Home Immunology & Inflammation SIK inhibitor HG-9-91-01 For research use only.

HG-9-91-01

Synonyms: SIK inhibitor 1

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 Chemical Structure

HG-9-91-01 Chemical Structure

CAS: 1456858-58-4

Selleck's HG-9-91-01 has been cited by 2 publications

Purity & Quality Control

Batch: S839301 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.81%
99.81

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models male 8-10 week-old C57BL/6 mice
Dosages --
Administration IP

Chemical Information & Solubility

Molecular Weight 567.68 Formula

C32H37N7O3
CAS No. 1456858-58-4 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (176.15 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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