Biochem/physiol Actions

Primary TargetCHOP

Reversible: yes

Cell permeable: yes

General description

A cell-permeable sulfonamidebenzamide derivative that acts as a potent and selective inducer of C/EBP-homologous protein (CHOP; AC₅₀ = 800 nM) without affecting XBP (AC₅₀ >80 µM). Displays a balanced profile in terms of its lipophilic profile (cLogP = 2.7), selectivity, and activation of CHO-CHOP luciferase reporter system. Exhibits high selectivity against a panel of 67 GPCR, nuclear receptors, transporters, and ion channels. Has significantly reduced activity towards dopamine receptor at high concentrations (68% at 10 µM). upregulates the expression of UPR target genes. Displays anti-proliferation properties in wild-type mouse embryonic fibroblasts (EC₅₀ = 4.8 µM), but does not affect CHOP knock out cells even at high concentrations (EC₅₀ >20 µM). Inhibits the proliferation of several cancer cell lines at low micromolar levels. Exhibits favorable pharmacokinetic profile (C_max = 140 nM; T_max = 0.17 h at 30 mg/kg, i.p. single dose).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Flaherty, D. P., et al. 2014. ACS Med Chem Lett.5, 1278.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)