Histatin 5 (TFA)(115966-68-2,free)

Research use only, not for human use.

Histatin 5 TFA inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively.Histatin 5 is a member of a family of low-molecular-weight salivary proteins secreted by parotid, submandibular, and sublingual glands. Using biotinylated gelatin as a substrate, Histatin 5 is found to inhibit the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively.

Histatin 5 TFA inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively.Histatin 5 is a member of a family of low-molecular-weight salivary proteins secreted by parotid, submandibular, and sublingual glands. Using biotinylated gelatin as a substrate, Histatin 5 is found to inhibit the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively. To localize the domain responsible for this inhibition, three peptides containing different regions of Histatin 5 are synthesized and tested as inhibitors of MMP-9. Peptides comprising residues 1 to 14 and residues 4 to 15 of Histatin 5 show much lower inhibitory activities (IC50s, 21.4 and 20.5 μM, respectively), while a peptide comprising residues 9 to 22 showed identical activity to Histatin 5 against MMP-9. Kinetic analysis of the inhibition of the Arg-gingipain reveals that Histatin 5 is a competitive inhibitor, affecting only the Km with a Ki of 15 μM. Histatin 5 is an inhibitor of mitochondrial respiration.The human salivary antifungal peptide Histatin 5 is taken up by Candida albicans cells and associates intracellularly with mitochondria. Histatin 5 inhibits respiration of isolated C. albicans mitochondria as well as the respiration of intact blastoconidia in a dose and time-dependent manner. Histatin 5 at a concentration of 33 uM inhibits state 2 respiration.

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Metabolic Enzyme/Protease

MMP

MMP-2|MMP-2

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3150.31

C135H196N51F3O35

>98% (HPLC)

O=C(O)C(F)(F)F.O=C(O)CC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](N)CC(O)=O)=O)CO)=O)CC1=CNC=N1)=O)C)=O)CCCCN)=O)CCCNC(N)=N)=O)CC2=CNC=N2)=O)CC3=CNC=N3)=O)=O)CC4=CC=C(O)C=C4)=O)CCCCN)=O)CCCNC(N)=N)=O)CCCCN)=O)CC5=CC=CC=C5)=O)CC6=CNC=N6)=O)C(N[C@@H](CCCCN)C(N[C@@H](CC7=CNC=N7)C(N[C@@H](CC8=CNC=N8)C(N[C@@H](CO)C(N[C@@H](CC9=CNC=N9)C(N[C@@H](CCCNC(N)=N)C(NCC(N[C@H](C(O)=O)CC%10=CC=C(O)C=C%10)=O)=O)=O)=O)=O)=O)=O)=O

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(-20℃)

With Ice Pack

≥ 2 years