A RIPK1 inhibitor
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GSK2982772

Item No. 29230

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-5-carboxamide
CAS Number
1622848-92-3
Molecular Formula
C20H19N5O3
Formula Weight
377.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMSO: 15mg/mLDMSO:PBS (pH 7.2) (1:5): 0.16mg/mLEthanol: 5mg/mL
SMILES
CN1C2=CC=CC=C2OC[C@H](NC(C3=NN=C(CC4=CC=CC=C4)N3)=O)C1=O
InChi Code
InChI=1S/C20H19N5O3/c1-25-15-9-5-6-10-16(15)28-12-14(20(25)27)21-19(26)18-22-17(23-24-18)11-13-7-3-2-4-8-13/h2-10,14H,11-12H2,1H3,(H,21,26)(H,22,23,24)/t14-/m0/s1
InChi Key
LYPAFUINURXJSG-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $263

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    10 mg

    $393

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    Product Description

    GSK2982772 is an inhibitor of receptor interacting serine/threonine kinase 1 (RIPK1; IC50s = 16 and 2,500 nM for the human and mouse enzymes, respectively).1 It is greater than 10,000-fold selective for RIPK1 over a panel of 339 kinases at 10 µM. GSK2982772 inhibits necrotic cell death induced by a combination of TNF-α and the caspase inhibitor QVD-OPh in U937 human monocytic and L929 murine fibrosarcoma cells (IC50s = 6.3 and 1,300 nM, respectively). GSK2982772 (3-300 nM) decreases IL-1β and IL-6 levels in intestinal mucosa tissue isolated from patients with ulcerative colitis. It increases survival in a mouse model of TNF-α-induced lethal shock when administered at doses of 3, 10, and 50 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. P.A., H., Berger, S.B., Jeong, J.U., 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. 60(4), 1247-1261 (2017).