BRD4 PROTAC 6b

Chemical Structure : BRD4 PROTAC 6b

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货号: PC-22990Not For Human Use, Lab Use Only.

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生物&药学活性

BRD4 PROTAC 6b is a potent, specific PROTAC degrader of BRD4 protein, suppresses BLBC cell growth by targeting BRD4, but not BRD2 and BRD3, for cereblon (CRBN)-mediated ubiquitination and proteasomal degradation.
Compound 6b (0.1 μM) induced time-dependent BRD4 degradation and degraded most BRD4 protein within 12 hours.
Compound 6b effectively inhibit multiple BLBC cell lines, with a marked decline in KLF5, c-Myc, SKP2, Bcl-2, and Bcl-XL levels, and increased levels of Bim, p21, and p27.
Compound 6b causes growth inhibition and cell cycle arrest in BLBC cell lines.
Compound 6b promotes BRD4 ubiquitination and degradation dependent on CRBN
Compound 6b significantly suppressed HCC1806 xenograft and UM1 patient-derived xenograft tumor growth in nude mice.

物理化学性质&存储条件

分子量	708.68
分子式	C37H30F2N6O7
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-(4-(2,3-difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)-4-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)butanamide

参考文献

1. Yanjie Kong, et al. Oncogene. 2024 Aug 20. doi: 10.1038/s41388-024-03121-1.

BRD4 PROTAC 6b

生物&药学活性

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BRD4 PROTAC 6b

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