Disitertide (P144) TFA is a bioactive peptide inhibitor of transforming growth factor TGFβ1, which specifically blocks its interaction with the receptor. Disitertide TFA is also an inhibitor (blocker/antagonist) of PI3K and an inducer of apoptosis.

Physicochemical Properties

Molecular Formula	C70H110N17O24S2F3
Molecular Weight	1694.84
Related CAS #	Disitertide diammonium;Disitertide;272105-42-7
Appearance	Off-white to light yellow solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	TGF-β1, P13K[1][2].
ln Vitro	In MC3T3-E1 cells, disitertide (P144, 100 μg/mL) TFA increases the production of Bax protein while suppressing PI3K and p-Akt [2]. TFA, an inhibitor of TGFβ1, suppresses the expression of MACC1-AS1 in GC cells, suggesting that a possible tactic to prevent MSC-induced stemness and chemotherapy resistance would be to target the TGFβ signaling pathway [3]. Disitertide (10 μg/mL to 200 μg/mL) TFA influences the growth, triggers apoptosis, and causes anoikis in GBM cell lines A172 and U-87 MG [5].
ln Vivo	After two weeks of therapy in a nude mouse "in vivo" model, dissolvertide (P144, Topical administration, 300 μg/mL) TFA improves the morphological aspects of hypertrophic scars and accelerates scar maturation [4].
Cell Assay	Western Blot Analysis[2] Cell Types: Mouse embryo osteoblast precursor MC3T3-E1 cells. Tested Concentrations: 100 μg/mL. Incubation Duration: 4 h. Experimental Results: Dramatically 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.
Animal Protocol	Animal/Disease Models: Human hypertrophic scars were implanted in 60 nude mice[4]. Doses: 300 μg/mL was added the Lipogel. Route of Administration: Topical application daily administered. Experimental Results: Successful shedding was achieved in 83,3% of the xenografts.
References	[1]. Targeting the TGFβ pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31. [2]. 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]. MSC-regulated lncRNA MACC1-AS1 promotes stemness and chemoresistance through fatty acid oxidation in gastric cancer. Oncogene. 2019 Jun;38(23):4637-4654. [4]. 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]. 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.

Solubility Data

Solubility (In Vitro)

H2O :< 0.1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (1.48 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (1.48 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (1.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.5900 mL	2.9501 mL	5.9003 mL
	5 mM	0.1180 mL	0.5900 mL	1.1801 mL
	10 mM	0.0590 mL	0.2950 mL	0.5900 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.