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GSK-872

GSK-872 (GSK2399872A) 是一种有效且特异性的 RIP3 激酶抑制剂，降低 RIPK3 介导的坏死和随后的 HMGB1 的细胞质易位和表达，可改善早期脑损伤中的脑水肿和神经功能缺损。它以高亲和力结合 RIP3 激酶结构域，IC50为1.8 nM，并抑制激酶活性，IC50为1.3 nM。

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

GSK872|GSK'872|GSK2399872A

验证数据展示

  • CAS No.: 1346546-69-7

    GSK-872
    CAS#: 1346546-69-7

产品信息

GSK-872 (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).

CAS号 1346546-69-7
分子式 C19H17N3O2S2
主要靶点 RIP kinase
主要通路 NF-κB信号通路|凋亡
分子量 383.48
纯度 99.30%， 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
别名 GSK872|GSK'872|GSK2399872A

靶点活性

RIP3K:1.8 nM

体内活性

In compared with no treatment after ischemic injury in vivo, GSK872 can significantly reduce HIF-1α expression [3].

体外活性

GSK872 (1 μM) has no inhibition for most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase. In HT-29 cells, GSK872 concentration-dependently blocks TNF-induced necroptosis. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK872 inhibits DAI- or TLR3-induced (RIP1-independent) death. It induces caspase activation and then induces apoptotic cell death[1].

溶解度

DMSO:71 mg/mL (185.1 mM),Ethanol:38 mg/mL (99.1 mM),H2O:<1 mg/mL

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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