Histatin 5 

Histatin 5 inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC₅₀s of 0.57 and 0.25 μM, respectively.

IC50: 0.57 μM (MMP-2), 0.25 μM (MMP-9)^[1]

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 inhibits 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 (IC₅₀, 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 K_m with a K_i of 15 μM^[1]. 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 μM inhibits state 2 respiration^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

3036.29

C₁₃₃H₁₉₅N₅₁O₃₃

115966-68-2

Asp-Ser-His-Ala-Lys-Arg-His-His-Gly-Tyr-Lys-Arg-Lys-Phe-His-Glu-Lys-His-His-Ser-His-Arg-Gly-Tyr

DSHAKRHHGYKRKFHEKHHSHRGY

[DSHAKRHHGYKRKFHEKHHSHRGY]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Gusman H, et al. Salivary histatin 5 is an inhibitor of both host and bacterial enzymes implicated in periodontaldisease. Infect Immun. 2001 Mar;69(3):1402-8.  [Content Brief]

  [2]. Helmerhorst EJ, et al. The human salivary peptide histatin 5 exerts its antifungal activity through the formation ofreactive oxygen species. Proc Natl Acad Sci U S A. 2001 Dec 4;98(25):14637-42.  [Content Brief]