transactivation

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。

Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) 是一种 p53 抑制剂，可抑制 p53 反应基因的 p53 依赖性反式激活。它也是芳烃受体的激动剂。

Tetramethylcurcumin 是一种新型姜黄素类似物，是一种有效的 STAT3 磷酸化、DNA 结合活性和体外反式激活抑制剂。它具有抗炎和抗癌作用。

ORM-15341 是雄激素受体拮抗剂，作用于 AR-HEK293细胞(IC50:38 nM)。

ZL0580 通过抑制 Tat 反式激活和转录延伸以及通过在 HIV 启动子处诱导抑制性染色质结构来诱导 HIV 抑制。

SC428作为一种雄性激素受体(AR)的抑制剂，专门针对AR的N-端结构域。该化合物能够有效抑制AR-V7、ARv567es以及全长AR(AR-FL)及其LBD变体的转激活作用。此外，SC428在雄激素刺激下显著阻止AR-FL的核内迁移、染色质结合，以及AR调控的基因转录。在体外实验中，SC428有效抑制肿瘤细胞的增殖，并且在小鼠体内，通过移植22Rv1肿瘤细胞模型，SC428通过诱导细胞凋亡显著抑制肿瘤生长。

NSC308848 是一种有效的 Myc 依赖性 apoptosis 诱导剂。它通过抑制 Myc 的转激活功能和妨碍 Myc 家族蛋白的 DNA 结合活性来发挥作用。

PPAR agonist6 (compound 5a) 是一种PPAR的激动剂，其对PPARα、PPARβ/δ和PPARγ的EC50值分别为3.6 μM和2.6 μM。PPAR agonist6 可以抑制L929细胞中TNFα依赖性NF-κB驱动的报告基因的转录激活[1]。

PPARδ agonist10 (compound 7) 是一种口服活性、选择性的PPARδ部分激动剂，对hPPARδ(LBD)-GAL4和mPPARδ的EC50值分别为0.053 μM和0.30 µM。在反式激活测定中，PPARδ agonist10 作为部分PPARδ激动剂，但在体外和体内均能完全激活肌肉细胞的游离脂肪酸氧化。该化合物适用于血脂异常的研究。

CGP64222, a peptoid Tat/transactivation response element inhibitor, inhibits human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry.

UNBS-1450 is a sodium channel antagonist. UNBS-1450 is a hemi-synthetic cardenolide derived from 2″-oxovorusharin, it is effective against various cancer cell types with an excellent differential toxicity. At low nanomolar concentrations, UNBS-1450 induce

10058-F4 (c-Myc Inhibitor) 是一种细胞渗透性噻唑烷酮，可特异性抑制 c-Myc-Max 相互作用并防止 c-Myc 靶基因表达的反式激活；诱导细胞周期停滞和凋亡。

BMS-695735, a benzimidazole inhibitor of insulin-like growth factor-1 receptor, has broad-spectrum antitumor activity in vivo. It was found that BMS-695735 had strong inhibition of CYP3A4, induction of CYP3A4 mediated by PXR transactivation, poor water so

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

(E)-Guggulsterone是一种Guggulsterone的异构体。(E)-Guggulsterone是一种FXR拮抗剂，能够降血脂，还能够诱导血红素氧化酶-1表达、阻断DENV NS2B/3B活性，抑制DENV复制。

Difelikefalin is a κ-opioid receptor (KOR) agonist.1It activates KOR in HEK293 cells expressing the human receptor (EC50= 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50= 0.048 nM). Difelikefalin is selective for KOR over the μ-opioid receptor (MOR; EC50= >1 μM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively). 1.Schteingart, C.D., Menzaghi, F., Jiang, G., et al.Synthetic peptide amides(2008)

Ro5-3335 (CBFβ-Runx1 inhibitor II) 是苯二氮化合物，是RUNX1-CBFβ 相互作用抑制剂，可抑制 RUNX1/CBFB 依赖性反式激活，能作为核心结合因子 (CBF) 白血病抑制剂。

BMS-687453 是一种选择性 PPARα激动剂，对人 PPARα的 EC50和 IC50分别为 10 nM 和 260 nM。它较弱地抑制 PPARγ 的活性，EC50和 IC50值分别为 4100 nM 和大于 15000 nM。

Anticancer agent 73 是一种抗癌剂，它能有效地靶向反式激活反应（TAR）RNA 结合蛋白2（TRBP），并破坏TRBP-Dicer 的相互作用。Anticancer agent 73 通过调节 HCC 细胞中 miRNA 组和蛋白质组的表达谱，在体外和体内抑制 HCC 的生长和转移。

Ivaltinostat (CG-200745) formic 是一种口服具有活力的泛 HDAC 抑制剂，具有异羟肟酸部分，能够在催化袋底部结合锌。Ivaltinostat formic 对组蛋白 H3 和微管蛋白的脱乙酰作用具有抑制效果。Ivaltinostat formic 能够促使 p53 的积累，诱导 p53 依赖性反式激活，并提高 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 增加 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU) 的敏感性。Ivaltinostat formic 诱导凋亡，并具有抗肿瘤效果。

JTP-117968 是一种选择性的糖皮质激素受体调节剂 (非甾类的 SGRM，IC50值为 6.8 nM)，表现出改善的转录抑制/转激活解离效果。

Difelikefalin TFA is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin TFA is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively).

Difelikefalin HCl is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin HCl is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively).

CCCTP is a potent inhibitor of the 11β-HSD-1 enzyme with reduced pregnane-X receptor (PXR) transactivation activity.