulating EZH2 m(6)A Modification. J Healthc Eng. 2022 Mar 29;2022:5794422. doi: 10.1155/2022/5794422. eCollection 2022.