Cadein1

General description

A cell-permeable isoquinolinium compound that preferentially induces apoptotic cell death in p53-deficient cancer cells with functional MMR (DNA mismatch repair) system.

A cell-permeable isoquinolinium compound that preferentially induces apoptotic cell death in p53-deficient cancer cells with functional MMR (DNA mismatch repair) system, including HCT116-Ch3/E6, HeLa, HT29, and SW620 (viability <19 %; 4-6 µM Cadein1 for 24 h), while exhibiting much reduced potency in MMR^-/p53⁺ (RKO and HCT116), MMR^-/p53^- (DLD-1 and HCT116-E6), and MMR⁺/p53⁺ (HCT116-Ch3 and HEK293) cancer cultures (viability = 40 to 92%; 4 µM Cadein1 for 24 h).

A cell-permeable isoquinolinium compound that preferentially induces p38 phosphorylation, caspase-3 activation, PARP cleavage, and apoptotic cell death in p53-deficient cancer cells with functional MMR (DNA mismatch repair) system, including HCT116-Ch3/E6, HT29, SW620 (viability = 10.6, 32, and 18.6%, respectively; 4 µM Cadein1 for 24 h), and HeLa (17.7% viability; 6 µM Cadein1 for 24 h), while exhibiting much reduced potency toward MMR^-/p53⁺ (80% and 68.6% viability of RKO and HCT116, respectively; 4 µM Cadein1 for 24 h), MMR^-/p53^- (51% and 49% viability of DLD-1 and HCT116-E6, respectively; 4 µM Cadein1 for 24 h), or MMR⁺/p53⁺ (55.4% and 92% viability of HCT116-Ch3 and HEK293, respectively; 4 µM Cadein1 for 24 h) cancer cells. MMR function knockdown in MMR⁺/p53^- SW620 cells confers Cadein1 resistance (70% viability; 4 µM Cadein1 for 24 h), likewise p53 downregulation in MMR⁺/p53⁺ HEK293 cells restores sensitivity to Cadein1 (45% viability; 4 µM Cadein1 for 24 h).

Legal Information

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

Other Notes

Jang, E.R., et al. 2010. J. Biol. Chem.285, 2986.

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 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)