1. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Apoptosis NF-κB Reactive Oxygen Species (ROS)
  3. CIGB-552

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

CIGB-552

CIGB-552 Chemical Structure

CAS No. : 1630763-23-3

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2][3][4].

In Vitro

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.

Cell Viability Assay[1]

Cell Line: H460, H-125, H-82, LS174T, MDA-231 and PBMC cells
Concentration: 0-200 μM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: H460, MCF7, and HT29 cells
Concentration: 20-60 μM, MG132 (HY-13259) as a control group
Incubation Time: 5 h
Result: Increased the protein level of COMMD1 in three types of cancer cells.

Western Blot Analysis[1]

Cell Line: H460 cells
Concentration: 25 μM
Incubation Time: 24 h
Result: Increased the level of protein Bax, decreased the amount of protein Bcl-2, and activated Caspase-3 and PARP cleavage.

Apoptosis Analysis[1]

Cell Line: H460 cells
Concentration: 25 μM
Incubation Time: 24, 48 h
Result: Significantly increased the apoptosis rate of cells compared to the control group.
Parmacokinetics
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
In Vivo

CIGB-552 (1 mg/kg; s.c.; three times a week; for three weeks) significantly inhibits tumor growth in the lung cancer miceand prolongs survival without causing significant toxicity[2].
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.

Animal Model: 5×10<4/sup> TC-1 cells injected the C57/BL6 female mice (8 weeks, 18-20g)[2]
Dosage: 1 mg/kg, combination with 0.4 mg/kg Cisplatin (HY-17394)
Administration: Subcutaneous injection (s.c.); three times a week for three weeks
Result: Significantly reduced tumor volume of the cancer mice.
Improved the survival rate of the cancer mice.
Animal Model: 7×104 CT-26 cells injected the BALB/c mice[4]
Dosage: 0.2 or 0.7 mg/kg
Administration: Subcutaneous injection (s.c.); two times a week for two weeks
Result: Inhibited the tumor volume of tumor mice and caused apoptosis of cells at the tumor site.
Animal Model: 1×107 HT-29 cells injected the female athymic nu/nu(nude) mice[4]
Dosage: 0.7 or 1.4 mg/kg
Administration: Subcutaneous injection (s.c.); two times a week for two weeks
Result: Inhibited the tumor volume of tumor mice and reduced tumor microvascular density.
Molecular Weight

2689.21

Formula

C131H198N38O24

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Ac-His-Ala-Arg-Ile-Lys-{d-Pro}-Thr-Phe-Arg-Arg-{d-Leu}-Lys-Trp-Lys-Tyr-Lys-Gly-Lys-Phe-Trp

Sequence Shortening

Ac-HARIK-{d-Pro}-TFRR-{d-Leu}-KWKYKGKFW

Shipping

Room temperature in continental US; may vary elsewhere.

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)

Solvent & Solubility
In Vitro: 

H2O : 17.3 mg/mL (6.43 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.3719 mL 1.8593 mL 3.7186 mL
5 mM 0.0744 mL 0.3719 mL 0.7437 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CIGB-552
Cat. No.:
HY-P11115
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