CIGB-552 TFA
Based on 1 Customer Validation
CIGB-552 TFA is a cell-penetrating peptide with anti-tumor properties with the IC50 of 23 μM in H460 cells. CIGB-552 TFA can increase the level of protein COMMD1. CIGB-552 TFA significantly inhibits the NF-κB signaling pathway. CIGB-552 TFA can promote apoptosis of the tumor cells. CIGB-552 TFA can induce the accumulation of reactive oxygen species (ROS) in tumor cells. CIGB-552 TFA has anti-inflammatory and anti-angiogenic effects. CIGB-552 TFA can be used for the research of the lung cancer and colon cancer.
For research use only. We do not sell to patients.
- Formula: C131H198N38O24·xC2HF3O2
- Molecular Weight:2689.21 (free base)
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Storage:
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)
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
CIGB-552 TFA (20-60 μM, 5 h) can increase the protein content of the anti-tumor related protein COMMD1[1].
CIGB-552 TFA (25 μM, 0-12 h) promotes the ubiquitination degradation of RelA and inhibits NF-κB signaling in H460 cells[1].
CIGB-552 TFA (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 TFA (25 μM, 24-48 h) can induce apoptosis in lung cancer cells[1].
CIGB-552 TFA (25 μM, 8 h) reduces cellular antioxidant capacity, leading to protein and lipid oxidative damage in H460 cells [1].
CIGB-552 TFA (37.5 μM, 1 h) induces the accumulation of reactive oxygen species (ROS) by inhibiting SOD1 activity, selectively killing tumor cells[2].
CIGB-552 TFA (75-150 μM, 24 h) can significantly inhibit TNF-α-induced NF-κB activation[3].
CIGB-552 TFA (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 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, 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:20-60 μM, MG132 (HY-13259) as a control group
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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, 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 TFA (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:5×104 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.
Chemical Information
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Appearance Solid
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Molecular Weight 2689.21 (free base)
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Formula C131H198N38O24·xC2HF3O2
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Sequence
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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Sequence Shortening
Ac-HARIK-{d-Pro}-TFRR-{d-Leu}-KWKYKGKFW
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Purity & Documentation
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Data Sheet (283 KB)
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SDS (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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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