GSK2643943A

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

GSK2643943A 是一种靶向 USP20 的去泛素化酶 (DUB) 抑制剂。GSK2643943A 对 USP20/Ub-Rho 具有亲和力, 其 IC50 值为 160 nM。GSK2643943A 具有抗肿瘤作用，可用于口腔鳞状细胞癌 (OSCC) 的研究。

GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .

Cell Viability Assay Cell Line:SCC9 cells Concentration:1 μM, 5 μM (GSK+0.01 MOI T1012) 1 μM (GSK+0.01 MOI/ 1 MOI T1012)Incubation Time:overnight Result:Displayed a significant drop in viability (R50%) (5 μM GSK+0.01 MOI T1012 infection) and 50% loss of SCC9 viability (1 μM GSK+0.01 MOI T1012 infection) .Remarkably reduced the viability of SCC9 upon exposure to 1 MOI T1012G infection.Western Blot Analysis Cell Line:SCC9 cells Concentration:1 μM Incubation Time:3h, 9 h and 20 h Result: Generally up-regulated the expression of viral proteins at various phases.RT-PCR Cell Line:SCC9 cells Concentration:1 μM Incubation Time:9 h Result: Significantly increased the accumulation of viral ICP8 and VP16 Mrna in SCC9 cells.

Animal Model:The subcutaneous xenograft model.(SCC9 or SCC7 cells (8×106 cells or 1×106 cells), 5-week-old, female, BALB/c nude mice or C3H/HeN mice, four groups, n = 6-7, per group)Dosage:5 mg/kg Administration: GSK2643943A (alone): intraperitoneal administration, daily, for 6 days.GSK2643943A (combination): intraperitoneal administration, daily for 6 days + intratumoral injection with 50 mL of 1×106PFU T1012G in PBS on day 1, day 4, and day 7.Result:Caused a visible drop of tumor volumes and significantly reduced the tumor volumes in mice with combined treatment of GSK2643943A and oHSV-1 T1012G. Increased slightly viral ICP0 and gD mRNA accumulation in SCC9 tumors.Animal Model:The SCC7 mouse model.Dosage:2.5 mg/kg Administration:GSK2643943A (alone): intraperitoneal administration, daily, for 9 days. GSK2643943A (combination): intraperitoneal administration, daily, for 9 days + intratumoral injection, with 50 mL of 1×107PFU T1012G in PBS on days 1, 4, 7, and 10.Result:Caused a visible drop of tumor volumes, significantly reduced in mice with combined treatment of GSK and oHSV-1 T1012G.Increased slightly viral ICP0 and gD mRNA accumulation in SCC7 tumors.

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Proteasome/Ubiquitin

DUB

DUB

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2449301-27-1

277.3

C17H12FN3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 125 mg/mL (450.78 mM )

Nc1[nH]c2cc(\C=C\c3cccc(F)c3)ccc2c1C#N

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(-20℃)

With Ice Pack

≥ 2 years