A selective inhibitor of RIP1
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GSK481

Item No. 20308

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-3-isoxazolecarboxamide
CAS Number
1622849-58-4
Molecular Formula
C21H19N3O4
Formula Weight
377.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mLDMSO: 30 mg/mLEthanol: 30 mg/mLEthanol:PBS (pH 7.2) (1:10): 0.09 mg/mL
λmax
238 nm
SMILES
O=C(C1=NOC(CC2=CC=CC=C2)=C1)N[C@@H](COC(C=CC=C3)=C3N4C)C4=OO=C(C1=NOC(CC2=CC=CC=C2)=C1)N[C@@H](COC(C=CC=C3)=C3N4C)C4=O
InChi Code
InChI=1S/C21H19N3O4/c1-24-18-9-5-6-10-19(18)27-13-17(21(24)26)22-20(25)16-12-15(28-23-16)11-14-7-3-2-4-8-14/h2-10,12,17H,11,13H2,1H3,(H,22,25)/t17-/m0/s1
InChi Key
KNOUWGGQMADIBV-KRWDZBQOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    25 mg

    $587

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    Product Description

    GSK481 is an inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1 or RIPK1) that blocks autophosphorylation of Ser166 on wild-type human RIP1 with an IC50 value of 2.8 nM.1 It is selective for RIP1 over a panel of over 450 other kinases, including RIP3.2,1 GSK481 inhibits RIP1 from human and cynomolgus monkey but is at least 100-fold less potent against non-primate RIP1.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Harris, P.A., King, B.W., Bandyopadhyay, D., et al. DNA-encoded library screening identifies benzo[b][1,4]oxazepin-4-ones as highly potent and monoselective receptor interacting protein 1 kinase inhibitors. J. Med. Chem. 59(5), 2163-2178 (2016).

    2. Geserick, P., Wang, J., Schilling, R., et al. Absence of RIPK3 predicts necroptosis resistance in malignant melanoma. Cell Death Dis. 6, e1884 (2015).