G9a degrader G9D-4 | G9a PROTAC | Probechem Biochemicals

Chemical Structure : G9a degrader G9D-4

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G9a degrader G9D-4 (G9D-4)

货号: PC-22748Not For Human Use, Lab Use Only.

G9D-4 is a first-in-class, potent, selective PRTOAC degrader of protein lysine methyltransferase G9a (EHMT2, KMT1C) with DC50 of 0.1 uM in PANC-1 cells, highly selective over GLP (DC50>10 uM).

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生物&药学活性

G9D-4 is a first-in-class, potent, selective PRTOAC degrader of protein lysine methyltransferase G9a (EHMT2, KMT1C) with DC50 of 0.1 uM in PANC-1 cells, highly selective over GLP (DC50>10 uM).
G9D-4 selectively and effectively reduced the H3K9me2 in a dose-dependent manner in PANC-1 cells, and has no effect on the methylation at other prominent lysine positions.
G9D-4 has no influence on the CRBN neo-substrates such as GSPT1 and CK1α.
G9a-G9D-4-CRBN ternary complex formation is necessary for G9a degradation, NEDD8-activating enzyme inhibitor MLN4924 and proteasome inhibitor MG132 also hinders the ability of G9D-4 to induce G9a degradation.
G9D-4 effectively inhibits cell growth against a panel pancreatic cancer cells: KP-4, PANC-1, ASPC-1, HPAF-II, Panc10.05, SW1990, Panc08.13, Panc04.03, Panc05.04, and Panc02.03, also inhibits 22Rv1 cell growth with IC50 of 9.9 uM.
G9D-4 (10 uM) caused significant induction of apoptosis in a dose- and time-dependent manner, with downregulation of H3K9me2 and the upregulation of γH2AX and cleaved PARP in PANC-1 cells.
G9D-4 sensitizes MRTX1133 against KRASG12D pancreatic cell lines.

物理化学性质&存储条件

分子量	936.21
分子式	C52H73N9O7
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(4-((2-cyclohexyl-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-yl)amino)piperidin-1-yl)-N-(8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)octyl)butanamide

参考文献

1. Yunkai Shi, et al. J Med Chem. 2024 Jul 23. doi: 10.1021/acs.jmedchem.4c01192.

G9a degrader G9D-4 (G9D-4)

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G9a degrader G9D-4 (G9D-4)

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物理化学性质&存储条件

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