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BG166667

GSK 2982772 - Bio-X

An ultraselective, first-in-class inhibitor of the Receptor Interacting Protein 1 (RIP1) kinase with nanomolar potency. The compound occupies allosteric pockets characteristic of type II and type III classes of kinase inhibitors. It blocks the TNF-induced necrotic cell death and reduces the production of cytokines IL-1β and IL-6 from ulcerative colitis explant tissue. Potential candidate for treatment of inflammatory diseases such as psoriasis, ulcerative colitis and rheumatoid arthritis.

Technical Data

CAS No: 1622848-92-3
Product Code: BG166667
MDL No: MFCD30489467
Chemical Formula: C20H19N5O3
Molecular Weight: 377.40

Literature


  • Harris PA et al. (2017). 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 60(4):1247-1261.
  • Finger JN et al. (2017). Identification of an antibody-based immunoassay for measuring direct target binding of RIPK1 inhibitors in cells and tissues. Pharmacol Res Perspect 5(6)

Solubility

Stability

Further Information


Datasheets


GSK 2982772 - Bio-X

CAS No:
1622848-92-3
MDL No:
MFCD30489467
Chemical Formula:
Molecular Weight:
377.40
Product Structure
References:
1. Harris PA et al. (2017). 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 60(4):1247-1261.
2. Finger JN et al. (2017). Identification of an antibody-based immunoassay for measuring direct target binding of RIPK1 inhibitors in cells and tissues. Pharmacol Res Perspect 5(6)

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