HG-9-91-01 - 99%, high purity , CAS No.1456858-58-4, Inhibitor of salt inducible kinase 1;Inhibitor of salt inducible kinase 2;Inhibitor of SIK family kinase 3

Item Number

H413999

• Synonyms: HG-9-91-01|1456858-58-4|SIK inhibitor 1|1-(2,4-dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-[6-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]urea|1-(2,4-dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)
• Specifications & Purity: Moligand™, ≥99%
• Biochemical and Physiological Mechanisms: 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.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of salt inducible kinase 1;Inhibitor of salt inducible kinase 2;Inhibitor of SIK family kinase 3

Product Description

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