ChemicalBook Product Catalog Biochemical Engineering Inhibitors Disitertide

Disitertide

Product NameDisitertide
CAS272105-42-7
MFC68H109N17O22S2
MW1580.84
EINECS
MOL File272105-42-7.mol

Chemical Properties

Boiling point	1968.7±65.0 °C(Predicted)
Density	1.327
storage temp.	Store at -20°C
solubility	DMSO : ≥ 200 mg/mL (126.52 mM);Water : < 0.1 mg/mL (insoluble)
pka	3.15±0.10(Predicted)
form	Solid
color	White to off-white
InChIKey	IUYPEUHIWDMJLM-INGCBPSVNA-N

Usage And Synthesis

Description

Disitertide is an inhibitor of TGF-β1. It prevents TGF-β1-dependent inhibition of MV1Lu proliferation in vitro and markedly reduces binding of TGF-β1 to its receptors. Disitertide blocks TGF-β1-dependent stimulation of a reporter gene under the control of human α2(I) collagen promoter. Treatment with Disitertide at low doses causes a significant inhibition of HSC activation and a marked reduction in liver fibrosis in a rat model of chronic exposure to CCl4. A dose as low as 70 μg of the 15-mer peptide Disitertide, given to rats (300 g body weight) on alternate days, decreases fibrogenesis significantly during chronic exposure to CCl4.

Biological Activity

Disitertide (P144) TFA is a polypeptide inhibitor of transforming growth factor TGFβ1, specifically blocking its interaction with the receptor. Disitertide (P144) is also an inhibitor of PI3K and an inducer of apoptosis.

in vitro

Disitertide (100 μg/mL) suppresses the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells.
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.
Disitertide (P144, 10 μg/mL to 200 μg/mL) affects proliferation,

Western Blot Analysis

Cell Line:	Mouse embryo osteoblast precursor MC3T3-E1 cells.
Concentration:
Concentration:	100 μg/mL.
Incubation Time:	4 h.
Result:	Significantly suppressed the protein expression levels of PI3K and p-Akt, and induced 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 clinical improvement of hypertrophic scar morphology features in an “in vivo” model in nude mice after two weeks of treatment.

Animal Model:	Human hypertrophic scars were implanted in 60 nude mice.
Dosage:	300 μg/mL was added the Lipogel.
Administration:	Topical application daily administered.
Result:	Successful shedding was achieved in 83,3% of the xenografts.

storage

Store at -20°C

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