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阻害剤

天然化合物

カタログ番号	製品名	別名	ターゲット
T12103	MR-L2		PDE
	MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).		PDE
T2013	Ponalrestat		Reductase
	Ponalrestat is an aldose reductase inhibitor.		Reductase
T22748	DQP 1105		NMDAR
	DQP 1105 is a NMDA receptor antagonist.		NMDAR
T9214	ELOVL6-IN-1		Others
	ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL6 activities, with an IC50 value of 0.350 μM. ELOVL6-IN-1 inhibits ELOVL6 in a noncompetitive manner...		Others
T11696	Ivachtin	Caspase-3 Inhibitor VII	Caspase
	Ivachtin (Caspase-3 Inhibitor VII) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor(IC50 = 23 nM) and is a modest inhibitor of the remaining caspases.		Caspase
T8461	SKI V		Apoptosis , PI3K , S1P Receptor
	SKI V is a potent and noncompetitive non-lipid sphingosine kinase (SPHK; SK) inhibitor (GST-hSK,IC50 : 2 μM), and is a PI3K inhibitor(hPI3k,IC50 : 6 μM), induces apoptosis and has antitumor activity		Apoptosis , PI3K , S1P Receptor
T6259	Dizocilpine	MK-801	NMDAR , iGluR
	MK-801 (Dizocilpine (MK-801)) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.		NMDAR , iGluR
T2694	KN-62		CaMK , P2X Receptor , Autophagy
	KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM.		CaMK , P2X Receptor , Autophagy
T4190	Ticlopidine	PCR 5332,Ticlid	ATPase , Adiponectin receptor
	Ticlopidine (PCR 5332) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor.		ATPase , Adiponectin receptor
T2463	ML141	CID-2950007	Apoptosis , CDK , Ras
	ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).		Apoptosis , CDK , Ras
T3320	Dizocilpine Maleate	(+)-Mk-801 Hydrogen Maleate,MK 801,Dizocilpine hydrogen maleate,(+)-MK 801 maleate,(+)-MK 801 (Maleate)	NMDAR , iGluR
	Dizocilpine Maleate (MK 801) is a potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) with Kd of 37.2 nM in rat brain membranes. The drug has been considered for the wide variety of ne...		NMDAR , iGluR
T3444	Merimepodib	VX-497,VI-21497	Dehydrogenase , Antiviral , HCV Protease , HBV
	Merimepodib (VX-497) is a novel noncompetitive inhibitor of Inosine monophosphate dehydrogenase(IMPDH).		Dehydrogenase , Antiviral , HCV Protease , HBV
T23353	(E/Z)-SIB-1893	SIB 1893	Others , GluR
	(E/Z)-SIB-1893 (SIB 1893) is the racemate of (E)-SIB-1893 and (Z)-SIB-1893. (E)-SIB-1893 is a selective, noncompetitive mGluR5 antagonist with anticonvulsant activity .		Others , GluR
T1979	AVN-944	VX-944	Dehydrogenase
	AVN-944 (VX-944)(VX-944) is a selective, noncompetitive inhibitor of human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.		Dehydrogenase
T8457	NPS2390		GluR
	NPS2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 (IC50 of 5.2 and 82 nM, respectively)		GluR
T22703	CYM-5520	CYM 5520	S1P Receptor , LPL Receptor
	CYM-5520 is a noncompetitive allosteric agonist of S1P2		S1P Receptor , LPL Receptor
T3591	URB602		Lipase , Antibacterial
	URB602 is a specific monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL (IC50: 28±4 μM) through a noncompetitive mechanism.		Lipase , Antibacterial
TP1888L1	[Ala113]-MBP (104-118) acetate		PKC
	[Ala113]MBP(104-118) acetate is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM.		PKC
T22425	Sevoflurane	Fluoromethyl	5-HT Receptor
	Sevoflurane (Fluoromethyl), a noncompetitive inhibitor of 5-HT3 receptor, acts as a low-soluble inhalation anesthetics.		5-HT Receptor
T3120	K858 (Racemic)	K858 Racemic,K858	Apoptosis , Kinesin
	K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner.		Apoptosis , Kinesin
T10852	CNS-5161 hydrochloride	CNS 5161A	NMDAR
