2 Results for "

active site cleft

" in MedChemExpress (MCE) Product Catalog:
Products (2)

2 Results for "active site cleft" in MCE Product Catalog:

  • Targets Recommended:
CP-69799
CP-69799
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Cat. No.: HY-P1609
CAS No.: 105116-61-8
Target:  

Renin Enteropeptidase

Research Areas:  

Cardiovascular Disease

CP-69799 is an azahomostatine-containing oligopeptide transition-state analogue inhibitor with a hog renin IC50 of 6e-9 M, human plasma renin IC50 of 3e-7 M and Ki of 0.310 μM, and endothiapepsin Ki of 0.27 μM. CP-69799 binds endothiapepsin’s active site cleft in extended conformation, fills S4 to S3' pockets, displaces native solvent molecules, induces domain rotation, and reduces thermal mobility of endothiapepsin’s flap and helix regions. CP-69799 acts as a transition-state analogue inhibitor of hog renin and human plasma renin. CP-69799 contains a polar lysine residue at the P2' position, with a nitrogen atom replacing the P1' Cα atom of the hydroxyethylene dipeptide isostere. CP-69799 can be used for the research of hypertension .
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LAF-153
LAF-153
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Cat. No.: HY-183876
CAS No.: 661482-39-9
Target:  

Aminopeptidase

Research Areas:  

Others

LAF-153 is a Methionine Aminopeptidase-2 (MetAP-2) inhibitor with human IC50 values of 0.074 μM and 0.16 μM.LAF-153 has a t-butyl group extending into the innermost portion of the MetAP-2 cleft, a lactam ring coordinated in the enzyme’s shallow surface pocket, and three hydroxyl groups coordinating to the two cobalt ions in the enzyme’s active site .
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