HG-9-91-01

InvivoChem Cat #:V3380CAS #:1456858-58-4Purity >=98%

Description: HG-9-91-01 is a novel, potent and highly selective inhibitor of salt-inducible kinase (SIKs) with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively. The selective SIK inhibitor HG-9-91-01 promotes dephosphorylation of transcriptional co-activators CRTC2/3 resulting in enhanced gluconeogenic gene expression and glucose production in hepatocytes, an effect that is abolished when an HG-9-91-01-insensitive mutant SIK is introduced or LKB1 is ablated. Although SIK2 was proposed as a key regulator of insulin-mediated suppression of gluconeogenesis, we provide genetic evidence that liver-specific ablation of SIK2 alone has no effect on gluconeogenesis and insulin does not modulate SIK2 phosphorylation or activity. Collectively, we demonstrate that the LKB1-SIK pathway functions as a key gluconeogenic gatekeeper in the liver.

Description:

References: Nat Commun. 2014 Aug 4; 5:4535; Proc Natl Acad Sci U S A. 2012 Oct 16; 109(42):16986-91.

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-20C for 3 years in powder form

Synonym: HG-9-91-01; HG-9-91-01; HG 9-91-01; HG9-91-01; HG99101; HG-99101; HG 99101
Chemical Name: 1-(2, 4-Dimethoxyphenyl)-3-(2, 6-dimethylphenyl)-1-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)urea
InChi Key: UYUHRKLITDJEHB-UHFFFAOYSA-N
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)
SMILES Code: O=C(NC1=C(C)C=CC=C1C)N(C2=CC=C(OC)C=C2OC)C3=NC=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=C3