| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
αvβ3 2.74 nM (IC50)
HSDVHK-NH2 targets the integrin αvβ3, a cell surface receptor that mediates cell adhesion to the extracellular matrix protein vitronectin. Integrin αvβ3 plays a critical role in angiogenesis, tumor metastasis, and bone resorption. By antagonizing the αvβ3-vitronectin interaction, HSDVHK-NH2 inhibits integrin-mediated signaling and cell adhesion. |
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| 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].
In vitro, HSDVHK-NH2 potently inhibits the integrin αvβ3-vitronectin interaction with an IC50 of 1.74 pg/mL (2.414 pM). This high potency makes it one of the most effective peptide-based integrin antagonists reported. The compound inhibits cell adhesion, migration, and signaling mediated by αvβ3 integrin, making it a valuable tool for studying angiogenesis and cancer metastasis. |
| ln Vivo |
In vivo activity data for HSDVHK-NH2 are not extensively detailed in the available literature. As a potent integrin αvβ3 antagonist, the compound would be expected to inhibit angiogenesis, tumor growth, and metastasis in vivo. Integrin αvβ3 is a well-validated target for anti-angiogenic therapy, and HSDVHK-NH2's high potency suggests potential for therapeutic applications.
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| Enzyme Assay |
Specific cell-free receptor binding assay protocols for HSDVHK-NH2 involve competitive binding assays using purified integrin αvβ3 protein and immobilized vitronectin. The peptide's ability to displace a labeled ligand or inhibit vitronectin binding to integrin αvβ3 is measured using ELISA or surface plasmon resonance. IC50 is determined from concentration-response curves.
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| 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. In vitro cell-based assays for HSDVHK-NH2 use cell lines expressing integrin αvβ3, such as endothelial cells or cancer cells. Cells are treated with HSDVHK-NH2, and cell adhesion to vitronectin-coated surfaces is measured. Cell migration and invasion assays (such as transwell or scratch assays) are used to assess the compound's functional effects. Signaling pathways downstream of integrin αvβ3 are evaluated by Western blot. |
| Animal Protocol |
In vivo animal studies for HSDVHK-NH2 are not detailed in the available literature. As an integrin αvβ3 antagonist, typical in vivo evaluation would involve tumor xenograft models to assess inhibition of angiogenesis and tumor growth. Matrigel plug assays or choroidal neovascularization models may be used to evaluate anti-angiogenic effects.
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| ADME/Pharmacokinetics |
HSDVHK-NH2 has a molecular formula of C30H48N12O9 and a molecular weight of 720.78 g/mol. It is a synthetic hexapeptide with a C-terminal amide that enhances stability. The compound is supplied as a solid powder and is soluble in aqueous buffers. Purity is typically ≥95%. Storage: at -20°C, protected from light and moisture.
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| Toxicity/Toxicokinetics |
Specific toxicological data for HSDVHK-NH2 are not detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic applications. As an integrin αvβ3 antagonist, potential toxicities may relate to effects on angiogenesis and bone homeostasis, though formal toxicological profiles are not reported.
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| References |
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| Additional Infomation |
HSDVHK-NH2 (CAS 848644-86-0) is a synthetic hexapeptide with a C-terminal amide that acts as a potent antagonist of the integrin αvβ3-vitronectin interaction with an IC50 of 1.74 pg/mL (2.414 pM). It is used in research on angiogenesis, cancer metastasis, and cell adhesion. No clinical trial or approved indication data are available.
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| Molecular Formula |
C30H48N12O9
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|---|---|
| Molecular Weight |
720.777125358582
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| Exact Mass |
720.366
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| CAS # |
848644-86-0
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| Related CAS # |
HSDVHK-NH2 TFA
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| PubChem CID |
90488969
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| Appearance |
White to off-white solid powder
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| LogP |
-6.6
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
51
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| Complexity |
1210
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| Defined Atom Stereocenter Count |
6
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| SMILES |
[C@H](C(=O)N[C@H](C(=O)N)CCCCN)(NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC1NC=NC=1)CC1NC=NC=1
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| InChi Key |
FSVRGWKWZIRBPC-KESUXUJOSA-N
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| InChi Code |
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
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| Chemical Name |
(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
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
H2O : 250 mg/mL (346.85 mM)
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|---|---|
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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