产品
编 号：F618155
分子式：C17H12FN3
分子量：277.3
分子式：C17H12FN3
分子量：277.3
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2449301-27-1
产品详情
生物活性：
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) .
体内研究：
GSK2643943A (5 mg/kg，ip，每天，持续 6 天) 在 SCC9 肿瘤中增强 oHSV-1 诱导的溶瘤作用。 GSK2643943A (2.5 mg/kg，ip，每天，持续 9 天) 在 SCC7 细胞中的 oHSV-1 T1012G 复制和溶瘤作用中发挥调节作用。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.
体外研究：
GSK2643943A 阻断 USP20 介导的蛋白质-泛素键裂解。 GSK2643943A (1 μM、5 μM；过夜) 使 SCC9 细胞对 oHSV-1 诱导的溶瘤作用更敏感。 GSK2643943A (1 μM) 在感染 0.01 MOI T1012G 的 SCC9 中导致病毒产量显著增加。
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) .
体内研究：
GSK2643943A (5 mg/kg，ip，每天，持续 6 天) 在 SCC9 肿瘤中增强 oHSV-1 诱导的溶瘤作用。 GSK2643943A (2.5 mg/kg，ip，每天，持续 9 天) 在 SCC7 细胞中的 oHSV-1 T1012G 复制和溶瘤作用中发挥调节作用。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.
体外研究：
GSK2643943A 阻断 USP20 介导的蛋白质-泛素键裂解。 GSK2643943A (1 μM、5 μM；过夜) 使 SCC9 细胞对 oHSV-1 诱导的溶瘤作用更敏感。 GSK2643943A (1 μM) 在感染 0.01 MOI T1012G 的 SCC9 中导致病毒产量显著增加。
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