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VSPPLTLGQLLS
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VSPPLTLGQLLS图片
CAS NO:1206896-24-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
VSPPLTLGQLLS 是小肽FGFR3抑制剂,是一种肽P3,能够抑制FGFR3的磷酸化。VSPPLTLGQLLS 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 is a small peptideFGFR3inhibitor, peptide P3, inhibitsFGFR3phosphorylation. 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

 

体外研究
(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].

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.
体内研究
(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].

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.
分子量

1224.45

Formula

C56H97N13O17

CAS 号

1206896-24-3

Sequence Shortening

VSPPLTLGQLLS

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.