GSK2643943A
目录号: PL01915 纯度: ≥98%
CAS No. :2449301-27-1
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中文名称
GSK2643943A
中文别名
2-氨基-6-(3-氟苯乙烯基)-1H-吲哚-3-腈
英文名称
GSK2643943A
英文别名
GSK2643943A;1H-​Indole-​3-​carbonitrile, 2-​amino-​6-​[2-​(3-​fluorophenyl)​ethenyl]​-;s6878;2-Amino-6-[(E)-2-(3-fluorophenyl)ethenyl]-1H-indole-3-carbonitrile;CID 137319705
Cas No.
2449301-27-1
分子式
C17H12FN3
分子量
277.30
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC 50 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) .
性状
Solid
IC50 & Target[1][2]
IC50: 160 nM (USP20/Ub-Rho)
体外研究(In Vitro)
GSK2643943A blocks the USP20-mediated cleavage of protein-ubiquitin bonds.
GSK2643943A (1 μM, 5 μM; overnight) renders SCC9 cells more susceptible to oHSV-1 induced oncolysis.
GSK2643943A (1μM) leds to a notable increase of virus yields in SCC9 with 0.01 MOI T1012G infection. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
GSK2643943A (5 mg/kg, i.p., daily, for 6 days) potentiates oHSV-1-induced oncolysis in SCC9 tumors.
GSK2643943A (2.5 mg/kg, i.p., daily, for 9 days) plays a regulatory role in oHSV-1 T1012G replication and oncolysis in SCC7 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Nishi Kumari, et al. Targeting the Ubiquitin Proteasome System in Cancer. Shahzad, Hafiz Naveed (2018). Neoplasm Targeting the Ubiquitin Proteasome System in Cancer. , 10.5772/intechopen.69560(Chapter 8).
[2]. Ruitao Lu, et al. USP18 and USP20 restrict oHSV-1 replication in resistant human oral squamous carcinoma cell line SCC9 and affect the viability of SCC9 cells. Mol Ther Oncolytics. 2021 Nov 11;23:477-487.
溶解度数据
In Vitro: DMSO : ≥ 125 mg/mL (450.78 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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