中文名：HG-9-91-01
英文名：HG-9-91-01
纯度：Moligand™，≥99%
货号：H413999
Cas号：1456858-58-4
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
HG-9-91-01 HG-9-91-01 (SIK inhibitor 1) is a potent and highly selective inhibitor of salt-inducible kinase (SIK) with IC50 of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3, respectively.
Targets
SIK1 (Cell-free assay); SIK2 (Cell-free assay); SIK3 (Cell-free assay) 0.92 nM; 6.6 nM; 9.6 nM
In vitro
HG-9-91-01 is a potent and selective inhibitor of SIK. HG-9-91-01 not only targets the ATP-binding site, but also a small hydrophobic pocket adjacent to this site that is created by the presence of a small amino acid residue at this gatekeeper site. 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 potently inhibits the SIKs and, crucially, does not inhibit any other member of the AMPK-related kinase subfamily, which all possess a large hydrophobic residue (Met or Leu) at the gatekeeper site. HG-9-91-01 increases LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion, even when cells are costimulated with IFNγ to generate fully polarized classically activated (M1) macrophages.
In vivo
HG-9-91-01 is > 99% serum bound and rapidly degraded by mouse liver microsomes (t1/2 = 11 min) making this compound unsuitable for direct injection into animals.
Cell Research(from reference)
Cell lines：Macrophages
Concentrations：500 nM
Incubation Time：1 h
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关键字： BCP25041 ; DTXSID401025699 ; SCHEMBL15271960 ; SIK inhibitor 1
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