Disitertide (Synonyms: P144)

Cat. No.: HY-P0118: FAQs
Data Sheet SDS Handling Instructions

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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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Disitertide diammonium) that retains the same biological activity.

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

Disitertide Chemical Structure

CAS No. : 272105-42-7

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Other Forms of Disitertide:

Disitertide TFA Get quote
Disitertide diammonium Get quote

13 Publications Citing Use of MCE Disitertide

: Disitertide 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
Customer Review

Description

In Vitro

Disitertide (P144, 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 (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].

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 (Topical application, 300 μg/mL) 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

Formula

C₆₈H₁₀₉N₁₇O₂₂S₂

CAS No.

272105-42-7

Appearance

Solid

Color

White to off-white

Sequence Shortening

TSLDASIIWAMMQN

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light, under nitrogen

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, under nitrogen)

Solvent & Solubility

In Vitro:

H₂O

Peptide Solubility and Storage Guidelines:

1. Calculate the length of the peptide.

2. Calculate the overall charge of the entire peptide according to the following table:

	Contents	Assign value
Acidic amino acid	Asp (D), Glu (E), and the C-terminal -COOH.	-1
Basic amino acid	Arg (R), Lys (K), His (H), and the N-terminal -NH₂	+1
Neutral amino acid	Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)	0

3. Recommended solution:

Overall charge of peptide	Details
Negative (<0)	1. Try to dissolve the peptide in water first. 2. If water fails, add NH₄OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0)	1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)	1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.58 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (1.58 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (1.58 mM); Clear solution

Purity & Documentation

Data Sheet (265 KB) SDS (103 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 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

Disitertide272105-42-7P144P 144P-144TGF-beta/SmadPI3KApoptosisTransforming growth factor betaPhosphoinositide 3-kinasetransforming growth factorpolypeptideGC cellsInhibitorinhibitorinhibit

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