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编 号:F743124
分子式:C56H97N13O17
分子量:1224.45
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1mg
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5mg
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10mg
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生物活性:
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.

体内研究:
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.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.Animal Model:Lymphatic reporter mice, Prox1-GFP model
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
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.

体外研究:
VSPPLTLGQLLS (5 μM and 10 μM; 24 h and 48 h) inhibits human primary lymphatic endothelial cell (LEC)s proliferation, migration, and tubule formation.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.VSPPLTLGQLLS (10 μM; 6 h) inhibits tyrosine kinase activity of FGFR3 and its typical downstream molecules, extracellular signal-regulated kinase/mitogen-activated protein kinase.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.VSPPLTLGQLLS (10 μM; 0-60 min) inhibits the ERK/MAPK pathway in FGFR3-expressing chondrocytic cell lineATDC5.
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