Chemical Structure : PP-C8
CAS No.:
3032108-74-7
PP-C8
(CDK12-cyclin K degrader)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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866.96
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Formula
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C43H51FN12O7
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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]-
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References
1. Tian Niu, et al. Eur J Med Chem. 2022 Jan 15;228:114012.
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