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ターゲット

阻害剤

天然化合物

リコンビナントタンパク質

カタログ番号	製品名	別名	ターゲット
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
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.
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.
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...
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...
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. Pharm...

Compounds

EPI-001

T6829

Synonym: EPI001,EPI 001

Target: Apoptosis, Androgen Receptor, PPAR

ORM-15341

T12323

Synonym:

Target: Androgen Receptor

Pifithrin-α hydrobromide

T2707

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

Target: Ferroptosis, Aryl Hydrocarbon Receptor, p53

ZL0580

T13974

Synonym:

Target: Epigenetic Reader Domain, HIV Protease

Synonym: c-Myc Inhibitor

Target: c-Myc, Autophagy

Anticancer agent 73

T60420

Synonym:

Target: DNA/RNA Synthesis

Ro5-3335

T4687

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

Target: DNA/RNA Synthesis

Synonym: CGP-64222,CGP 64222

Target:

Difelikefalin (trifluoroacetate salt)

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

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

カタログ番号	製品名	ターゲット
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
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 ...
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 regulat...

天然物製品

Tetramethylcurcumin

TN2269

Synonym:

Target: Apoptosis, STAT

Recombinant Proteins

Species：

Expression System：

Tag：

カタログ番号	製品名	Species	Expression System
TMPH-01345	FIZ1 Protein, Human, Recombinant (His)	Human	E. coli
	May be a transcriptional repressor of NRL function in photoreceptors. Does not repress CRX-mediated transactivation. FIZ1 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The ...
TMPH-02272	JAK1 Protein, Human, Recombinant (E. coli, His)	Human	E. coli
	Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but ...
TMPH-02961	JAK1 Protein, Mouse, Recombinant (His)	Mouse	E. coli
	Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but ...
TMPH-01305	ER beta Protein, Human, Recombinant (His)	Human	P. pastoris (Yeast)
	Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1/ER-alpha, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner.; Lacks ...
TMPH-02273	JAK1 Protein, Human, Recombinant (His)	Human	P. pastoris (Yeast)
	Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but ...
TMPH-01304	ER beta Protein, Human, Recombinant (E. coli, His)	Human	E. coli
	Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1/ER-alpha, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner.; Lacks ...
TMPH-01654	MAGEA1 Protein, Human, Recombinant (His)	Human	P. pastoris (Yeast)
	May be involved in transcriptional regulation through interaction with SNW1 and recruiting histone deactelyase HDAC1. May inhibit notch intracellular domain (NICD) transactivation. May play a role in embryonal developmen...
TMPH-01796	NR4A1 Protein, Human, Recombinant (His & Myc)	Human	E. coli
	Orphan nuclear receptor. May act concomitantly with NURR1 in regulating the expression of delayed-early genes during liver regeneration. Binds the NGFI-B response element (NBRE) 5'-AAAAGGTCA-3'. May inhibit NF-kappa-B tr...
TMPH-01512	HIF1AN Protein, Human, Recombinant (His)	Human	P. pastoris (Yeast)
	Hydroxylates HIF-1 alpha at 'Asn-803' in the C-terminal transactivation domain (CAD). Functions as an oxygen sensor and, under normoxic conditions, the hydroxylation prevents interaction of HIF-1 with transcriptional coa...
TMPH-02055	RBPMS Protein, Human, Recombinant (His & Myc)	Human	E. coli
	Acts as a coactivator of transcriptional activity. Required to increase TGFB1/Smad-mediated transactivation. Acts through SMAD2, SMAD3 and SMAD4 to increase transcriptional activity. Increases phosphorylation of SMAD2 an...
TMPH-02941	MAFK Protein, Mouse, Recombinant (His & Myc & SUMO)	Mouse	E. coli
	Since they lack a putative transactivation domain, the small Mafs behave as transcriptional repressors when they dimerize among themselves. However, they act as transcriptional activators by dimerizing with other (usuall...
TMPH-02940	MAFK Protein, Mouse, Recombinant (His & Myc)	Mouse	HEK293 Cells
	Since they lack a putative transactivation domain, the small Mafs behave as transcriptional repressors when they dimerize among themselves. However, they act as transcriptional activators by dimerizing with other (usuall...
TMPJ-00886	ATF1 Protein, Human, Recombinant (His)	Human	E. coli
	Cyclic AMP-dependent transcription factor ATF-1(ATF1) which contains 1 bZIP (basic-leucine zipper) domain and 1 KID (kinase-inducible) domain, belongs to the bZIP family. It influences cellular physiologic processes by r...
TMPY-06821	THRB Protein, Human, Recombinant (His)	Human	E. coli
	Thyroid hormone receptor beta (THRB), also known as TRbeta and NR1A2, belongs to the nuclear hormone receptor family. Featuring an N-terminal transactivation domain, a central DNA-binding domain, and a hormone/ligand-bin...
TMPH-02613	ATF-5 Protein, Mouse, Recombinant (His & Myc)	Mouse	E. coli
	Transcription factor that either stimulates or represses gene transcription through binding of different DNA regulatory elements such as cAMP response element (CRE) (consensus: 5'-GTGACGT[AC][AG]-3'), ATF5-specific respo...