For research use only. Not for therapeutic Use.
GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 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[1][2][3].
GSK-872 hydrochloride (0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner[1].
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[3].
| Catalog Number | I045691 |
| CAS Number | 2703752-81-0 |
| Synonyms | N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine;hydrochloride |
| Molecular Formula | C19H18ClN3O2S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H17N3O2S2.ClH/c1-12(2)26(23,24)14-4-5-16-15(10-14)17(7-8-20-16)22-13-3-6-19-18(9-13)21-11-25-19;/h3-12H,1-2H3,(H,20,22);1H |
| InChIKey | VKCVPZFWFZKUJY-UHFFFAOYSA-N |
| SMILES | CC(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=CC4=C(C=C3)SC=N4.Cl |
| Reference | [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]. Chen T, et al. Inhibiting of RIPK3 attenuates early brain injury following subarachnoid hemorrhage: Possibly through alleviating necroptosis. Biomed Pharmacother. 2018;107:563-570. |
