VSPPLTLGQLLS TFA 是小肽FGFR3抑制剂，是一种肽P3，能够抑制FGFR3的磷酸化。VSPPLTLGQLLS TFA 抑制 9-cisRA 诱导的气管淋巴管生成，并阻止淋巴内皮细胞(LEC)增殖、迁移和小管形成。
| 生物活性 | VSPPLTLGQLLS TFA is a small peptideFGFR3inhibitor, peptide P3, inhibitsFGFR3phosphorylation. 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 |
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体外研究
(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].
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. |
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体内研究
(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].
| 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. |
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| Sequence Shortening | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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