HG-9-91-01

For research use only.

Catalog No.S8393 Synonyms: SIK inhibitor 1

1 publication

HG-9-91-01 Chemical Structure

CAS No. 1456858-58-4

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.

Selleck's HG-9-91-01 has been cited by 1 publication

Purity & Quality Control

Choose Selective SIK Inhibitors

Biological Activity

Description 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 [1]
(Cell-free assay)
SIK2 [1]
(Cell-free assay)
SIK3 [1]
(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.[1]

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.[2]

Protocol

Cell Research:

[1]

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  • Cell lines: Macrophages
  • Concentrations: 500 nM
  • Incubation Time: 1 h
  • Method:

    Macrophages are treated for 1 h with 500 nM HG-9-91-01 or an equivalent volume of DMSO for control incubations then stimulated for up to 24 h with 1 μg/mL Pam3CSK4, 2 μg/mL lipoteichoic acid (LTA), 100 ng/mL LPS, 1 μg/mL R837, or 2 μM CpG. Proteins are extracted and immunoblotted by using the indicated antibodies. RNA is extracted by using the RNeasy Micro Kit. cDNA is generated by using the iScript cDNA synthesis kit and quantified by qPCR using the SsoFast EvaGreen Supermix. The relative expression of each gene is calculated from Ct values by using the Pfaffl method and is normalized against the mRNA levels of 18S or GAPDH RNA. Fold induction for each gene is reported relative to untreated control cells, which is set to 1. The concentrations of TNFα, IL-6, IL-10, IL-12p40, and RANTES in culture supernatants were measured by using the Bio-Plex Pro Assay system from Bio-Rad.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: male 8-10 week-old C57BL/6 mice
  • Dosages: --
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (176.15 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 567.68
Formula

C32H37N7O3

CAS No. 1456858-58-4
Storage powder
in solvent
Synonyms SIK inhibitor 1
Smiles 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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID