Obtustatin
Based on 4 publication(s) in Google Scholar
Obtustatin is a non-RGD disintegrin consisting of 41 residues. Obtustatin inhibits the adhesion of α1β1 integrin to type IV Collagen (HY-NP003), blocks α1β1 integrin signaling in endothelial cells, and suppresses FGF2-induced angiogenesis. Obtustatin inhibits tumor progression in mouse models and upregulates VEGF expression in sarcoma-bearing mice. Obtustatin can be used in research related to Lewis lung carcinoma and S-180 sarcoma.
For research use only. We do not sell to patients.
- Purity : 99.94%
- CAS No.: 404882-00-4
- Formula: C184H284N52O57S8
- Molecular Weight:4393.06
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Storage:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Obtustatin
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Biological Activity
Description
In Vitro
Obtustatin potently inhibits the binding of soluble α1β1 integrin to type IV Collagen (HY-NP003), with an IC50 of 0.8 nM[1].
Obtustatin (0-18 nM; 30 min) inhibits the adhesion of α1K562 cells to type IV collagen, with an IC50 of 2 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Obtustatin (5 mg/kg; i.p.; once every other day; for 1 week) significantly inhibits the growth of established Lewis lung carcinoma in syngeneic C57BL/6 mice[1].
Obtustatin (1 mg/kg; intratumoral injection; once daily for 5 consecutive days) inhibits the growth of S-180 sarcoma in mice via an anti-angiogenic mechanism associated with the upregulated expression of VEGF, with an inhibition rate of 33%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:embryos (10-day-old)[1]
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Dosage:5 µg/disk
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Administration:topical; single application at 24 hours after initial disk placement
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Result:Reduced the FGF2-stimulated angiogenesis index (vessel branch points) from 179 to 79, corresponding to 84% inhibition of angiogenesis.
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Animal Model:C57BL/6 (4 animals per group)[1]
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Dosage:5 mg/kg
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Administration:i.p.; every other day; 1 week
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Result:Reduced tumor volume by approximately 50% after 1 week of treatment compared to control.
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Animal Model:unspecified[2]
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Dosage:1 mg/kg
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Administration:intratumoral injection; daily; 5 days
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Result:Reduced average S-180 sarcoma weight by 33% (average inhibitory rate 32.5%).
Showed no significant weight loss in treated mice.
Increased VEGF expression in treated tumors.
Left expression levels of caspase 8, procaspase 9, caspase 5, and cleaved caspase 3 unchanged relative to controls.
Chemical Information
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CAS No. 404882-00-4
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Appearance Solid
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Molecular Weight 4393.06
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Formula C184H284N52O57S8
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Color White to off-white
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Sequence
Cys-Thr-Thr-Gly-Pro-Cys-Cys-Arg-Gln-Cys-Lys-Leu-Lys-Pro-Ala-Gly-Thr-Thr-Cys-Trp-Lys-Thr-Ser-Leu-Thr-Ser-His-Tyr-Cys-Thr-Gly-Lys-Ser-Cys-Asp-Cys-Pro-Leu-Tyr-Pro-Gly (Disulfide bridge: Cys1-Cys10, Cys6-Cys29, Cys7-Cys34, Cys19-Cys36)
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Sequence Shortening
CTTGPCCRQCKLKPAGTTCWKTSLTSHYCTGKSCDCPLYPG (Disulfide bridge: Cys1-Cys10, Cys6-Cys29, Cys7-Cys34, Cys19-Cys36)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (4)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Targeting Microglial CD49a Inhibits Neuroinflammation and Demonstrates Therapeutic Potential for Parkinson's Disease. [Abstract]2025 Dec 29:e15138. PMID: 41462565 -
Acta Neuropathol Commun
JMJD6-driven epigenetic activation of COL4A2 reprograms glioblastoma vascularization via integrin α1β1-dependent PI3K/MAPK signaling. [Abstract]2025 Sep 24;13(1):194. PMID: 40993804 -
J Cell Sci
Bile canaliculi formation in primary hepatocytes requires α1β1 integrin-dependent adherens junction re-organization. [Abstract]2025 Dec 1;138(23):jcs264412. PMID: 41347643 -
Exp Eye Res
Therapeutic targeting of ITGA1 delayed retinoblastoma progression through suppression of STAT3 signaling. [Abstract]2025 Nov:260:110636. PMID: 40939856
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (22.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (0.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (0.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Human pluripotent stem cell endothelial-cell differentiation
Human pluripotent stem cell endothelial differentiation is based on stepwise developmental patterning: early activation of WNT/GSK3β inhibition promotes mesodermal or vascular progenitor entry, followed by endothelial specification using VEGF-related signaling, BMP4, FGF2, Notch modulation, or cAMP depending on the published protocol. Endothelial differentiation is read out by acquisition of CD31, CD34, VE-cadherin/CD144, KDR/VEGFR2, vWF, Tie2, NOS3, acetylated LDL uptake, tube/network formation, barrier function, and in vivo vessel-forming capacity where tested.
