Chemical Structure : LC-K2CAin-3
CAS No.:
LC-K2CAin-3
Catalog No.: PC-25379Not For Human Use, Lab Use Only.
LC-K2CAin-3 is a potent, highly selective CDK2-Cyclin A2 protein-protein interaction (PPI) inhibitor with IC50 of 32.1 nM in HTRF assays.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
LC-K2CAin-3 is a potent, highly selective CDK2-Cyclin A2 protein-protein interaction (PPI) inhibitor with IC50 of 32.1 nM in HTRF assays.
LC-K2CAin-3 shows no significantly affecting the interactions of CDK2 with Cyclin E1, CDK1 with Cyclin B1, CDK9 with Cyclin T1, or those of CDK4 and CDK6 with Cyclin D3.
LC-K2CAin-3 binds to and stabilizes the A-loop, inducing conformational changes of A-loop and α-C-Helix, which are likely responsible for the disruption of the CDK2–Cyclin A2 interaction.
LC-K2CAin-3 suppresses the proliferation of melanoma cells (A2058 cell, IC50=5.93 uM), and trigger apoptosis and induce G2/M phase arrest, but markedly less effective in CDK2-low VMM5A cells (IC50 > 14 µM).
Physicochemical Properties
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M.Wt
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624.66
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Formula
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C27H34F2N6O7S
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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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methyl 3-(4-(3-((3-((1-(ethylsulfonyl)piperidin-4-yl)carbamoyl)-1H-pyrazol-4-yl)carbamoyl)-2,4-difluorophenyl)piperidin-1-yl)-3-oxopropanoate
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References
1. Sun G, et al. Angew Chem Int Ed Engl. 2025 Aug 19:e202513542.
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