T7 Peptide TFA
Based on 1 Customer Validation
T7 Peptide TFA is a protein synthesis inhibitor and anti-angiogenic agent, with a Kd of 10 nM for human transferrin receptor. T7 Peptide TFA inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide TFA induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide TFA is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.20%
- Fòrmula: C137H189N33O39S3.xC2HF3O2
- Peso molecular:3018.36 (free base)
-
Almacenamiento:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Descripciòn
In Vitro
T7 peptide TFA (4.5 μM; 21 h) specifically inhibits cap-dependent translation in C-PAE cells without affecting cap-independent translation[1].
T7 peptide (4.5 μM) inhibits total protein synthesis in MLEC-wt cells[1].
T7 peptide TFA (4.5 μM) does not inhibit total protein synthesis in MLEC-β3 null cells, indicating dependence on αVβ3 integrin for this activity[1].
T7 peptide TFA (4.5 μM) does not inhibit total protein synthesis in MEF-wt cells, indicating αVβ3 integrin expression is essential but not sufficient for this activity[1].
T7 peptide TFA (4.5 μM) does not inhibit total protein synthesis in non-endothelial cell lines, demonstrating endothelial cell specificity for this activity[1].
The T7 peptide TFA (0.25-2 μM; 6-24 h) significantly reduces viability of Huh-7 and Hep3B human HCC cells in a concentration- and time-dependent manner, but has minimal effect on normal human liver L-02 cells[3].
The T7 peptide TFA (0.25-1 μM; 24 h) induces significant apoptosis (both early and late) in Huh-7 and Hep3B human HCC cells[3].
The T7 peptide TFA (0.25-1 μM; 24 h) induces G0/G1 cell cycle arrest in Huh-7 and Hep3B human HCC cells[3].
The T7 peptide TFA (0.5-1 μM; 24 h) upregulates pro-apoptotic Bax, Fas, and FasL and downregulates anti-apoptotic Bcl-2 in a concentration-dependent manner in Huh-7 and Hep3B human HCC cells[3].
The T7 peptide TFA (0.5-1 μM; 24 h) induces autophagy in Huh-7 and Hep3B human HCC cells by upregulating Beclin-1, Atg5, and LC3-II in a concentration-dependent manner[3].
The T7 peptide TFA (1 μM; 24 h) has enhanced apoptotic effect in Huh-7 and Hep3B human HCC cells when autophagy is inhibited[3].
The T7 peptide TFA (0.5-1 μM; 24 h) induces autophagy in Huh-7 and Hep3B human HCC cells via inhibition of the Akt/mTOR signaling pathway, and co-treatment with Akt/mTOR inhibitors enhances this autophagic response[3].
T7 peptide (5 μM; 2 h at 37 °C) modified LDL shows enhanced cellular uptake in bEnd.3 and C6 cells via synergistic mediation by TfR and LDLR[4].
T7 peptide TFA (0.5-6% molar ratio; 4 h at 37 °C) modification enhances BBB penetration and subsequent C6 glioma cell uptake, with optimal efficacy observed at a 4% molar ratio of T7 to LDL[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:human hepatocellular carcinoma (HCC) Huh-7, Hep3B cells; normal human liver L-02 cells
-
Concentration:0.25-2 μM (24 h); 1 μM (6, 12, 24 h)
-
Incubation Time:24 h (0.25, 0.5, 1, 2 μM); 6 h, 12 h, 24 h (1 μM)
-
Result:Significantly decreased viability of Huh-7 and Hep3B cells in a concentration- and time-dependent manner.
Had little effect on viability of L-02 cells.
-
Cell Line:human HCC Huh-7, Hep3B cells
-
Concentration:0.25-1 μM
-
Incubation Time:24 h
-
Result:Significantly enhanced apoptotic cell death, with increases in both early and late apoptosis in Huh-7 and Hep3B cells.
-
Cell Line:human HCC Huh-7, Hep3B cells
-
Concentration:0.25-2 μM (24 h);
-
Incubation Time:24 h
-
Result:Arrested cells in the G0/G1 phase, with corresponding decreases in S phase and G2/M phase populations.
-
Cell Line:human HCC Huh-7, Hep3B cells
-
Concentration:0.5-1 μM
-
Incubation Time:24 h
-
Result:Upregulated expression of Bax, Fas, and FasL, and downregulated expression of Bcl-2 in a concentration-dependent manner.
In Vivo
T7 peptide TFA (4% molar ratio; 0.5 mg/kg; intravenous tail vein injection) conjugation to LDL particles enhances accumulation in intracranial glioma tissue in female ICR mice bearing C6 glioma[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c athymic nude (male, 5-6 weeks old, 18-22 g, Hep3B human HCC cells xenograft)[3]
-
Dosage:2.5 mg/kg; 5 mg/kg
-
Administration:i.p.; every other day;30 days
-
Result:Suppressed Hep3B xenograft tumor growth with tumor growth at day 35.
Increased tumor tissue apoptotic.
Upregulated Bax protein expression at both doses.
Downregulated Bcl-2 protein expression at both doses.
Reduced phosphorylated Akt (Ser473) and phosphorylated mTOR (Ser2448) levels at both doses, with no significant change in total Akt or mTOR protein levels.
Caused no obvious mouse weight loss with either dose.
Chemical Information
-
Appearance Solid
-
Peso molecular 3018.36 (free base)
-
Fòrmula C137H189N33O39S3.xC2HF3O2
-
Color White to off-white
-
Synonyms
Tumstatin (74-98), human TFA
-
Sequence
Thr-Met-Pro-Phe-Leu-Phe-Cys-Asn-Val-Asn-Asp-Val-Cys-Asn-Phe-Ala-Ser-Arg-Asn-Asp-Tyr-Ser-Tyr-Trp-Leu (Disulfide bridge: Cys7-Cys13)
-
Sequence Shortening
TMPFLFCNVNDVCNFASRNDYSYWL (Disulfide bridge: Cys7-Cys13)
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (292 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Maeshima Y, et al. Tumstatin, an endothelial cell-specific inhibitor of protein synthesis. Science. 2002 Jan 4;295(5552):140-3. [Content Brief]
[2]. Liang M, et al. Enhanced blood-brain barrier penetration and glioma therapy mediated by T7 peptide-modified low-density lipoprotein particles. Drug Deliv. 2018;25(1):1652-1663. [Content Brief]
[3]. Liu F, et al. T7 peptide cytotoxicity in human hepatocellular carcinoma cells is mediated by suppression of autophagy. Int J Mol Med. 2019;44(2):523-534. [Content Brief]
[4]. Kim G, et al. Systemic delivery of microRNA-21 antisense oligonucleotides to the brain using T7-peptide decorated exosomes. J Control Release. 2020;317:273-281. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
T7 Peptide TFA Related Classifications
HY-P10323A Related Classifications
Powered by Bioz