Description
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:
- 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.
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