For research use only. Not for therapeutic Use.
HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM)[1][2].
HSDVHK significantly inhibited bFGF-induced cell migration compared to the PBS control group[1].
The Arg-Gly-Asp (RGD)-binding site recognition by HSDVHK-NH2 (P11) is site specific because the HSDVHK-NH2 (P11) is inactive for the complex formation of a denatured form of integrin–vitronectin. HSDVHK-NH2 (P11) shows a strong antagonism against avb3-GRGDSP interaction with an IC50 value of 25.72 nM[2].
HSDVHK-NH2 (P11) inhibits the HUVEC proliferation due to the induction of HUVEC cell death through caspases activations and its mechanism is related with increased p53 expression[3].
| Catalog Number | P000275 |
| CAS Number | 848644-86-0 |
| Synonyms | (3S)-3-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid |
| Molecular Formula | C30H48N12O9 |
| Purity | ≥95% |
| InChI | InChI=1S/C30H48N12O9/c1-15(2)24(30(51)40-20(8-17-11-35-14-37-17)27(48)38-19(25(33)46)5-3-4-6-31)42-28(49)21(9-23(44)45)39-29(50)22(12-43)41-26(47)18(32)7-16-10-34-13-36-16/h10-11,13-15,18-22,24,43H,3-9,12,31-32H2,1-2H3,(H2,33,46)(H,34,36)(H,35,37)(H,38,48)(H,39,50)(H,40,51)(H,41,47)(H,42,49)(H,44,45)/t18-,19-,20-,21-,22-,24-/m0/s1 |
| InChIKey | FSVRGWKWZIRBPC-KESUXUJOSA-N |
| SMILES | CC(C)C(C(=O)NC(CC1=CN=CN1)C(=O)NC(CCCCN)C(=O)N)NC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(CC2=CN=CN2)N |
| Reference | [1]. Yoonsuk Lee, et al. High-throughput screening of novel peptide inhibitors of an integrin receptor from the hexapeptide library by using a protein microarray chip. J Biomol Screen. 2004 Dec;9(8):687-94. [2]. Youngjin Choi, et al. Site-specific inhibition of integrin alpha v beta 3-vitronectin association by a ser-asp-val sequence through an Arg-Gly-Asp-binding site of the integrin. Proteomics. 2010 Jan;10(1):72-80. [3]. Ji-Young Bang, et al. Pharmacoproteomic analysis of a novel cell-permeable peptide inhibitor of tumor-induced angiogenesis. Mol Cell Proteomics. 2011 Aug;10(8):M110.005264. |
