CIGB-552

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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].

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

CIGB-552 Chemical Structure

CAS No. : 1630763-23-3

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Biological Activity
Purity & Documentation
References
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Description

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^[4]

Species	Dose	Route	Indicator	value
Mice	5 ug	s.c.	T_max	0.33 h
Mice	5 ug	s.c.	AUC_0-∞	161.30 ng·h/mL
Mice	5 ug	s.c.	V_d/F	362.29 mL
Mice	5 ug	s.c.	MRT	7 h
Mice	5 ug	s.c.	T_1/2	8.10 h
Mice	5 ug	s.c.	C_max	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:	5×104 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.

1630763-23-3

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

SMILES

OC(C=C1)=CC=C1C[C@@H](C(N[C@@H](CCCCN)C(NCC(N[C@@H](CCCCN)C(N[C@H](C(N[C@H](C(O)=O)CC2=CNC3=CC=CC=C23)=O)CC4=CC=CC=C4)=O)=O)=O)=O)NC([C@H](CCCCN)NC([C@@H](NC([C@H](CCCCN)NC([C@@H](CC(C)C)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@@H](NC([C@H]([C@H](O)C)NC([C@@H]5N(CCC5)C([C@H](CCCCN)NC([C@H]([C@@H](C)CC)NC([C@H](CCCNC(N)=N)NC([C@H](C)NC([C@@H](NC(C)=O)CC6=CN=CN6)=O)=O)=O)=O)=O)=O)=O)CC7=CC=CC=C7)=O)=O)=O)=O)=O)CC8=CNC9=CC=CC=C89)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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]

CIGB-552 Related Classifications

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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.

Keywords:

CIGB-5521630763-23-3CIGB552CIGB 552ApoptosisNF-κBReactive Oxygen Species (ROS)Nuclear factor-κBNuclear factor-kappaBantitumorCOMMD1NFκBHIFlung cancercolon cancerinflammationInhibitorinhibitorinhibit

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