HSDVHK-NH2

Cat No.:V27085 Purity: ≥98%
HSDVHK-NH2 is an inhibitor (blocker/antagonist) of the integrin αvβ3-vitreous binding protein interaction with IC50 of 1.74 pg/mL (2.414 pM).
HSDVHK-NH2 Chemical Structure CAS No.: 848644-86-0
Product category: Integrin
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
HSDVHK-NH2 is an inhibitor (blocker/antagonist) of the integrin αvβ3-vitreous binding protein interaction with IC50 of 1.74 pg/mL (2.414 pM).
Biological Activity I Assay Protocols (From Reference)
Targets
αvβ3 2.74 nM (IC50)
ln Vitro
In comparison to the PBS control group, HSDVHK dramatically reduced the bFGF-induced cell migration[1]. Since HSDVHK-NH2 (P11) is inactive for the complex formation of a denatured version of integrin–vitronectin, its recognition of the Arg-Gly-Asp (RGD)-binding site is site-specific. At an IC50 value of 25.72 nM, HSDVHK-NH2 (P11) exhibits substantial antagonistic activity against the avb3-GRGDSP interaction[2]. By inducing HUVEC cell death by caspase activations, HSDVHK-NH2 (P11) suppresses HUVEC proliferation. This mechanism is associated with enhanced p53 expression[3].
Cell Assay
Cell Proliferation Assay [3]
Cell Types: HUVEC cells.
Tested Concentrations: 0.1, 1, 10, and 100 μg/mL.
Incubation Duration: 72 h.
Experimental Results: Dramatically inhibited HUVEC proliferation on denatured collagen-coated plates in a dose-dependent manner.
References
[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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C30H48N12O9
Molecular Weight
720.78
CAS #
848644-86-0
Related CAS #
HSDVHK-NH2 TFA
SMILES
O=C([C@H](C(C)C)NC([C@H](CC(=O)O)NC([C@H](CO)NC([C@H](CC1=CN=CN1)N)=O)=O)=O)N[C@H](C(N[C@H](C(N)=O)CCCCN)=O)CC1=CN=CN1
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O : 250 mg/mL (346.85 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 100 mg/mL (138.74 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.3874 mL 6.9369 mL 13.8739 mL
5 mM 0.2775 mL 1.3874 mL 2.7748 mL
10 mM 0.1387 mL 0.6937 mL 1.3874 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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