GSK-872

CAS号

1346546-69-7

分子式

C19H17N3O2S2

主要靶点

RIP kinase

仅限科研使用

Cat No : CM06404

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Synonyms

cytoplasmic|deficits|edema|HMGB1|GSK 872|GSK872|GSK'872|GSK-872|GSK2399872A|brain|Receptor-interacting protein kinases|RIPkinase|RIPK|RIP3K|RIP kinase|neurological|Inhibitor|inhibit|translocation



产品信息

CAS号 1346546-69-7
分子式 C19H17N3O2S2
主要靶点 RIP kinase
主要通路 凋亡|NF-κB 信号通路
分子量 383.49
纯度 99.3%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 cytoplasmic|deficits|edema|HMGB1|GSK 872|GSK872|GSK'872|GSK-872|GSK2399872A|brain|Receptor-interacting protein kinases|RIPkinase|RIPK|RIP3K|RIP kinase|neurological|Inhibitor|inhibit|translocation

靶点活性

RIP3K:1.8 nM

体内活性

与未经治疗的缺血损伤相比,GSK872能显著降低HIF-1α表达[3]。

体外活性

GSK872(1 μM)对测试的大部分300种人类蛋白激酶均无抑制作用。它不能抑制RIP1激酶。在HT-29细胞中,GSK872浓度依赖性地阻断TNF诱导的坏死性细胞死亡。在细胞基础的实验中,与细胞外生化实验相比,IC50有100至1000倍的变化。GSK872抑制DAI或TLR3诱导的(RIP1独立的)细胞死亡。它诱导caspase激活,进而诱导凋亡细胞死亡[1]。

溶解度

Ethanol:38 mg/mL (99.09 mM);DMSO:55 mg/mL (143.42 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

参考文献

1.Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014, 56(4):481-95.
2.Kaiser WJ, et al. Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL. J Biol Chem. 2013 Oct 25;288(43):31268-79.
3.Yang XS, et al. Hypoxia-inducible factor-1 alpha is involved in RIP-induced necroptosis caused by in vitro and in vivo ischemic brain injury.Sci Rep. 2017 Jul 19;7(1):5818.

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