Disitertide (P144) 是转化生长因子TGFβ1的多肽抑制剂，特异性的阻断其与受体间的相互作用。Disitertide (P144) 也是PI3K的抑制剂和凋亡 (apoptosis) 诱导剂。
| 生物活性 | Disitertide (P144) is a peptidictransforming growth factor-beta 1 (TGF-β1)inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also aPI3Kinhibitor and anapoptosisinducer[1][2][3][4][5].
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体外研究
(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].
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 |
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体内研究
(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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -80°C | 2 years | | -20°C | 1 year | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 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. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (1.58 mM); Clear solution 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (1.58 mM); Suspended solution; Need ultrasonic 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (1.58 mM); Clear solution
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