An broad-spectrum MMP inhibitor (IC50s = 6.1

PD 166793 – 10 mg

Brand:
Cayman
CAS:
199850-67-4
Storage:
-20
UN-No:
Non-Hazardous - /

PD 166793 is a broad-spectrum matrix metalloproteinase (MMP) inhibitor (IC50s = 6.1, 0.047, 0.012, 7.2, 7.9, 0.008, and 0.24 μM for MMP-1, MMP-2, MMP-3, MMP-7, MMP-9, MMP-13CD, and MMP-14CD, respectively).{39768} It reverses peroxynitrite-induced decreases in contraction cease time, a measure of cardiac contractility, in isolated rat ventricular myocytes when used at a concentration of 2 μM.{39769} In vivo, PD 166793 (2 mg/kg per day, p.o.) reduces left ventricular (LV) peak wall stress in a porcine model of congestive heart failure.{39770} It reduces LV dilation and preserves systolic function in a rat model of progressive heart failure.{39768} PD 166793 also inhibits age-associated increases in aortic gelatinase and interstitial collagenase activity and mean arterial pressure in rats.{39771}  

 

Available on backorder

Add to quotes
SKU: 23762 - 10 mg Category:

Description

An broad-spectrum MMP inhibitor (IC50s = 6.1, 0.047, 0.012, 7.2, 7.9, 0.008, and 0.24 μM for MMP-1, MMP-2, MMP-3, MMP-7, MMP-9, MMP13CD, and MMP-14CD, respectively); reverses peroxynitrite-induced decreases in contraction cease time in isolated rat ventricular myocytes at 2 μM; reduces LV peak wall stress in a porcine model of congestive heart failure at 2 mg/kg per day; reduces LV dilation and preserves systolic function in a rat model of progressive heart failure; inhibits age-associated increases in aortic gelatinase and interstitial collagenase activity and mean arterial pressure in rats,

Formal name: N-[(4′-bromo[1,1′-biphenyl]-4-yl)sulfonyl]-L-valine

Synonyms: 

Molecular weight: 412.3

CAS: 199850-67-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Myocardial Contractility

Related products

  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 1 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 50 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 50 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page