2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride

Description

SC144 is an orally bioavailable gp130 inhibitor. It inhibits phosphorylation of STAT1, STAT3, and Akt induced by leukemia inhibitory factor (LIF) and IL-6, but not IFN-γ, in OVCAR-8 ovarian cancer cells when used at a concentration of 20 μM. SC144 induces cell cycle arrest at the G₀/G₁ phase in MDA-MB-435 breast and HT-29 colorectal cancer cells and inhibits proliferation of 14 cancer cell lines, including prostate, ovarian, lung, breast, and colorectal cancer cells, with IC₅₀ values ranging from 0.4 to 4 μM. It reduces tumor growth in OVCAR-8 and MDA-MB-435 mouse xenograft models.

Uses

SC 144 Hydrochloride has been shown to have antitumor properties.

Uses

SC144 hydrochloride has been used:

• as a glycoprotein 130 (gp130) inhibitor to evaluate the effect of bazedoxifene on interleukin (IL-6) mediated cell viability in pancreatic cancer cells
• as a gp130 inhibitor to study its effects on signal transducer and activator of transcription 3 (STAT3) activation in mesenchymal precursor?cells?(KMM)?cells
• as an interleukin 6 signal transducer (IL-6ST) inhibitor in media to test its ability to block serum-induced migration/invasion

Biochem/physiol Actions

SC144 is a potent inhibitor of glycoprotein 130 (gp130). SC144 binds to gp130 and blocks STAT3 phosphorylation, nuclear translocation and expression of STAT3 responsive genes. SC144 inhibits the growth of several tumor cell lines, independent of p53 or hormone receptor levels, and inhibits growth of ovarain tumor xenografts in mice.

storage

Store at -20°C