PP-C8 | CDK12 PROTAC | Probechem Biochemicals

Chemical Structure : PP-C8

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PP-C8 (CDK12-cyclin K degrader)

货号: PC-24233Not For Human Use, Lab Use Only.

PP-C8 is a potent, selective CDK12-cyclin K complex PROTAC degrader with DC50 of DC50 of 416 nM and 412 nM for CDK12 and CycK protein levels respectively, does not affect CDK13.

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生物&药学活性

PP-C8 is a potent, selective CDK12-cyclin K complex PROTAC degrader with DC50 of DC50 of 416 nM and 412 nM for CDK12 and CycK protein levels respectively, does not affect CDK13.
PP-C8 induces profound degradation of cyclin K simultaneously and downregulates the mRNA level of DNA-damage response genes.
PP-C8-induced CDK12-CycK degradation does not change the overall phosphorylation level of RNAPII CTD Ser2.
PP-C8 mediated CDK12-CycK complex degradation is cereblon and UPS-dependent PROTAC-MOA.
PP-C8 down-regulates the DDR related genes expression through CDK12/cyclin K complex degradation.
PP-C8 induced CDK12-Cyclin K degradation demonstrates superior synergistic antiproliferative activity with the PARP inhibition.

物理化学性质&存储条件

分子量	866.96
分子式	C43H51FN12O7
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	Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[8-[[6-fluoro-2-[[[9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]amino]methyl]-1H-benzimidazol-5-yl]amino]octyl]-

参考文献

1. Tian Niu, et al. Eur J Med Chem. 2022 Jan 15;228:114012.

PP-C8 (CDK12-cyclin K degrader)

生物&药学活性

物理化学性质&存储条件

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PP-C8 (CDK12-cyclin K degrader)

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物理化学性质&存储条件

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