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Vascular/Branching Fractal Analysis
Vascular/branching fractal analysis quantifies the geometric complexity of vessel trees or vascular networks from segmented 2D images, commonly by converting vessels into binary and/or skeletonized maps and estimating fractal dimension using box-counting or related approaches. Fractal dimension is interpreted as an image-derived readout of vascular branching complexity, space filling, or density, and has been applied to retinal photographs, fluorescein angiography, OCT angiography, capillary perfusion maps, and in vitro Matrigel angiogenesis networks. The assay readout is generated from vessel-positive pixels after image preprocessing, vessel segmentation, binarization, and optional skeletonization; reported outputs include fractal dimension, vessel density, branchpoint density, endpoint density, vessel length density, tortuosity, and generation-based branching metrics when VESGEN-style analysis is used. The biological interpretation is limited to quantitative vascular patterning and s
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Endothelial Tube Formation Assay
Endothelial tube formation assay evaluates the ability of endothelial cells to attach, migrate, align, and organize into capillary-like networks when cultured on gelled basement membrane extract or Matrigel; the readout is the morphology and quantity of tube-like networks, which reflects an in vitro endothelial morphogenesis step related to angiogenesis. Basement membrane extract/Matrigel provides laminin-rich extracellular matrix cues that support endothelial differentiation into capillary-like structures, but it can contain biologically active growth factors, so growth-factor-reduced matrix is preferred when testing defined angiogenic stimulators or inhibitors.
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Endothelial Cell Migration/Angiogenic Sprouting Assay
Endothelial cell migration and angiogenic sprouting assays are in vitro (and partially ex vivo-adapted) functional models that quantify the ability of endothelial cells to undergo coordinated migration, extracellular matrix invasion, and multicellular organization into capillary-like sprouts in response to pro-angiogenic stimuli such as VEGF, bFGF, or conditioned microenvironments. These assays are used to model early angiogenic events including tip-cell formation, directional migration, and lumen-like sprout extension, which collectively reflect angiogenic activation and vascular morphogenesis processes observed in vivo.
Purity & Documentation
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Data Sheet (291 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Marcinkiewicz C, et al. Obtustatin: a potent selective inhibitor of alpha1beta1 integrin in vitro and angiogenesis in vivo. Cancer Res. 2003 May 1;63(9):2020-3. [Content Brief]
[2]. Ghazaryan N, et al. The antitumor efficacy of monomeric disintegrin obtustatin in S-180 sarcoma mouse model. Invest New Drugs. 2019;37(5):1044-1051. [Content Brief]
[3]. Paz Moreno-Murciano M, et al. NMR solution structure of the non-RGD disintegrin obtustatin. J Mol Biol. 2003;329(1):135-145. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.2276 mL | 1.1382 mL | 2.2763 mL | 5.6908 mL |
| 5 mM | 0.0455 mL | 0.2276 mL | 0.4553 mL | 1.1382 mL | |
| 10 mM | 0.0228 mL | 0.1138 mL | 0.2276 mL | 0.5691 mL | |
| 15 mM | 0.0152 mL | 0.0759 mL | 0.1518 mL | 0.3794 mL | |
| 20 mM | 0.0114 mL | 0.0569 mL | 0.1138 mL | 0.2845 mL |
Obtustatin Related Classifications
HY-P1408 Related Classifications
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