HG-9-91-01

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

HG-9-91-01 是一种有效、高选择性的盐诱导激酶 (SIK) 抑制剂，对 SIK1、SIK2 和 SIK3 的 IC50 值分别为 0.92 nM、6.6 nM 和 9.6 nM。

HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIKs) inhibitor for SIK1, SIK2 and SIK3. Inhibition of SIK kinase activity induces an anti-inflammatory phenotype in macrophages.

HG-9-91-01 inhibits a number of protein tyrosine kinases that possess a threonine residue at the gatekeeper site, such as Src family members (Src, Lck, and Yes), BTK, and the FGF and Ephrin receptors. HG-9-91-01 demonstrates a strong correlation between the potency of SIK2 inhibition and enhanced IL-10 production. In agreement with these reports, pretreating BMDCs with HG-9-91-01, a recently described inhibitor of SIK1-3, along with several other kinases, results in concentration-dependent potentiation of zymosan-induced IL-10 production with an EC50 ~200 nM and a maximum effect similar to that observed with PGE2. HG-9-91-01 has more than a 100-fold greater potency against SIKs than AMPK (IC50=4.5 μM) in a cell-free assay. HG-9-91-01 treatment dose dependently increased mRNA expression of Pck1 and G6pc and that effect is similar in cells treated with 4 μM HG-9-91-01. Consistent with this observation, there is also a dose-dependent increase in glucose production following HG-9-91-01 treatment.

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HG-9-91-01 | HG-9-91-01 | HG 9-91-01

Angiogenesis

PKC

SIK1|SIK2|SIK3

Inflammation/Immunology

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1456858-58-4

567.68

C32H37N7O3

>98% (HPLC)

DMSO : ≥ 150 mg/mL; 264.23 mM

CC1=C(C(=CC=C1)C)NC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC=NC(=C3)NC4=CC=C(C=C4)N5CCN(CC5)C

1-(2,4-Dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)urea

(-20℃)

With Ice Pack

≥ 2 years