Disitertide TFA (Synonyms: P144 TFA)

Cat. No.: HY-P0118A: FAQs
Data Sheet SDS Handling Instructions

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Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide TFA is also a PI3K inhibitor and an apoptosis inducer.

For research use only. We do not sell to patients.

Disitertide TFA Chemical Structure

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Other In-stock Forms of Disitertide TFA:

Disitertide

Other Forms of Disitertide TFA:

Disitertide In-stock
Disitertide diammonium Get quote

13 Publications Citing Use of MCE Disitertide TFA

: Disitertide TFA purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Jan;28(1):219-232. [Abstract]; LINC00941-overexpressing cells treated with Disitertide (10 μM) shows increased mRNA and protein levels of ZO-1 and Ecadherin compared with controls. LINC00941-silenced cells show decreased mRNA and protein levels of ZO-1 and E-cadherin but increased mRNA and protein levels of Vimentin, Fibronectin, and Twist1.

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

TGF-β1, P13K^[1]^[2].

In Vitro

Disitertide (P144, 100 μg/mL) TFA 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) TFA 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) TFA 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.

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.

In Vivo

Disitertide (P144, Topical application, 300 μg/mL) TFA 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.

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

Molecular Weight

1580.82 (free acid)

Formula

C₆₈H₁₀₉N₁₇O₂₂S₂.xC₂HF₃O₂

Appearance

Solid

Color

Off-white to light yellow

Sequence

Thr-Ser-Leu-Asp-Ala-Ser-Ile-Ile-Trp-Ala-Met-Met-Gln-Asn

Sequence Shortening

TSLDASIIWAMMQN

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

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

Solvent & Solubility

In Vitro:

H₂O : < 0.1 mg/mL (insoluble)

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL; Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL; Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Data Sheet (276 KB) SDS (252 KB) Handling Instructions (2659 KB)

References

[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]

Disitertide TFA Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DisitertideP144P 144P-144TGF-beta/SmadPI3KApoptosisTransforming growth factor betaPhosphoinositide 3-kinasetransforming growth factorpolypeptideGC cellsInhibitorinhibitorinhibit

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