VSPPLTLGQLLS
Based on 1 Customer Validation
VSPPLTLGQLLS is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.53%
- CAS 番号: 1206896-24-3
- 分子式: C56H97N13O17
- 分子量:1224.45
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保管条件:
Sealed storage, away from moisture and light.
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)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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生物活性
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FGFR3 |
K650M-FGFR3 |
K644E FGFR3 |
VSPPLTLGQLLS (5 μM and 10 μM; 24 h and 48 h) inhibits human primary lymphatic endothelial cell (LEC)s proliferation, migration, and tubule formation[1].
VSPPLTLGQLLS shows effective inhibition in FGFR3 phosphorylation in LECs and also demonstrated to be effective in ATDC5 chondrogenic cells, 293T cells, explanted metatarsal bone cultures, and an in vivo mouse model of thanatophoric dysplasia II[1][2].
VSPPLTLGQLLS (10 μM; 6 h) inhibits tyrosine kinase activity of FGFR3 and its typical downstream molecules, extracellular signal-regulated kinase/mitogen-activated protein kinase[2].
VSPPLTLGQLLS (0, 1, 10, and 50 μM; 24 h and 3 or 7 days, respectively) also promotes proliferation and chondrogenic differentiation of cultured ATDC5 chondrogenic cells[2].
VSPPLTLGQLLS (10 μM; 0-60 min) inhibits the ERK/MAPK pathway in FGFR3-expressing chondrocytic cell line ATDC5[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human primary lymphatic endothelial cell (LEC)s; ATDC5 chondrogenic cells
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Concentration:10 μM
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Incubation Time:0, 5, 10, 30, 45, 60 min
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Result:Inhibited FGFR3 phosphorylation at Tyr 724 in human primary lymphatic endothelial cell (LEC)s.
Inhibited the FGF2-mediated ERK/MAPK phosphorylation in FGFR3-expressing chondrocytic cell line ATDC5.
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Cell Line:Human primary lymphatic endothelial cell (LEC)s
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Concentration:2.5 μM, 5 μM, and 10 μM
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Incubation Time:15 min for pre-incubation and co-incubation with 1 μM 9-cisRA for 48 hr
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Result:Inhibited LEC proliferation.
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Cell Line:Human primary lymphatic endothelial cell (LEC)s
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Concentration:5 μM
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Incubation Time:15 min for pre-incubation and co-incubation with 1 μM 9-cisRA for 24 hr; observed at 0, 24, 48 hr
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Result:Inhibited LEC migration tubule formation.
VSPPLTLGQLLS alleviates the bone growth retardation in bone rudiments from mice mimicking human thanatophoric dysplasia type II (TDII), reversed the neonatal lethality of TDII mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lymphatic reporter mice, Prox1-GFP model[1]
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Dosage:1 mM
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Administration:Intranasal dropping; once daily for 7 days; accompanied with 1 mM 9-cisRA or not
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Result:Significantly inhibited total lymphatic vessel length and number of sprouts compared increase induced by 9-cisRA.
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Animal Model:Fgfr3Neo-K644E/+EIIa-Cre mice (TDII mice) from Fgfr3Neo-K644E/+ mice crossed with heterozygous EIIa-Cre mice[2]
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Dosage:10 μM
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Administration:Treated for 7 days
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Result:Suppressed FGFR3-mediated growth inhibition in cultured murine metatarsal bones.
Rescued the lethal phenotype in thanatophoric dysplasia type II (TDII) mice.
Rescued the abnormal growth plate and the lung phenotypes in the TDII mice.
化学情報
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CAS 番号 1206896-24-3
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性状 Solid
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分子量 1224.45
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分子式 C56H97N13O17
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Color White to off-white
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シーケンスの短縮
VSPPLTLGQLLS
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture and light
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)
溶剤 & 溶解度
H2O : 50 mg/mL (40.83 mM; Need ultrasonic)
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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参考文献
[1]. Perrault DP, et al. Small Peptide Modulation of Fibroblast Growth Factor Receptor 3-Dependent Postnatal Lymphangiogenesis. Lymphat Res Biol. 2019 Feb;17(1):19-29. [Content Brief]
[2]. Jin M, et al. A novel FGFR3-binding peptide inhibits FGFR3 signaling and reverses the lethal phenotype of mice mimicking human thanatophoric dysplasia. Hum Mol Genet. 2012 Dec 15;21(26):5443-55. [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). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.8167 mL | 4.0835 mL | 8.1669 mL | 20.4173 mL |
| 5 mM | 0.1633 mL | 0.8167 mL | 1.6334 mL | 4.0835 mL | |
| 10 mM | 0.0817 mL | 0.4083 mL | 0.8167 mL | 2.0417 mL | |
| 15 mM | 0.0544 mL | 0.2722 mL | 0.5445 mL | 1.3612 mL | |
| 20 mM | 0.0408 mL | 0.2042 mL | 0.4083 mL | 1.0209 mL | |
| 25 mM | 0.0327 mL | 0.1633 mL | 0.3267 mL | 0.8167 mL | |
| 30 mM | 0.0272 mL | 0.1361 mL | 0.2722 mL | 0.6806 mL | |
| 40 mM | 0.0204 mL | 0.1021 mL | 0.2042 mL | 0.5104 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
VSPPLTLGQLLS 関連分類
HY-P3695 関連分類
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