1. GPCR/G Protein Immunology/Inflammation Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  2. CXCR Apoptosis Caspase Akt ERK
  3. Peptide E5

Peptide E5 是一种靶向 CXCR4/CXCL12 轴的拮抗剂。Peptide E5 可阻断 CXCR4/CXCL12 轴,下调 CXCR4 的表达,并抑制下游 AktErk 的磷酸化。Peptide E5 可诱导乳腺癌细胞凋亡 (apoptosis),抑制迁移和黏附。Peptide E5 可抑制 CXCL12 介导的内皮祖细胞募集,从而抑制肿瘤血管生成。Peptide E5 可用于乳腺癌的相关研究。

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Custom Peptide Synthesis

Peptide E5

Peptide E5 Chemical Structure

CAS No. : 1643580-44-2

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Peptide E5 is an antagonist targeting the CXCR4/CXCL12 axis. Peptide E5 blocks the CXCR4/CXCL12 axis, downregulates CXCR4 expression, and inhibits the phosphorylation of downstream Akt and Erk. Peptide E5 induces apoptosis, suppresses migration and adhesion of breast cancer cells. Peptide E5 inhibits CXCL12-mediated endothelial progenitor cell recruitment, thereby suppressing tumor angiogenesis. Peptide E5 is applicable to relevant research on breast cancer[1].

体外研究
(In Vitro)

Peptide E5 (0.1 μM; 40 min) 对高表达 CXCR4 的 4T1 乳腺癌细胞和 HUVEC 具有特异性结合亲和力,但对低表达 CXCR4 的 MS-5 细胞无此结合活性[1]
Peptide E5 (0-100 μM; 24 h) 对 4T1 细胞可诱导浓度依赖性细胞毒性和凋亡[1]
Peptide E5 (0.1-10 μM; 1 h pre-incubation) 可抑制 CXCL12 诱导的 4T1 乳腺癌细胞和 HUVEC 的迁移,以及 MS-5 条件培养基诱导的 4T1 细胞迁移[1]
Peptide E5 (0.1-10 μM; 2 h pre-incubation) 以浓度依赖的方式抑制 4T1 乳腺癌细胞与 MS-5 基质细胞的黏附[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: murine breast cancer 4T1 cells, HUVECs
Concentration: 0, 1, 10, 25, 50 and 100 μM
Incubation Time: 24 h
Result: Maintained 4T1 cell viability above 90% at concentrations <25 μM.
Reduced 4T1 cell viability to 72% at 50 μM, 57% at 75 μM, and 49% at 100 μM.
Sustained HUVEC viability above 90% at all tested concentrations up to 100 μM.

Western Blot Analysis[1]

Cell Line: murine breast cancer 4T1 cells
Concentration: 0, 1, 10, 25, 50 and 100 μM
Incubation Time: 24 h
Result: increased the levels of cleaved caspase-3.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax T1/2
Mice[1] 40 mg/kg s.c. 2 h 10 h
体内研究
(In Vivo)

Peptide E5 (40 mg/kg; s.c.; every other day; day 7-33) 仅具有微弱的单药抗肿瘤活性,但可显著增强紫杉醇 Paclitaxel (HY-B0015) 和 Cyclophosphamide (HY-17420) 的抗肿瘤疗效[1]
Peptide E5 (40 mg/kg; s.c.; single dose) 在健康雌性 BALB/c 小鼠中具有相对较长的 in vivo 半衰期 (约 10 小时),其主要清除途径为肝脏代谢[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (female, 5-6 weeks old, orthotopic inoculation of 1×106 4T1 murine breast cancer cells)[1]
Dosage: 40 mg/kg
Administration: s.c.; every other day; day 7-33
Result: Did not show a significant inhibitory effect on tumor weight compared to the control group when administered alone.
Significantly reduced tumor weight compared to the control group and paclitaxel-alone group when combined with paclitaxel.
Significantly reduced tumor weight compared to the cyclophosphamide-alone group and prolonged survival compared to the cyclophosphamide-alone group when combined with cyclophosphamide.
Significantly decreased CD31 levels in tumor tissue when administered alone and in combination with paclitaxel or cyclophosphamide.
Downregulated CXCR4 expression in tumor tissue when combined with paclitaxel or cyclophosphamide.
Significantly inhibited Akt and Erk phosphorylation in tumor tissue when administered alone and in combination with cyclophosphamide.
分子量

2613.95

Formula

C113H181N39O31S

CAS 号
Sequence

Gly-Gly-Arg-Ser-Phe-Phe-Leu-Leu-Arg-Arg-Ile-Gln-Gly-Cys-Arg-Phe-Arg-Asn-Thr-Val-Asp-Asp

Sequence Shortening

GGRSFFLLRRIQGCRFRNTVDD

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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Peptide E5
目录号:
HY-P11728
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