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

VSPPLTLGQLLS TFA is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS TFA inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation.

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VSPPLTLGQLLS TFA Chemical Structure

VSPPLTLGQLLS TFA Chemical Structure

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VSPPLTLGQLLS TFA Related Antibodies

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Description

VSPPLTLGQLLS TFA is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS TFA 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 TFA (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 TFA 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 TFA (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 TFA (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 TFA (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 TFA 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 TFA (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 TFA 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

1338.47

Formula

C58H98F3N13O19
Sequence Shortening

VSPPLTLGQLLS
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Storage

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References
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VSPPLTLGQLLS TFA Related Classifications

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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.

Keywords:

VSPPLTLGQLLSFGFRFibroblast growth factor receptor9-cis retinoic acidlymphangiogenesislymphatic endothelial celllymphedemapeptide inhibitorInhibitorinhibitorinhibit

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