HDAC7 PROTAC B14

Chemical Structure : HDAC7 PROTAC B14

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货号: PC-24640Not For Human Use, Lab Use Only.

HDAC7 PROTAC B14 is a potent, exceedingly selective HDAC7 PROTAC degrader with DC50 of 25.1 nM in NB4 cells.

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生物&药学活性

HDAC7 PROTAC B14 is a potent, exceedingly selective HDAC7 PROTAC degrader with DC50 of 25.1 nM in NB4 cells.
B14 induced the HDAC7 degradation in a concentration-dependent manner in both DHL6 and NB4 cells.
B14 (1 μmol/L) induced a significant reduction in HDAC7 protein level was observed, reaching over 85% degradation at 24 h.
B14 exhibited specific degradation selectivity for HDAC7 over other Class I HDACs (HDAC1, HDAC2, HDAC3, HDAC8), while Class IIb HDACs (HDAC6, HDAC10).
B14 also had limited influence on the degradation of neo-substrates such as SALL4, IKZF1/3 (IKZF3 was not detected in NB4 cells in both proteomics and immunoblotting analyses), and GSPT1 in DHL6 and NB4 cells.
B14 induced a concentration-dependent cell cycle arrest in the G0 phase in DHL6 and NB4 cells, markedly inhibited cell proliferation with IC50 of 1.00 and 0.84 uM respectively.

物理化学性质&存储条件

分子量	992.09
分子式	C51H52F3N9O7S
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	N-((1-(2-(1-(1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperidine-4-carbonyl)piperidin-4-yl)ethyl)-4-(4-phenylthiazol-2-yl)piperidin-4-yl)methyl)-3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)benzamide

参考文献

1. Yuheng Jin, et al. Acta Pharm Sin B. 2025 Mar;15(3):1659-1679.

HDAC7 PROTAC B14

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物理化学性质&存储条件

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HDAC7 PROTAC B14

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