Skp2 inhibitor 1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Skp2 inhibitor 1(compound 14i) 是一种 Skp2 抑制剂，干扰 Skp2-Cks1 相互作用，IC50为 2.8 μM。Skp2 inhibitor 1 也具有抗癌活性。

Skp2 inhibitor 1 (compound 14i) is a potent and selective Skp2 inhibitor against the Skp2-Cks1 interaction with an IC50 of 2.8 μM. Skp inhibitor 1 exhibits anticancer activity.

Cell Viability Assay Cell Line:PC-3 , MGC-803 Concentration:0-10 μM Incubation Time:72 h Result:Against the Skp2?Cks1 interaction with an IC50 value of 2.8 μM, and against PC-3 and MGC-803 cells with IC50 values of 4.8 and 7.0 μM, respectively. Apoptosis Analysis Cell Line:PC-3 , MGC-803 Concentration:2.5 μM , 5 μM , 10 μM Incubation Time:0-48 h Result:Leaded to cell cycle S-phase arrest in a dose-dependent manner, and induced apoptosis in a dose-dependent manner, such as nuclear fragmentation, condensation, and cell shrinkage.Cell Proliferation Assay Cell Line:PC-3 , MGC-803 Concentration:0.5 μM , 1 μM , 2 μM Incubation Time:10 days Result:Inhibited colony-forming abilities in a dose-dependent manner.Cell Migration Assay Cell Line:PC-3 , MGC-803 Concentration:2.5 μM , 5 μM , 10 μM Incubation Time:48 h Result:Inhibited migration in a dose-dependent manner.Cell Invasion Assay Cell Line:PC-3 , MGC-803 Concentration:0.5 μM , 1 μM , 2 μM Incubation Time:48 h Result:Inhibited invasion in a dose-dependent manner.Western Blot Analysis Cell Line:PC-3 , MGC-803 Concentration:2.5 μM , 5 μM , 10 μM Incubation Time:0-48 h Result:Inhibited the protein levels of Skp2 in a dose-dependent manner, restored the expression of p21 and p27 in a time-dependent manner.

Animal Model:The xenograft models of PC-3 and MGC-803 cells in NOD-SCID mice.Dosage:10 mg/kg; 25 mg/kg, 50 mg/kg Administration:Intraperitoneal injection (i.p.) Result:Inhibited tumor growth without obvious toxicity, the tumor growth inhibition ratio was 55.68, 71.86, and 90.42% with 10, 25, and 50 mg/Kg/2 day, respectively.

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Other Targets

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2760612-63-1

406.91

C23H23ClN4O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (122.88 mM; 超声助溶 )

O=C(NC1CCN(C2=NC(C3=CC=CC=C3)=C(N=C2)C=4C=CC=CC4)CC1)CCl

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(-20℃)

With Ice Pack

≥ 2 years