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

CIGB-552 是一种具有抗肿瘤特性的细胞穿透肽,在 H460 细胞中的 IC50 为 23 μM。CIGB-552 可以增加 COMMD1 蛋白的水平。CIGB-552 显著抑制 NF-κB 信号通路。CIGB-552 可以促进肿瘤细胞的凋亡 (apoptosis)。CIGB-552 可以诱导肿瘤细胞中活性氧 (ROS) 的积累。CIGB-552 具有抗炎和抗血管生成作用。CIGB-552 可用于肺癌和结肠癌的研究。

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Custom Peptide Synthesis

CIGB-552

CIGB-552 Chemical Structure

CAS No. : 1630763-23-3

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查看 NF-κB 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

CIGB-552 (20-60 μM,5 小时) 可以增加抗肿瘤相关蛋白 COMMD1 的蛋白质含量[1]

CIGB-552 (25 μM,0-12 小时) 促进 RelA 的泛素化降解并抑制 H460 细胞中 NF-κB 信号传导[1]

CIGB-552 (25 μM,0-24 小时) 可提高 H460 细胞中促凋亡蛋白的水平,降低抗凋亡蛋白的含量[1]

CIGB-552 (25 μM,24-48 小时) 可诱导肺癌细胞凋亡[1]

CIGB-552 (25 μM,8 小时) 会降低 H460 细胞抗氧化能力,导致蛋白质和脂质氧化损伤[1]

CIGB-552 (37.5 μM,1 小时) 通过抑制 SOD1 活性诱导活性氧 (ROS) 的积累,选择性杀死肿瘤细胞[2]

CIGB-552 (75-150 μM,24 小时) 可以显著抑制 TNF-α 诱导的 NF-κB 活化[3]

CIGB-552 (2.5-25 μM,24 小时) 通过 COMMD1 抑制缺氧诱导的 HIF-1 激活,从而发挥抗血管生成作用[3]

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
药代动力学
(Parmacokinetics)[4]
Species Dose Route Indicator value
Mice 5 ug s.c. Tmax 0.33 h
Mice 5 ug s.c. AUC0-∞ 161.30 ng·h/mL
Mice 5 ug s.c. Vd/F 362.29 mL
Mice 5 ug s.c. MRT 7 h
Mice 5 ug s.c. T1/2 8.10 h
Mice 5 ug s.c. Cmax 82.2 ng/mL
体内研究
(In Vivo)

CIGB-552 (1 mg/kg;皮下注射;每周三次;持续三周) 显著抑制肺癌小鼠的肿瘤生长,延长存活时间,但不会造成显著毒性[2]
CIGB-552 (0.2-1.4 mg/kg;皮下注射;每周两次;持续两周) 显著抑制结肠癌小鼠的肿瘤生长,并具有抗血管生成作用[4]

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.
分子量

2689.21

Formula

C131H198N38O24

CAS 号
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

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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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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CIGB-552
目录号:
HY-P11115
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