Chemical Structure : YJZ5118
CAS No.:
YJZ5118
Catalog No.: PC-24231Not For Human Use, Lab Use Only.
YJZ5118 is a potent, highly selective covalent inhibitor of CDK12/13 with IC50 of 39.5/26.4 nM, respectively, demonstrates high selectivity over other CDKs.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
YJZ5118 is a potent, highly selective covalent inhibitor of CDK12/13 with IC50 of 39.5/26.4 nM, respectively, demonstrates high selectivity over other CDKs.
YJZ5118 potently suppresses VCaP cell growth with an IC50 value of 23.7 nM.
YJZ5118 covalently binds with Cys1039 of CDK12.
YJZ5118 (100 nM) inhibits the phosphorylation of RNA polymerase II at Ser2 in VCaP cells, also has significant inhibitory effects on the expression of downstream gene RAD51 and markedly increaseds apoptotic marker c-PARP.
YJZ5118 not only provokes Akt phosphorylation but also exhibits a synergistic antitumor effect when combined with Akt inhibitors.
Physicochemical Properties
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M.Wt
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620.80
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Formula
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C36H44N8O2
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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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N-(5-(3-Benzyl-1-((1R,4R)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)ureido)-2-(4-(dimethylamino)piperidin-1-yl)phenyl)acrylamide
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References
1. Yang J, et al. J Med Chem. 2025 Mar 13. doi: 10.1021/acs.jmedchem.5c00127.
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