GSK-872|1346546-69-7|-陌孚医药/Medlife

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GSK-872

目录号: PL11038 纯度: ≥99%

CAS No. :1346546-69-7

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中文名称	GSK-872
中文别名	N-5-苯并噻唑基-6-[(1-甲基乙基)磺酰基]-4-喹啉胺
英文名称	GSK-872
英文别名	GSK'872;GSK872;N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine;N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-Quinolinamine;N-(6-(isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine;GSK2399872A;GSK'872 (GSK2399872A);AOB4887;GSK 872;BCP28887;s8465;AK00779012;GSK-872
Cas No.	1346546-69-7
分子式	C₁₉H₁₇N₃O₂S₂
分子量	383.49
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	GSK-872 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 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 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 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 (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 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	Powder -20°C 3 years；4°C 2 years
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. [3]. C

溶解度数据	In Vitro: DMSO : 100 mg/mL (260.76 mM; Need ultrasonic)配制储备液

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