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

Physicochemical Properties

Molecular Formula	C68H115N19O22S2
Molecular Weight	1614.88
Related CAS #	Disitertide;272105-42-7;Disitertide TFA
Appearance	White to off-white 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

ln Vitro	In MC3T3-E1 cells, disitertide (P144, 100 μg/mL) diammonium induces the expression of Bax protein while suppressing the levels of p-Akt and PI3K protein expression[2]. It is possible to suppress MSC-induced stemness and chemoresistance by targeting the TGFβ signaling system, as evidenced by the fact that disitertide (a TGF-β1 inhibitor) diammonium abrogates the MACC1-AS1 expression in GC cells[3]. In A172 and U-87 MG GBM cell lines, disitertide (10 μg/mL to 200 μg/mL) diammonium influences proliferation, promotes apoptosis, and causes anoikis[5].
ln Vivo	After two weeks of treatment, doritertide (P144, topical application, 300 μg/mL) diammonium may ameliorate hypertrophic scar morphological aspects and encourage scar maturation in a nude mouse "in vivo" model[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)	DMSO :~10 mg/mL (~6.19 mM) H2O :~9.09 mg/mL (~5.63 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 5 mg/mL (3.10 mM) in 50% PEG300 +50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.6192 mL	3.0962 mL	6.1924 mL
	5 mM	0.1238 mL	0.6192 mL	1.2385 mL
	10 mM	0.0619 mL	0.3096 mL	0.6192 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.