Disitertide (P144) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor and an apoptosis inducer[1][2][3][4][5].
体外研究 (In Vitro)
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[2]. 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[3]. 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[5].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[2]
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 (In Vivo)
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[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Human hypertrophic scars were implanted in 60 nude mice[4].
Dosage:
300 μg/mL was added the Lipogel.
Administration:
Topical application daily administered.
Result:
Successful shedding was achieved in 83,3% of the xenografts.
Clinical Trial
分子量
1580.82
Formula
C68H109N17O22S2
CAS 号
272105-42-7
Sequence Shortening
TSLDASIIWAMMQN
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-80°C
2 years
-20°C
1 year
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. Cindy Neuzillet, et al. Targeting the TGFβ pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.
[2]. Jun Yang, et al. Upregulation of microRNA‑590 in rheumatoid arthritis promotes apoptosis of bone cells through transforming growth factor‑β1/phosphoinositide 3‑kinase/Akt signaling. Int J Mol Med. 2019 May;43(5):2212-2220.
[3]. Wanming He, et al. MSC-regulated lncRNA MACC1-AS1 promotes stemness and chemoresistance through fatty acid oxidation in gastric cancer. Oncogene. 2019 Jun;38(23):4637-4654.
[4]. Shan Shan Qiu, et al. Effect of P144® (Anti-TGF-β) in an “In Vivo” Human Hypertrophic Scar Model in Nude Mice. PLoS One. 2015 Dec 31;10(12):e0144489.
[5]. Gabriel Gallo-Oller, et al. P144, a Transforming Growth Factor beta inhibitor peptide, generates antitumoral effects and modifies SMAD7 and SKI levels in human glioblastoma cell lines. Cancer Lett. 2016 Oct 10;381(1):67-75.
