2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. VSPPLTLGQLLS

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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VSPPLTLGQLLS Chemical Structure

VSPPLTLGQLLS Chemical Structure

CAS No. : 1206896-24-3

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target[1][2]

FGFR3

 

K650M-FGFR3

 

K644E FGFR3

 

In Vitro

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.

VSPPLTLGQLLS Related Antibodies

Western Blot Analysis[1][2]

Cell Line: Human primary lymphatic endothelial cell (LEC)s; ATDC5 chondrogenic cells
Concentration: 10 μM
Incubation Time: 0, 5, 10, 30, 45, 60 min
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.

Cell Proliferation Assay[1]

Cell Line: Human primary lymphatic endothelial cell (LEC)s
Concentration: 2.5 μM, 5 μM, and 10 μM
Incubation Time: 15 min for pre-incubation and co-incubation with 1 μM 9-cisRA for 48 hr
Result: Inhibited LEC proliferation.

Cell Migration Assay [1]

Cell Line: Human primary lymphatic endothelial cell (LEC)s
Concentration: 5 μM
Incubation Time: 15 min for pre-incubation and co-incubation with 1 μM 9-cisRA for 24 hr; observed at 0, 24, 48 hr
Result: Inhibited LEC migration tubule formation.
In Vivo

VSPPLTLGQLLS (1 mM; intranasal dropping; onced daily for 7 d) blocks 9-cisRA-induced lymphangiogenesis in vivo, while 9-cisRA is an isoform of vitamin A involving in AIDS-related Kaposi Sarcoma[1].
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.

Animal Model: Lymphatic reporter mice, Prox1-GFP model[1]
Dosage: 1 mM
Administration: Intranasal dropping; once daily for 7 days; accompanied with 1 mM 9-cisRA or not
Result: Significantly inhibited total lymphatic vessel length and number of sprouts compared increase induced by 9-cisRA.
Animal Model: Fgfr3Neo-K644E/+EIIa-Cre mice (TDII mice) from Fgfr3Neo-K644E/+ mice crossed with heterozygous EIIa-Cre mice[2]
Dosage: 10 μM
Administration: Treated for 7 days
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.
Molecular Weight

1224.45

Formula

C56H97N13O17
CAS No.
Appearance

Solid

Color

White to off-white

Sequence Shortening

VSPPLTLGQLLS
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (40.83 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8167 mL 4.0835 mL 8.1669 mL
5 mM 0.1633 mL 0.8167 mL 1.6334 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). 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.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
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). 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.

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VSPPLTLGQLLS Related Classifications

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  • 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.

Keywords:

VSPPLTLGQLLS1206896-24-3FGFRFibroblast growth factor receptor9-cis retinoic acidlymphangiogenesislymphatic endothelial celllymphedemapeptide inhibitorInhibitorinhibitorinhibit

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