Inhibitor SourceBook™ Second Edition

Matrix Metalloproteinase Inhibitors, continued
Calbiochem • Inhibitor SourceBook
Proteases
Product Cat. No. Comments Size Price
MMP-2/MMP-3 Inhibitor I 444239 {N-[[(4,5-Dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]carbonyl]-Lphenylalanine
Methyl Ester}
A potent inhibitor of MMP-2 (K i = 7 mM) and MMP-3 (K i = 290 nM).
MMP-2/MMP-3 Inhibitor II 444240 {a-[[[4,5-Dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]carbonyl]amino]-
((2-pyridyl)piperazinyl)-(S)-benzenepropanamide}
A potent inhibitor of MMP-2 (K i = 4.5 mM) and MMP-3 (K i = 520 nM).
MMP-2/MMP-9 Inhibitor I 444241 {(2R)-2-[(4-Biphenylylsulfonyl)amino]-3-phenylpropionic Acid}
A potent inhibitor of MMP-2 (IC 50 = 3 0 nM) and MMP-9 (IC 50 = 240 nM).
MMP-2/MMP-9 Inhibitor II 444249 {(2R)-[(4-Biphenylylsulfonyl)amino]-N-hydroxy-3-phenylpropionamide}
A potent inhibitor of type IV collagenases, MMP-2 (IC 50 = 7 nM) and
MMP-9 (IC 50 = 30 nM).
MMP-2/MMP-9 Inhibitor III 444251 A cyclic peptide that acts as a potent inhibitor of MMP-2 (IC 50 = 0 mM)
and MMP-9 (IC 50 = 0 mM).
MMP-2/MMP-9 Inhibitor IV 444274 (SB-3CT)
A potent, selective, slow-binding, and mechanism-based inhibitor of
human MMP-2 (K i = 3.9 nM) and MMP-9 (K i = 600 nM). Does not
affect the activities of MMP- (K i = 206 mM) MMP-3 (K i = 5 mM), or
MMP-7 (K i = 96 mM).
N MMP-2/MMP-9 Inhibitor V 444285 A cell-permeable sulfonamido analog of SB-3CT (Cat. No. 444274) that
displays enhanced aqueous solubility and improved selectivity
(K i = 6 nM, 80 nM, and 900 nM for MMP-2, -9 and - 4, respectively).
Binds to the active-site and acts as a mechanism-based, irreversible
inhibitor of MMPs.
MMP-3 Inhibitor I 444218 (Ac-RCGVPD-NH 2 ; Stromelysin-1 Inhibitor)
An inhibitor of MMP-3 (IC 50 = 5 mM). Based on a segment from the
conserved region of the N-terminal propeptide domain.
MMP-3 Inhibitor II 444225 [N-Isobutyl-N-(4-methoxyphenylsulfonyl)-glycylhydroxamic Acid; NNGH]
A potent inhibitor of human MMP-3 (K i = 30 nM).
MMP-3 Inhibitor III 444242 {N-[[(4,5-Dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]carbonyl]-Lphenylalanine}
A potent inhibitor of MMP-3 (K i = 3.2 mM) that inhibits MMP-2 only at
higher concentrations (K i >200 mM).
MMP-3 Inhibitor IV 444243 {a-[[[(4,5-Dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]carbonyl]amino]
-N-(cyclohexylmethyl)-(S)-benzenepropanamide}
A potent inhibitor of MMP-3 (K i = 8 0 nM) that inhibits MMP-2 only at
higher concentrations (K i >200 mM).
MMP-3 Inhibitor V 444260 (4-Dibenzofuran-2´-yl-4-hydroximino-butyric Acid)
A potent and competitive inhibitor of MMP-3. Inhibits both human and
rabbit MMP-3 (wild type and mutants) with K i values in the low mM range.
MMP-3 Inhibitor VI 444265 [4-(4´-Biphenyl)-4-hydroxyimino-butyric Acid]
A potent and competitive inhibitor of MMP-3. Inhibits both human and
rabbit MMP-3 (wild type and mutants) with K i values in the low mM range.
MMP-3 Inhibitor VII 444280 {3-[4-(4-cyanophenyl)phenoxy]propanohydroxamic Acid}
A potent nonpeptide inhibitor of MMP-3 (stromelysin; IC 50 = 25 nM
against the catalytic domain).
MMP-3 Inhibitor VIII 444281 {N-Hydroxy-2(R)-{[(4-methoxyphenyl)sulfonyl]-[benzylamino]}-4methylpentanamide}
A cell-permeable, potent inhibitor of human MMP-3 (stromelysin;
K i = 23 nM) and murine macrophage metalloelastase (MME/MMP- 2;
IC 50 = 3 nM).
MMP-8 Inhibitor I 444237 {(3R)-(+)-[2-(4-Methoxybenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-
3-hydroxamate]}
MMP-8 Inhibitor I,
Negative Control
A potent inhibitor of MMP-8 (IC 50 = 4 nM).
444238 {(3S)-(–)-[2-(4-Methoxybenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-
3-hydroxamate]}
A negative control for MMP-8 Inhibitor I (Cat. No. 444237; IC 50 = mM).
5 mg $ 46
2 mg $ 5
5 mg $ 46
mg $ 5
mg $ 36
500 mg $ 23
500 mg $ 34
5 mg $202
5 mg $85
2 mg $ 42
2 mg $ 7
5 mg $84
5 mg $55
mg $ 03
5 mg $ 78
mg $79
mg $55
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