An inhibitor of salt-inducible kinases
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HG-9-91-01

Item No. 19179

Technical Information
Formal Name
N-(2,4-dimethoxyphenyl)-N'-(2,6-dimethylphenyl)-N-[6-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]-urea
CAS Number
1456858-58-4
Molecular Formula
C32H37N7O3
Formula Weight
Purity
≥95%
A crystalline solid
DMF: 5 mg/mlDMSO: 3 mg/mlEthanol: 5 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg
λmax
303 nm
SMILES
CC1=C(NC(N(C2=C(OC)C=C(OC)C=C2)C3=NC=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=C3)=O)C(C)=CC=C1
InChi Code
InChI=1S/C32H37N7O3/c1-22-7-6-8-23(2)31(22)36-32(40)39(27-14-13-26(41-4)19-28(27)42-5)30-20-29(33-21-34-30)35-24-9-11-25(12-10-24)38-17-15-37(3)16-18-38/h6-14,19-21H,15-18H2,1-5H3,(H,36,40)(H,33,34,35)
InChi Key
UYUHRKLITDJEHB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    HG-9-91-01 is an inhibitor of salt-inducible kinases (SIKs; IC50s = 0.92, 6.6, and 9.6 nM for SIK1, SIK2, and SIK3, respectively).1 It also inhibits Src, Lck, Yes, and BTK, as well as FGF and Ephrin receptors.1 HG-9-91-01 increases LPS-stimulated IL-10 production and suppresses pro-inflammatory cytokine secretion in bone marrow-derived macrophages.1 SIK inhibitors, including HG-9-91-01, enhance CREB-dependent gene transcription and IL-10 production in bone marrow-derived dendritic cells, THP-1 cells, and human primary macrophages.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Clark, K., MacKenzie, K.F., Petkevicius, K., et alPhosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc. Natl. Acad. Sci. USA 109(42), 16986-16991 (2012).