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TC14012 acetate

TC14012 acetate 是 T140 的血清稳定衍生物，是一种选择性的肽模拟 CXCR4 拮抗剂，IC50 为 19.3 nM。 TC14012 还是一种有效的 CXCR7 激动剂，EC50 为 350 nM，可将 β-arrestin 2 募集到 CXCR7。 TC14012 具有抗癌活性和抗 HIV 活性。

CAS号

TP2112L

分子式

C92H144N34O21S2

主要靶点

CXCR

仅限科研使用

Cat No : CM13707

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Synonyms

TC14012 acetate(368874-34-4 free base)

验证数据展示

  • CAS No.: TP2112L

    TC14012 acetate
    CAS#: TP2112L

产品信息

TC14012 acetate is a serum-stable derivative of T140 which is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is also a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-cancer activity and anti-HIV activity.

CAS号 TP2112L
分子式 C92H144N34O21S2
主要靶点 CXCR
主要通路 G蛋白偶联受体|自噬|免疫与炎症
分子量 2126.47
纯度 99.71%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 TC14012 acetate(368874-34-4 free base)

靶点活性

CXCR4:19.3 nM|CXCR7:350 nM (EC50)

体外活性

TC14012 (1 mM) inhibits more than 95% the infection of the CXCR4-expressing cells by the HXB2 (X4) or 89.6 (dual-tropic) strain. TC14012 (1 mM) does not inhibit all the infection of the CCR5-expressing cells by the SF162 (R5) or 89.6 (dualtropic) strain. TC14012 leads to erk 1/2 phosphorylation in U373 cells, which express endogenous CXCR7 but not CXCR4. CXCR7 and the CXCR7-Cter4 chimera are able to recruit arrestin upon stimulation with TC14012 whereas CXCR4 and CXCR4-Cter7 remain silent.

参考文献

1.H Tamamura, et al. Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1897-902. 2.Stéphanie Gravel, et al. The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains. J Biol Chem. 2010 Dec 3;285(49):37939-43.

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