[CAS NO. 848249-10-5] HS-243

Name: HS-243
Brand: Arctom Scientific
SKU: SLK-S9701

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PRODUCTS SPECIFICATIONS [848249-10-5]

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Catalog

SLK-S9701

Brand

Selleck

CAS

848249-10-5

DESCRIPTION [848249-10-5]

Overview

MDL	-
Molecular Weight	324.33
Molecular Formula	C17H16N4O3
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

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	3.0833 mL	15.4164 mL	30.8328 mL
5 mM	0.6167 mL	3.0833 mL	6.1666 mL
10 mM	0.3083 mL	1.5416 mL	3.0833 mL
50 mM	-	-	-

Description

HS-243 is a highly potent inhibitor with IC50 of 24 nM, 20 nM and 0.5 μM for IRAK-1, IRAK-4 and TAK1, respectively.

Targets

IRAK-4 ^[1] (Cell-free assay)	IRAK-1 ^[1] (Cell-free assay)	TAK1 ^[1] (Cell-free assay)
20 nM	24 nM	0.5 μM

In vitro

HS-243 has exquisite selectivity toward both IRAK-1 (IC50 = 24 nM) and IRAK-4 (IC50 = 20 nM), with only minimal TAK1-inhibiting activity (IC50 = 0.5 μM). Using HS-243 and takinib, we evaluates the consequences of cytokine/chemokine responses after selective inhibition of IRAK-1/4 or TAK1 in response to lipopolysaccharide challenge in human rheumatoid arthritis fibroblast-like synoviocytes. HS-243 specifically inhibits intracellular IRAKs without TAK1 inhibition and these kinases have distinct, nonredundant signaling roles.

References

[1] Scott A Scarneo, et al. J Biol Chem. 2020 Feb 7;295(6):1565-1574.