496265

Oncrasin-1

A cell-permeable indolecarboxaldehyde compound that selectively induces apoptosis in cells harboring mutant K-Ras both in vitro and in vivo.

• Synonym(s): Oncrasin-1, 1-((4-Chlorobenzyl)-1H-indole-3-carboxaldehyde, Oncogenic Ras Tumor- Inhibiting compound 1, 1-((4-Chlorobenzyl)-1H-indole-3-carboxaldehyde, Oncogenic Ras Tumor-Inhibiting compound 1
• Empirical Formula (Hill Notation): C₁₆H₁₂ClNO
• CAS Number: 75629-57-1
• Molecular Weight: 269.73
• MDL number: MFCD01051808
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white to light pink
• solubility: DMSO: soluble; ethanol: soluble
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C16H12ClNO/c17-14-7-5-12(6-8-14)9-18-10-13(11-19)15-3-1-2-4-16(15)18/h1-8,10-11H,9H2
• InChI key: ZDRQMXCSSAPUMM-UHFFFAOYSA-N

Description

General description

A cell-permeable indolecarboxaldehyde compound that selectively induces apoptosis in cells harboring mutant K-Ras both in vitro (IC₅₀ = 0.11, 0.25, 1.0, 1.58, and 4.81 µM in H2887, H460, H2122, A549, and T29Kt1 cultures, respectively) and in vivo (75% suppression of H460-derived tumor growth in mice; 100 mg/kg via daily i.p.), while exhibiting little or much reduced potency toward cells with wild-type Ras or mutant N-Ras (IC₅₀ ≥31 µM). Oncrasin-1 treatment is shown to induce PKCι aggregation with splicing factors in the nucleus and dissociation between PKCι and CDK9/Cyclin T1 in K-Ras mutant cultures, resulting in decreased RNA polymerase II phosphorylation and a suppression of RNA processing in general. Oncrasin-1-induced cell death requires the presence of both mutant K-Ras and PKCι, siRNA-mediated knockdown of either enzyme is demonstrated to abolish its cytotoxicity in H460 and T29Kt1 cultures.

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Reconstitution

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

Other Notes

Guo, W., et al. 2009. Mol. Cancer Ther.8, 441.
Guo, W., et al. 2008. Cancer Res.68, 7403.

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