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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.20%
- 分子式: C137H189N33O39S3.xC2HF3O2
- 分子量:3018.36 (free base)
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保管条件:
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)
生物活性
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.
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Cell Line:human hepatocellular carcinoma (HCC) Huh-7, Hep3B cells; normal human liver L-02 cells
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Concentration:0.25-2 μM (24 h); 1 μM (6, 12, 24 h)
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Incubation Time:24 h (0.25, 0.5, 1, 2 μM); 6 h, 12 h, 24 h (1 μM)
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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.
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Cell Line:human HCC Huh-7, Hep3B cells
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Concentration:0.25-1 μM
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Incubation Time:24 h
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Result:Significantly enhanced apoptotic cell death, with increases in both early and late apoptosis in Huh-7 and Hep3B cells.
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Cell Line:human HCC Huh-7, Hep3B cells
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Concentration:0.25-2 μM (24 h);
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Incubation Time:24 h
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Result:Arrested cells in the G0/G1 phase, with corresponding decreases in S phase and G2/M phase populations.
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Cell Line:human HCC Huh-7, Hep3B cells
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Concentration:0.5-1 μM
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Incubation Time:24 h
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Result:Upregulated expression of Bax, Fas, and FasL, and downregulated expression of Bcl-2 in a concentration-dependent manner.
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.
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Animal Model:BALB/c athymic nude (male, 5-6 weeks old, 18-22 g, Hep3B human HCC cells xenograft)[3]
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Dosage:2.5 mg/kg; 5 mg/kg
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Administration:i.p.; every other day;30 days
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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.
化学情報
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性状 Solid
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分子量 3018.36 (free base)
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分子式 C137H189N33O39S3.xC2HF3O2
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Color White to off-white
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別名
Tumstatin (74-98), human TFA
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配列
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)
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シーケンスの短縮
TMPFLFCNVNDVCNFASRNDYSYWL (Disulfide bridge: Cys7-Cys13)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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)
純度とドキュメンテーション
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データシート (291 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)