GSK840

GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.

Product information

CAS Number: 2361146-30-5

Molecular Weight: 365.43

Formula: C21H23N3O3

Chemical Name: tert-butyl 2-{4-[5-(methylcarbamoyl)-1H-1, 3-benzodiazol-1-yl]phenyl}acetate

Smiles: CNC(=O)C1C=C2N=CN(C2=CC=1)C1C=CC(CC(=O)OC(C)(C)C)=CC=1

InChiKey: UGTLDBJIOSYXRR-UHFFFAOYSA-N

InChi: InChI=1S/C21H23N3O3/c1-21(2,3)27-19(25)11-14-5-8-16(9-6-14)24-13-23-17-12-15(20(26)22-4)7-10-18(17)24/h5-10,12-13H,11H2,1-4H3,(H,22,26)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 110 mg/mL (301.02 mM; Need ultrasonic)

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: ≥360 days 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:

GSK840 (GSK'840) (0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in a concentration-dependent manner. GSK840 binds the kinase domain and inhibits kinase activity with high specificity, targeting a broader range of pro-necrotic stimuli than can be achieved with RIP1 kinase inhibitors.

References:

1. Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014 Nov 20;56(4):481-95.

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