[CAS NO. 1456858-58-4]  HG-9-91-01

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PRODUCTS SPECIFICATIONS [1456858-58-4]

Catalog
SLK-S8393
Brand
Selleck
CAS
1456858-58-4

DESCRIPTION [1456858-58-4]

Overview

MDL-
Molecular Weight567.68
Molecular FormulaC32H37N7O3
SMILES-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.7616 mL8.8078 mL17.6156 mL
5 mM0.3523 mL1.7616 mL3.5231 mL
10 mM0.1762 mL0.8808 mL1.7616 mL
50 mM0.0352 mL0.1762 mL0.3523 mL

Description

HG-9-91-01 (SIK inhibitor 1) is a potent and highly selective inhibitor of 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 nM6.6 nM9.6 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.