General description
A highly potent and selective CAAX peptidomimetic of the carboxyl terminal of Ras proteins that inhibits farnesyl transferase (FTase) in vitro (IC50 = 500 pM). Inhibits geranylgeranyltransferase I (GGTase I) at much higher concentration (IC50 = 50 nM). Has been shown to selectively block the growth of a human lung carcinoma expressing oncogenic K-Ras in nude mice. Also inhibits oncogenic signaling and tumor growth of NIH 3T3 cells transformed with the Ras oncogene at 20 µM.
Biochem/physiol Actions
Cell permeable: no
Primary Target
FTase in vitro
Product does not compete with ATP.
Reversible: no
Target IC50: 500 pM against FTase in vitro
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Physical form
Supplied as a trifluoroacetate salt.
Reconstitution
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 1 week at -70°C.
Other Notes
Lantry, L.E., et al. 2000. Carcinogenesis21, 113.
Lerner, E.C., et al. 1995. J. Biol. Chem. 270, 26802.
Sun, J., et al. 1995. Cancer Res. 55, 4243.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 433.59. Empirical Formula: C21H27N3O3S2. Quality Level: 100. Assay: ≥. 90% (HPLC). form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, desiccated (hygroscopic). color: white. solubility: DMSO: 25 . mg/mL. shipped in: ambient. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 41115408
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 344550-250UG
