transactivation — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T6829	EPI-001	EPI001,EPI 001	Apoptosis , Androgen Receptor , PPAR
	EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.		Apoptosis , Androgen Receptor , PPAR
T12323	ORM-15341		Androgen Receptor
	ORM-15341 is a potent and full antagonist for human AR (hAR)( with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells)		Androgen Receptor
T2707	Pifithrin-α hydrobromide	Pifithrin hydrobromide,Pifithrin-α (PFTα) HBr,Pifithrin-α,PFTα,PFTα hydrobromide	Ferroptosis , Aryl Hydrocarbon Receptor , p53
	Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes.		Ferroptosis , Aryl Hydrocarbon Receptor , p53
T13974	ZL0580		Epigenetic Reader Domain , HIV Protease
	ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter.		Epigenetic Reader Domain , HIV Protease
T5532	BMS-687453		PPAR
	BMS-687453 is a potent and selective PPAR alpha agonist, with an EC(50) of 10 nM for human PPARalpha and approximately 410-fold selectivity vs human PPARgamma in PPAR-GAL4 transactivation assays.		PPAR
T7395	Lanifibranor	IVA337	PPAR
	Lanifibranor (IVA337) is an agonist of peroxisome proliferator-activated receptors (PPARs) with EC50 values of 1,537, 866, and 206 nM for human recombinant PPARα, PPARβ, and PPARγ, respectively, for transactivation activ...		PPAR
TN2269	Tetramethylcurcumin		Apoptosis , STAT
	Tetramethylcurcumin is a novel curcumin analog, is an effective inhibitors of STAT3 phosphorylation, DNA binding activity, and transactivation in vitro.it also inhibits colony formation in soft agar, cell invasion, and e...		Apoptosis , STAT
T3048	10058-F4	c-Myc Inhibitor	c-Myc , Autophagy
	10058-F4 (c-Myc Inhibitor) is a cell-permeable thiazolidinone that specifically inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression; induces cell-cycle arrest and apoptosis.		c-Myc , Autophagy
T60420	Anticancer agent 73		DNA/RNA Synthesis
	Anticancer agent 73 is an anticancer agent which potently targets transactivation response(TAR) RNA-binding protein 2 (TRBP) and disrupts the TRBP-Dicer interaction. Anticancer agent 73 suppresses the growth and metasta...		DNA/RNA Synthesis
T4687	Ro5-3335	CBFβ-Runx1 inhibitor II,Ro 5-3335	DNA/RNA Synthesis
	Ro5-3335 (CBFβ-Runx1 inhibitor II) is core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). Ro5-3335 represses RUNX1/CBFβ-dependent transactivation ...		DNA/RNA Synthesis
T70387	CCCTP
	CCCTP is a potent inhibitor of the 11β-HSD-1 enzyme with reduced pregnane-X receptor (PXR) transactivation activity.
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 ...
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 m...
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.
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...
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 m...
T63636	JTP-117968
	JTP-117968 is a selective glucocorticoid receptor modulator (non-steroidal SGRM with an IC50 value of 6.8 nM) that exhibits improved transcriptional inhibition/transactivation dissociation.
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 ...
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 nanomol...
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 ...