Chemical Structure : Skp2-Cks1 inhibitor E35
CAS No.:
2254132-52-8
Skp2-Cks1 inhibitor E35
Catalog No.: PC-25478Not For Human Use, Lab Use Only.
Skp2-Cks1 inhibitor E35 is a potent small molecule inhibitor of S-phase kinase-associated protein 2 (Skp2), inhbits Skp2-Cks1 protein-protein interaction (PPI) with IC50 of 4.86 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Skp2-Cks1 inhibitor E35 is a potent small molecule inhibitor of S-phase kinase-associated protein 2 (Skp2), inhbits Skp2-Cks1 protein-protein interaction (PPI) with IC50 of 4.86 uM.
E35 directly engages Skp2 in living cells.
E35 directly breaks Skp2-Cks1 in pull-down assays and thermally stabilizes endogenous Skp2 in MGC-803 and PC-3 cells.
E35 significantly inhibits colony formation and migration, as well as arrested the cell cycle at the S-phase.
E35 markedly decreases the expression of Skp2, as well as increased the expression of its substrates p21 and p27.
E35 (25 and 50 mg/kg/2 day, intragastric administration for 21 days) showed an obvious inhibitory effect on MGC-803 xenograft mice without obvious toxicity.
Physicochemical Properties
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M.Wt
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457.35
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Formula
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C20H17BrN4O2S
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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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2-((4-bromobenzyl)thio)-7-(2,4-dimethoxyphenyl)-[1,2,4]triazolo[1,5-a]pyrimidine
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References
1. Kamel EM, et al. Eur J Pharmacol. 2025 Sep 6:178129.
2. Hu K, et al. J Med Chem. 2024 Sep 26;67(18):16435-16454.
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