1. Cytoskeleton Protein Tyrosine Kinase/RTK
  2. Integrin VEGFR
  3. Obtustatin

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.

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Obtustatin

Obtustatin Chemical Structure

CAS No. : 404882-00-4

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Based on 4 publication(s) in Google Scholar

Other Forms of Obtustatin:

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Description

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[1][2][3].

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.

In Vivo

Obtustatin (5 µg/disk; local administration; single dose at 24 hours after initial filter paper placement) potently inhibits FGF2-induced angiogenesis in the chick embryo chorioallantoic membrane (CAM) model[1].
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.

Animal Model: embryos (10-day-old)[1]
Dosage: 5 µg/disk
Administration: topical; single application at 24 hours after initial disk placement
Result: Reduced the FGF2-stimulated angiogenesis index (vessel branch points) from 179 to 79, corresponding to 84% inhibition of angiogenesis.
Animal Model: C57BL/6 (4 animals per group)[1]
Dosage: 5 mg/kg
Administration: i.p.; every other day; 1 week
Result: Reduced tumor volume by approximately 50% after 1 week of treatment compared to control.
Animal Model: unspecified[2]
Dosage: 1 mg/kg
Administration: intratumoral injection; daily; 5 days
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.
Molecular Weight

4393.06

Formula

C184H284N52O57S8

CAS No.
Appearance

Solid

Color

White to off-white

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)

Sequence Shortening

CTTGPCCRQCKLKPAGTTCWKTSLTSHYCTGKSCDCPLYPG (Disulfide bridge: Cys1-Cys10, Cys6-Cys29, Cys7-Cys34, Cys19-Cys36)

Shipping

Room temperature in continental US; may vary elsewhere.

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)

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2276 mL 1.1382 mL 2.2763 mL
5 mM 0.0455 mL 0.2276 mL 0.4553 mL
View the 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.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.94%

References

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
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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Obtustatin
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HY-P1408
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