MMP-9/MMP-13 inhibitor IA piperazine-based, cell-permeable inhibitor of MMP-9 and MMP-13

MMP-9/MMP-13 inhibitor I (CAS 204140-01-2)

MMP-9/MMP-13 inhibitor I | CAS 204140-01-2 is rated 5.0 out of 5 by 1.
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Synonym: N-Hydroxy-1-(4-methoxyphenyl)sulfonyl-4-(4-biphenylcarbonyl)piperazine-2-carboxamide
Application: A piperazine-based, cell-permeable inhibitor of MMP-9 and MMP-13
CAS Number: 204140-01-2
Purity: ≥95%
Molecular Weight: 495.55
Molecular Formula: C25H25N3O6S
* Refer to Certificate of Analysis for lot specific data (including water content).
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MMP-9/MMP-13 Inhibitor I is a piperazine-based, cell-permeable, and highly potent inhibitor of MMP-9 (IC50 = 900 pM) and MMP-13 (IC50 = 900 pM). Reported to inhibit MMP-1 and MMP-3 at much higher concentrations (IC50 = 43 nM and 23 nM, respectively). Also acts as an inhibitor of MMP-7 (IC50 = 930 nM).


References

1. Cheng, M. et al. 2000. J. Med. Chem. 43(3): 369-380. PMID: 10669564
2. Prato, M. et al. 2005. J. Immunol. 175(10): 6436-6442. PMID: 16272296

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mg/ml), and methanol (1 mg/ml).
Storage :
Store at -20° C
Melting Point :
336.84° C (Predicted)
Boiling Point :
765.98° C (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.64 (Predicted)
IC50 :
MMP-9: IC50 = 0.9 nM; MMP-13 : IC50 = 0.9 nM; MMP-3: IC50 = 23 nM; MMP-1: IC50 = 43 nM; MMP-7: IC50 = 930 nM
pK Values :
pKa: 9.38 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9983251
MDL Number :
MFCD03453559
SMILES :
C1=C(C=CC=C1)C2=CC=C(C=C2)C(=O)N3CC(N(CC3)C[S](=O)(=O)C4=CC=C(C=C4)OC)C(=O)NO

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Certificate of Analysis

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MMP-9/MMP-13 inhibitor I  Product Citations

See how others have used MMP-9/MMP-13 inhibitor I. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 25582709  Blocki, A. et al. 2015. Molecular therapy : the journal of the American Society of Gene Therapy. 23: 510-22.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Prato Prato, M. et al. (PubMed 16272296) demonstrate that trophozoite-parasitized RBCs/hemozoin-fed adherent human monocytes displayed increased MMP-9 activity and protein/mRNA expression, produced TNF-alpha time-dependently, and showed higher matrix invasion ability. MMP-9 activation was specific for trophozoite/hemozoin-fed monocytes, was dependent on TNF-alpha production, and abrogated by anti-TNF-alpha Ab and by MMP-9/MMP-13 inhibitor I. -SCBT Publication Review
Date published: 2015-02-10
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