Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer.
IC50&Target
TGF-β1, P13K.
体外研究
Disitertide (100 μg/mL) suppresses the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells. Disitertide (TGF-β1 inhibitor) abrogates the MACC1- AS1 expression in GC cells, suggesting that targeting TGFβ signaling pathway may be a potential strategy to inhibit MSC-induced stemness and chemoresistance.
Disitertide (P144, 10 μg/mL to 200 μg/mL) affects proliferation, induces apoptosis as well as anoikis in A172 and U-87 MG GBM cell lines.
Western Blot Analysis
Cell Line:
Mouse embryo osteoblast precursor MC3T3-E1 cells.
Concentration:
100 μg/mL.
Incubation Time:
4 h.
Result:
Significantly suppressed the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells compared with the miR-590 group.
体内研究
Disitertide (Topical application, 300 μg/mL) may promote scar maturation and clinical improvement of hypertrophic scar morphology features in an “in vivo” model in nude mice after two weeks of treatment.
Animal Model:
Human hypertrophic scars were implanted in 60 nude mice.
Dosage:
300 μg/mL was added the Lipogel.
Administration:
Topical application daily administered.
Result:
Successful shedding was achieved in 83,3% of the xenografts.
运输条件
Room temperature in continental US; may vary elsewhere.