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19

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6829	EPI-001 EPI001,EPI 001	Apoptosis; Androgen Receptor; PPAR	Apoptosis; DNA Damage/DNA Repair; Endocrinology/Hormones; Metabolism
	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。
T12323	ORM-15341	Androgen Receptor	Endocrinology/Hormones
	ORM-15341 是雄激素受体拮抗剂，作用于 AR-HEK293细胞(IC50:38 nM)。
T13974	ZL0580	Epigenetic Reader Domain; HIV Protease	Chromatin/Epigenetic; Microbiology/Virology; Proteases/Proteasome
	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。
T3048	10058-F4 c-Myc Inhibitor	c-Myc; Autophagy	Autophagy; Cell Cycle/Checkpoint
	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。
T2707	Pifithrin-α hydrobromide Pifithrin hydrobromide,Pifithrin-α (PFTα) HBr,Pifithrin-α,PFTα,PFTα hydrobromide	Ferroptosis; Aryl Hydrocarbon Receptor; p53	Apoptosis; Immunology/Inflammation
	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。
T7395	Lanifibranor IVA337	PPAR	DNA Damage/DNA Repair; Metabolism
	Lanifibranor (IVA337) 是泛过氧化物酶体增殖物激活受体 (PPAR) 激动剂，对人类PPARα，PPARσ和PPARγ的EC50值分别为 1.5, 0.87 和 0.21 μM。
T5532	BMS-687453	PPAR	DNA Damage/DNA Repair; Metabolism
	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。
T60420	Anticancer agent 73	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	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。
T4687	Ro5-3335 CBFβ-Runx1 inhibitor II,Ro 5-3335	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	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。
T26999	CGP64222 CGP-64222,CGP 64222
	CGP64222, a peptoid Tat/transactivation response element inhibitor, inhibits human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry.
T69537	Difelikefalin HCl
	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...
T69530	Difelikefalin TFA
	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...
T70387	CCCTP
	CCCTP is a potent inhibitor of the 11β-HSD-1 enzyme with reduced pregnane-X receptor (PXR) transactivation activity.
T30538	BMS-695735 CHEMBL459729,DNC008930,BMS 695735,BMS695735,BDBM27888
	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
T63636	JTP-117968
	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。
T37483	Difelikefalin (trifluoroacetate salt)
	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 m...
T29060	UNBS-1450 UNBS 1450,UBS1450,UBS-1450,UBS 1450
	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
T71305	Clofibric Acid-d4
	Clofibric acid-d4 is intended for use as an internal standard for the quantification of clofibric acid by GC- or LC-MS. Clofibric acid is a peroxisome proliferator-activated receptor α (PPARα) agonist (EC50 = 50 µM in a transactivation assay) and the active metabolite of clofibrate. It is formed from clofibrate by tissue and serum esterases. Dietary administration of clofibric acid (0.067-0.22%) reduces serum cholesterol, phospholipid, and triglyceride levels in rats. It decreases glutamate oxal...
T35813	CAY10592
	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) ...

化合物

Cat.No: T6829

Synonym: EPI001,EPI 001

Target: Apoptosis, Androgen Receptor, PPAR

Cat.No: T12323

Target: Androgen Receptor

Cat.No: T13974

Target: Epigenetic Reader Domain, HIV Protease

Cat.No: T3048

Synonym: c-Myc Inhibitor

Target: c-Myc, Autophagy

Pifithrin-α hydrobromide

Cat.No: T2707

Synonym: Pifithrin hydrobromide,Pifithrin-α (PFTα) HBr,Pifithrin-α,PFTα,PFTα hydrobromide

Target: Ferroptosis, Aryl Hydrocarbon Receptor, p53

Cat.No: T7395

Synonym: IVA337

Target: PPAR

Cat.No: T5532

Target: PPAR

Anticancer agent 73

Cat.No: T60420

Target: DNA/RNA Synthesis

Cat.No: T4687

Synonym: CBFβ-Runx1 inhibitor II,Ro 5-3335

Target: DNA/RNA Synthesis

Cat.No: T26999

Synonym: CGP-64222,CGP 64222

Difelikefalin HCl

Cat.No: T69537

Difelikefalin TFA

Cat.No: T69530

Cat.No: T70387

Cat.No: T30538

Synonym: CHEMBL459729,DNC008930,BMS 695735,BMS695735,BDBM27888

Cat.No: T63636

Difelikefalin (trifluoroacetate salt)

Cat.No: T37483

Cat.No: T29060

Synonym: UNBS 1450,UBS1450,UBS-1450,UBS 1450

Clofibric Acid-d4

Cat.No: T71305

Cat.No: T35813

Cat. No.	Product Name	Target	Signaling Pathways
TN2269	Tetramethylcurcumin	Apoptosis; STAT	Apoptosis; JAK/STAT signaling; Stem Cells
	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。
T36438	Sporogen-AO 1
	Sporogen-AO 1 is a fungal metabolite originally isolated fromA. oryzaethat has diverse biological activities.1,2,3,4,5It inhibits HIV-1 Tat transactivation in a cell-based assay with an IC50value of 15.8 μM.4Sporogen-AO 1 is cytotoxic to HeLa, KB, and NCI H187 cancer cells (IC50s = 8.3, 9, and 5.1 μM, respectively).2,5It is active againstC. albicans(MIC = 4 mM).3 1.Tanaka, S., Wada, K., Marumo, S., et al.Structure of sporogen-ao 1, a sporogenic substance of Aspergillus oryzaeTetrahedron Lett.25(...
T36563	(E)-Guggulsterone
	Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hy...

天然产物

Tetramethylcurcumin

Cat.No: TN2269

Target: Apoptosis, STAT

Cat.No: T36438

(E)-Guggulsterone

Cat.No: T36563

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