BiochemProbe — Life Science Research Reagents

GSK2982772 free base · Synonyms: GSK-2982772 · GSK 2982772

GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor.

For research use only. Not for human or veterinary use.

Purity >98% Stock Inquire

GSK2982772 structure

CAS No.: 1622848-92-3

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
500 mg USD 850.00 BP-02513-500mg In stock Get quote
1 g USD 1,350.00 BP-02513-1g In stock Get quote
2 g USD 2,298.00 BP-02513-2g In stock Get quote
5 g Inquire BP-02513-5g In stock Inquire

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Description

GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively .

Biological activity

GSK2982772 is a potent inhibitor of selective receptor interaction protein kinase 1 (RIPK1), with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively. GSK2982772 binds effectively to RIP1, has sensitive kinase specificity, and has excellent activity in blocking many TNF-dependent cellular responses. RIP1 is an important upstream kinase that has been shown to regulate inflammation through specific functions of scaffold and kinase. In vivo, GSK2982772 showed good free fractions in the blood of rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%).

Identifiers

SMILES
CN1C2=CC=CC=C2OC[C@H](NC(=O)C2=NC(CC3=CC=CC=C3)=NN2)C1=O
InChIKey
LYPAFUINURXJSG-AWEZNQCLSA-N

Specifications

MW (average)
377.3966
Formula
C20H19N5O3
CAS No.
1622848-92-3
Physical state
Solid
Color
White to yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -20°C, 1 year

Solubility

Soluble in DMSO; H2O

References

[1].Harris PA, et al. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 23;60(4):1247-1261.

Same target

Search RIP kinase

Same research area

Search Infection

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