General description
A cell-permeable biphenylsulfonylvaline compound that acts as a potent inhibitor against MMP-2, -3, and -13 (IC50 = 47, 12, and 8 nM, respectively) and a weaker inhibitor against AMP deaminase (20% inhibition at 0.1 µM), MMP-1, -7, -9, and -14 (IC50 = 6.1, 7.2, 7.9, and 0.24 µM, respectively). Shown to offer therapeutic benefits in vivo in various animal models of heart failure and diabetes.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MMP-2, -3, and -13
Product does not compete with ATP.
Reversible: no
Target IC50: 47, 12, and 8 nM, against MMP-2, -3, and -13, respectively
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Paolocci, N., et al. 2006. J. Pharm. Exp. Ther.317, 506.
Zhou, Y.P., et al. 2005. Diabetes54, 2612.
Peterson, J.T., et al. 2001. Circulation103, 2303.
Spinale, F.G., et al. 1999. Circ. Res.85, 364.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
| Quality Segment | 100 |
| assay | ≥98% (TLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | off-white |
| solubility | DMSO: 40 mg/mL,ethanol: 40 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | [S](=O)(=O)(N[C@@H](C(C)C)C(=O)O)c1ccc(cc1)c2ccc(cc2)Br |
| InChI | 1S/C17H18BrNO4S/c1-11(2)16(17(20)21)19-24(22,23)15-9-5-13(6-10-15)12-3-7-14(18)8-4-12/h3-11,16,19H,1-2H3,(H,20,21)/t16-/m0/s1 |
| InChI key | GJOCABIDMCKCEG-INIZCTEOSA-N |
