A RIPK2 inhibitor
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GSK2983559

Item No. 31458

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[4-(5-benzothiazolylamino)-6-[(1,1-dimethylethyl)sulfonyl]-7-quinazolinyl]oxy]-ethanol, 1-(dihydrogen phosphate)
CAS Number
1579965-12-0
Molecular Formula
C21H23N4O7PS2
Formula Weight
538.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: slightly solubleDMSO: 1 mg/mlPBS (pH 7.2): 1 mg/ml
λmax
218, 245, 344 nm
SMILES
O=P(O)(OCCOC1=CC2=NC=NC(NC3=CC4=C(SC=N4)C=C3)=C2C=C1S(=O)(C(C)(C)C)=O)O
InChi Code
InChI=1S/C21H23N4O7PS2/c1-21(2,3)35(29,30)19-9-14-15(10-17(19)31-6-7-32-33(26,27)28)22-11-23-20(14)25-13-4-5-18-16(8-13)24-12-34-18/h4-5,8-12H,6-7H2,1-3H3,(H,22,23,25)(H2,26,27,28)
InChi Key
MJLYDVMFNHZMLV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    GSK2983559 is a receptor-interacting protein kinase 2 (RIPK2) inhibitor.1 It inhibits RIPK2 by 65% in a kinase assay when used at a concentration of 10 µM. GSK2983559 (10 µM) also inhibits VEGFR3 by greater than 90%, as well as 14 additional kinases by 60 to 89% in a panel of 344 kinases. In vivo, GSK2983559 (7.5 and 145 mg/kg twice per day) reduces colonic damage in a mouse model of TNBS-induced colitis. GSK2983559 is also a prodrug that is cleaved to an active metabolite in the gastrointestinal tract that inhibits RIPK2 more potently than GSK2983559.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Haile, P.A., Casillas, L.N., Votta, B.J., et al. Discovery of a first-in-class receptor interacting protein 2 (RIP2) kinase specific clinical candidate, 2-((4-(benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl dihydrogen phosphate, for the treatment of inflammatory diseases. J. Med. Chem. 62(14), 6482-6494 (2019).