GSK-872

GSK-872 is a receptor-interacting protein kinase-3 (RIP3) inhibitor. GSK-872 inhibits TNF- and virus-induced necrosis in 3T3-SA fibroblasts. It also inhibits necrosis induced by toll-like receptor 3 (TLR3).

Product information

CAS Number: 1346546-69-7

Molecular Weight: 383.49

Formula: C19H17N3O2S2

Synonym:

GSK872

GSK-872

GSK 872

Chemical Name: N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-quinolinamine

Smiles: CC(C)S(=O)(=O)C1=CC2C(C=C1)=NC=CC=2NC1C=C2N=CSC2=CC=1

InChiKey: ZCDBTQNFAPKACC-UHFFFAOYSA-N

InChi: InChI=1S/C19H17N3O2S2/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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GSK-872 (GSK'872; 0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner.

References:

1. Liao L, Shang L, Li N, Wang S, Wang M, Huang Y, Chen D, Huang J, Xiong K. Mixed lineage kinase domain-like protein induces RGC-5 necroptosis following elevated hydrostatic pressure. Acta Biochim Biophys Sin (Shanghai). 2017 Oct 1;49(10):879-889. doi: 10.1093/abbs/gmx088. PubMed PMID: 28981598.
2. Cekay MJ, Roesler S, Frank T, Knuth AK, Eckhardt I, Fulda S. Smac mimetics and type II interferon synergistically induce necroptosis in various cancer cell lines. Cancer Lett. 2017 Sep 18. pii: S0304-3835(17)30549-9. doi: 10.1016/j.canlet.2017.09.002. [Epub ahead of print] PubMed PMID: 28923396.
3. Lu B, Gong X, Wang ZQ, Ding Y, Wang C, Luo TF, Piao MH, Meng FK, Chi GF, Luo YN, Ge PF. Shikonin induces glioma cell necroptosis in vitro by ROS overproduction and promoting RIP1/RIP3 necrosome formation. Acta Pharmacol Sin. 2017 Aug 17. doi: 10.1038/aps.2017.112. [Epub ahead of print] PubMed PMID: 28816233.
4. Yang XS, Yi TL, Zhang S, Xu ZW, Yu ZQ, Sun HT, Yang C, Tu Y, Cheng SX. 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. doi: 10.1038/s41598-017-06088-0. PubMed PMID: 28724891; PubMed Central PMCID: PMC5517428.
5. Bhatti IA, Abhari BA, Fulda S. Identification of a synergistic combination of Smac mimetic and Bortezomib to trigger cell death in B-cell non-Hodgkin lymphoma cells. Cancer Lett. 2017 Oct 1;405:63-72. doi: 10.1016/j.canlet.2017.07.008. Epub 2017 Jul 14. PubMed PMID: 28716527.

Products are for research use only. Not for human use.