General description
A cell-permeable pentanylbenzamide compound that acts as an allosteric, reversible, and selective inhibitor of the collgenolytic activity of MT1-MMP. Does not affect the catalytic activity of cellular MT-1-MMP thus allows it to retain its ability to activate MMP-2. Selectively targets the hemopexin (PEX) domain of MT1-MMP, thereby repressing its pro-tumorigenic activity. Its binding to the PEX domain is dependent on Met-328, Arg-330, Asp-376, Met-422, and Ser-470 in the druggable pocket of the enzyme. Shown to block 184B5-MT cell migration on collagen-1 and repress MCF7-β3/MT tumor growth in xenografted mice (0.5 mg/kg, intratumoral).
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 1 year at -20°C.
Other Notes
Remacle, A.G., et al. 2012. Cancer Res.72, 2339.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 260.16. Empirical Formula: C12H15Cl2NO. Quality Level: 100. Assay: ≥. 98% (HPLC). form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 100 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. SMILES string: ClC1: C(Cl)C: C(C(NC(C)CCC): O)C: C1. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51434810
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 444295-25MG
