HG-9-91-01 (C005B-309683)

Biochem/physiol Actions

HG-9-91-01 is an ATP site-targeting WH-4-023 (KIN112) structural analog that inhibits salt-inducible kinases (SIKs) with improved potency (IC50 = 0.6/6.6/9.6 nM against SIK1/2/3) and selectivity, exhibiting significant inhibitory activity only against 4 kinases among a panel of 108 (% inhibition at 100 nM ∼85/EPHA2, 88/EPHA4, 91/Src, 88/YES1) and much reduced or little potency toward the others (by <67% inhibition at 100 nM), including AMPK-related kinases BTK, MARK and NUAK. HG-9-91-01 (500 nM) enhances LPS-induced IL-10 production, while suppresses proinflammatory cytokine secretion from murine marrow-derived macrophages & dendritic cells (BMDMs & BMDCs) as well as primary human macrophages in a CRTC3-dependent manner. A useful tool for studying SIKs-mediated cellular signaling events.

UPC:

51111746

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

5

Unit of Measurement:

MG

MPN:

SML3029-5MG

CAS:

1456858-58-4