化合物EPI-001 T6829

Product Introduction
Bioactivity


英文名: EPI-001

描述: EPI-001 是一种选择性雄激素受体 (AR) 的抑制剂，靶向 AR 的反式激活单元 5，可抑制 AR 氨基末端结构域的反式激活，IC50值约为 6 μM。它也是一种选择性的PPARγ调节剂，对去势抵抗性前列腺癌具有活性。

细胞实验: LNCaP cells are treated with bicalutamide (BIC) or EPI-001 for 1 hr before the addition of R1881 (0.1 nM) for 4 days. LNCaP cells are treated with OCM (50%) with, or without, EPI-001 for 3 days (serum-free, androgen-free, phenol red-free conditions).(Only for Reference)

体外活性: EPI-001 blocks transactivation of the AR NTD, interacts with the AF-1 region, inhibits protein-protein interactions with AR, and reduces AR interaction with androgen-response elements on target genes. In LNCaP cells, EPI-001 inhibits both androgen-dependent and androgen-independent (OCM-induced) cell proliferation. [1] In LNCaP cells, EPI-001 also acts as a PPAR-gamma modulator to result in inhibition of androgen receptor expression and activity, which inhibits prostate cancer growth. [2]

体内活性: In male mice bearing CRPC LNCaP s.c. xenografts, EPI-001 (50 mg/kg, i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth by reducing proliferation and increasing apoptosis. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 70 mg/mL (177.3 mM)
Ethanol : 70 mg/mL (177.3 mM)


关键字: Androgen | amino-terminal | anti-tumor | domain | EPI-001 | PPAR | inhibit | Peroxisome proliferator-activated receptors | PPARγ | Apoptosis | transactivation | Receptor | NTD | Androgen Receptor | Inhibitor

相关产品: Apoptosis inducer 11 | L-Cystathionine | NSC 95397 | Thalidomide | DC_AC50 | KH16 | NVP-TNKS656 | Tuvusertib | Diphenyl disulfide | Pectolinarin

相关库: Anti-Prostate Cancer Compound Library | ReFRAME Related Library | Inhibitor Library | Anti-Diabetic Compound Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library | Apoptosis Compound Library | Metabolism Compound Library | Preclinical Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途