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CDK inhibitor 24

Chemical Structure : CDK inhibitor 24

CAS No.:

CDK inhibitor 24

Catalog No.: PC-49076Not For Human Use, Lab Use Only.

CDK inhibitor 24 is a potent inhibitor of cyclin-dependent kinases (CDKs) with IC50 of 4/20/64 nM for CDK2/9/12, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CDK inhibitor 24 is a potent inhibitor of cyclin-dependent kinases (CDKs) with IC50 of 4/20/64 nM for CDK2/9/12, respectively.
CDK inhibitor 24 causes dephosphorylation of retinoblastoma protein and RNA polymerase II, leading to induction of apoptosis in cellular assays in lymphoma cell lines.
CDK inhibitor 24 also induces proteasome-dependent degradation of cyclin K both in vitro and in a patient-derived xenograft in vivo.
CDK inhibitor 24 has a dual mechanism of action, acting as a CDK inhibitor and as a molecular glue inducing an interaction between CDK12 and DDB1 that leads to polyubiquitination of cyclin K and its subsequent degradation.

Physicochemical Properties

M.Wt 420.539
Formula C21H24N8S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-(1H-pyrazol-1-yl)benzyl)-5-((2-aminoethyl)thio)-3-cyclobutyl-2H-pyrazolo[4,3-d]pyrimidin-7-amine

References

1. Radek Jorda, et al. J. Med. Chem. 2022.

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