205536

Cadein1

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

• Synonym(s): Cadein1
• Empirical Formula (Hill Notation): C₃₃H₄₈F₂INO₂
• Molecular Weight: 655.64
• MDL number: MFCD32671841
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: yellow
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: FC1=CC=CC(F)=C1C[N+](CC2)=C(C3=C2C=C(C(OC)=C3)OC)CCCCCCCCCCCCCCC.[I-]

Description

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, including HCT116-Ch3/E6, HeLa, HT29, and SW620 (viability &lt19 %; 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 apoptotic cell death in p53-deficient cancer cells with functional MMR (DNA mismatch repair) system.

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).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable