CIGB-552
Based on 1 Customer Validation
CIGB-552 is a cell-penetrating peptide with anti-tumor properties with the IC50 of 23 μM in H460 cells. CIGB-552 can increase the level of protein COMMD1. CIGB-552 significantly inhibits the NF-κB signaling pathway. CIGB-552 can promote apoptosis of the tumor cells. CIGB-552 can induce the accumulation of reactive oxygen species (ROS) in tumor cells. CIGB-552 has anti-inflammatory and anti-angiogenic effects. CIGB-552 can be used for the research of the lung cancer and colon cancer.
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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: 98.66%
- CAS 番号: 1630763-23-3
- 分子式: C131H198N38O24
- 分子量:2689.21
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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
CIGB-552 (20-60 μM, 5 h) can increase the protein content of the anti-tumor related protein COMMD1[1].
CIGB-552 (25 μM, 0-12 h) promotes the ubiquitination degradation of RelA and inhibits NF-κB signaling in H460 cells[1].
CIGB-552 (25 μM, 0-24 h) can increase the level of pro apoptotic proteins and reduce the level of anti apoptotic proteins in H460 cells[1].
CIGB-552 (25 μM, 24-48 h) can induce apoptosis in lung cancer cells[1].
CIGB-552 (25 μM, 8 h) reduces cellular antioxidant capacity, leading to protein and lipid oxidative damage in H460 cells [1].
CIGB-552 (37.5 μM, 1 h) induces the accumulation of reactive oxygen species (ROS) by inhibiting SOD1 activity, selectively killing tumor cells[2].
CIGB-552 (75-150 μM, 24 h) can significantly inhibit TNF-α-induced NF-κB activation[3].
CIGB-552 (2.5-25 μM, 24 h) exerts anti angiogenic effects by inhibiting hypoxia induced HIF-1 activation through COMMD1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H460, H-125, H-82, LS174T, MDA-231 and PBMC cells
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Concentration:0-200 μM
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Incubation Time:48 h
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Result:Had better cytotoxicity against H460 (IC50 = 23 μM, H-125 (IC50 = 42 μM), H-82 (IC50 = 15 μM), LS174T (IC50 = 22 μM), MDA-231 (IC50 = 40 μM) and PBMC (IC50 = 249 μM) cells compared to the control group.
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Cell Line:H460, MCF7, and HT29 cells
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Concentration:20-60 μM, MG132 (HY-13259) as a control group
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Incubation Time:5 h
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Result:Increased the protein level of COMMD1 in three types of cancer cells.
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Cell Line:H460 cells
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Concentration:25 μM
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Incubation Time:24 h
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Result:Increased the level of protein Bax, decreased the amount of protein Bcl-2, and activated Caspase-3 and PARP cleavage.
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Cell Line:H460 cells
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Concentration:25 μM
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Incubation Time:24, 48 h
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Result:Significantly increased the apoptosis rate of cells compared to the control group.
| Species | Dose | Route | Tmax | AUC0-∞ | Vd/F | MRT | T1/2 | Cmax |
|---|---|---|---|---|---|---|---|---|
| Mice[4] | 5 ug | s.c. | 0.33 h | 161.30 ng·h/mL | 362.29 mL | 7 h | 8.10 h | 82.2 ng/mL |
CIGB-552 (0.2-1.4 mg/kg; s.c.; two times a week; for two weeks) significantly inhibits tumor growth in mice with colon cancer and has anti angiogenic effects[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5×10<4/sup> TC-1 cells injected the C57/BL6 female mice (8 weeks, 18-20g)[2]
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Dosage:1 mg/kg, combination with 0.4 mg/kg Cisplatin (HY-17394)
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Administration:Subcutaneous injection (s.c.); three times a week for three weeks
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Result:Significantly reduced tumor volume of the cancer mice.
Improved the survival rate of the cancer mice.
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Animal Model:7×104 CT-26 cells injected the BALB/c mice[4]
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Dosage:0.2 or 0.7 mg/kg
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Administration:Subcutaneous injection (s.c.); two times a week for two weeks
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Result:Inhibited the tumor volume of tumor mice and caused apoptosis of cells at the tumor site.
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Animal Model:1×107 HT-29 cells injected the female athymic nu/nu(nude) mice[4]
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Dosage:0.7 or 1.4 mg/kg
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Administration:Subcutaneous injection (s.c.); two times a week for two weeks
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Result:Inhibited the tumor volume of tumor mice and reduced tumor microvascular density.
化学情報
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CAS 番号 1630763-23-3
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性状 Solid
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分子量 2689.21
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分子式 C131H198N38O24
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Color White to off-white
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配列
Ac-His-Ala-Arg-Ile-Lys-{d-Pro}-Thr-Phe-Arg-Arg-{d-Leu}-Lys-Trp-Lys-Tyr-Lys-Gly-Lys-Phe-Trp
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シーケンスの短縮
Ac-HARIK-{d-Pro}-TFRR-{d-Leu}-KWKYKGKFW
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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)
溶剤 & 溶解度
H2O : 17.3 mg/mL (6.43 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (284 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Fernández Massó JR, et al. The Antitumor Peptide CIGB-552 Increases COMMD1 and Inhibits Growth of Human Lung Cancer Cells. J Amino Acids. 2013;2013:251398. [Content Brief]
[2]. Gomez Rodriguez Y, et al. Synergic effect of anticancer peptide CIGB-552 and Cisplatin in lung cancer models. Mol Biol Rep. 2022 Apr;49(4):3197-3212. [Content Brief]
[3]. Daghero H, et al. The Anticancer Peptide CIGB-552 Exerts Anti-Inflammatory and Anti-Angiogenic Effects through COMMD1. Molecules. 2020 Dec 31;26(1):152. [Content Brief]
[4]. Vallespí MG, et al. Antitumor efficacy, pharmacokinetic and biodistribution studies of the anticancer peptide CIGB-552 in mouse models. J Pept Sci. 2014 Nov;20(11):850-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.3719 mL | 1.8593 mL | 3.7186 mL | 9.2964 mL |
| 5 mM | 0.0744 mL | 0.3719 mL | 0.7437 mL | 1.8593 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.