Disitertide diammonium  (Synonyms: P144 diammonium)

Disitertide (P144) diammonium is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide diammonium is also a PI3K inhibitor and an apoptosis inducer^{[1][2][3][4][5]}.

Disitertide (P144, 100 μg/mL) diammonium 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) diammonium 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 (10 μg/mL to 200 μg/mL) diammonium affects proliferation, induces apoptosis as well as anoikis in A172 and U-87 MG GBM cell lines^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Disitertide (P144, Topical application, 300 μg/mL) diammonium may promote scar maturation and improvement of hypertrophic scar morphology features in an "in vivo" model in nude mice after two weeks of treatment^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1614.88

C₆₈H₁₁₅N₁₉O₂₂S₂

Solid

White to off-white

TSLDASIIWAMMQN

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Cindy Neuzillet, et al. Targeting the TGFβ pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]