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
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
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.
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.
1.Clark K, MacKenzie KF, Petkevicius K, Kristariyanto Y, Zhang J, Choi HG, Peggie M, Plater L, Pedrioli PG, McIver E et al.. (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages.. Proc Natl Acad Sci USA, 109 (42):(16986-91). [PMID:23033494]
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G2221203