CHOP Activator, Cpd12

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).

Cell permeable: yes

Primary Target
CHOP

Reversible: yes

Packaged under inert gas

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

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

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

Toxicity: Standard Handling (A)