GSK-872 hydrochloride|2703752-81-0|-陌孚医药/Medlife

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GSK-872 hydrochloride

目录号: PL11016 纯度: ≥99%

CAS No. :2703752-81-0

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中文名称	GSK-872 hydrochloride
英文名称	GSK-872 hydrochloride
英文别名	GSK-872 hydrochloride
Cas No.	2703752-81-0
分子式	C₁₉H₁₈ClN₃O₂S₂
分子量	419.95
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	GSK-872 hydrochloride 是 RIPK3 抑制剂，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。GSK-872 hydrochloride 降低 RIPK3 介导的坏死 (necroptosis) 和随后的 HMGB1 的细胞质易位和表达，并改善早期脑损伤中的脑水肿和神经功能缺损。
生物活性	GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC 50 of 1.8 nM, and inhibits kinase activity with an IC 50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
性状	Solid
IC50 & Target[1][2]	IC50: 1.3 nM (RIPK3)
体外研究(In Vitro)	GSK-872 (GSK872; 0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)	GSK-872 hydrochloride (25 mM; intracerebroventricular injection) can attenuate brain edema and improve neurological function following subarachnoid hemorrhage (SAH) and reduce the number of necrotic cells. GSK-872 hydrochloride can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein. 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	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014 Nov 20;56(4):481-95. [2]. Arora D, et al. Deltamethrin induced RIPK3-mediated caspase-independent non-apoptotic cell death in rat primary hepatocytes. Biochem Biophys Res Commun. 2016 Oct 14;479(2):217-223.

溶解度数据	In Vitro: DMSO : 10 mg/mL (23.81 mM; ultrasonic and warming and heat to 60°C)H₂O : 2.5 mg/mL (5.95 mM; ultrasonic and warming and heat to 60°C)

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