	CNS-5161 hydrochloride (CNS 5161A) is a new antagonist of NMDA ion-channel. It interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.		NMDAR
T21584	CP 465022		iGluR
	CP 465022 hydrochloride is a potent, and selective noncompetitive antagonist of AMPA receptor with anticonvulsant activity. CP 465022 hydrochloride inhibits Kainate-induced response with an IC50 of 25 nM in rat cortical ...		iGluR
T1220	Ethidium bromide	EtBr,Homidium bromide,EB	AChR
	Ethidium bromide (EB) A trypanocidal agent and possible antiviral agent that is widely used in experimental cell biology and biochemistry. Ethidium has several experimentally useful properties including binding to nucle...		AChR
T8842	IMT1B	3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-,LDC203974	Others , DNA/RNA Synthesis
	IMT1B (LDC203974) is an orally administered, specific noncompetitive allosteric inhibitor of the mitochondrial RNA polymerase (POLRMT), effectively suppressing mitochondrial DNA (mtDNA) expression. This action confers it...		Others , DNA/RNA Synthesis
T21766	ML352
	ML352, a noncompetitive inhibitor of the presynaptic choline transporter (CHT), exhibits K i values of 92 nM in HEK293 cells with human CHT expression and 166 nM in mouse forebrain synaptosomes [1].
T14194	β-NETA	α-NETA	AChE
	β-NETA (α-NETA) is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM and is a potent chemokine-like receptor-1 (CMKLR1) antagonist. β-NETA has anti-cancer activit...		AChE
T3483	FTIDC		GluR
	FTIDC is a highly potent and selective allosteric antagonist of mGluR1 receptors and shows very weak potency against human and rat mGluR5 receptors. The inhibition of FTIDC for mGluR1 receptors is shown to be in noncompe...		GluR
T14844	BX430		P2X Receptor , Calcium Channel
	BX430 is used for chronic pain and cardiovascular disease and it is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity.		P2X Receptor , Calcium Channel
T8976	PD-089828		EGFR , FGFR , PDGFR , Src
	PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 ...		EGFR , FGFR , PDGFR , Src
T28754	Sepin-1	Sepin 1,Sepin1,2H-Benzimidazole, 2,2-dimethyl-5-nitro-, 1,3-dioxide	Others
	Sepin-1 is a noncompetitive inhibitor of separase (IC50 = 14.8 µM). Sepin-1 can inhibit the growth of breast cancer xenograft tumors in mice and human cancer cell lines by inhibiting cell proliferation and inducing apopt...		Others
T12425	PF-06424439 methanesulfonate		Acyltransferase , Transferase
	PF-06424439 methanesulfonate, an orally administered, potent, and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM, demonstrates slow reversibility and time-dependent inh...		Acyltransferase , Transferase
T14884	CBR-5884		Others , Dehydrogenase
	CBR-5884 is an selective, active of phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with h...		Others , Dehydrogenase
T68599	Orphenadrine	Orphenadrine (free base)	Sodium Channel , NMDAR , AChR
	Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagoni...		Sodium Channel , NMDAR , AChR
T32033	GYKI-46903 HCl	GYKI-46,903,GYKI 46,903,GYKI 46903,GYKI46,903,GYKI-46903,GYKI46903
	GYKI-46903 is a noncompetitive 5-HT3 receptor antagonist.
T16017	MB-07803		Others
	MB07803 is an orally available prodrug of an effective, noncompetitive inhibitor of fructose 1,6-bisphosphatase (FBPase) (EC50: 140 nM and t1/2 of 7.6±2.9 h).		Others
T27674	JNJ-27141491	JNJ 27141491
	JNJ-27141491 is a potent, noncompetitive antagonist of human CCR2.
T28614	RPC425 free base	RPC425,RPC-425,RPC 425
	RPC425 is a noncompetitive inhibitors of the Betaine-γ-Aminobutyric Acid Transporter 1 (BGT1).
T25516	I-A09	I-A-09,IA 09
	I-A09 is a noncompetitive mPTPB inhibitor.
T27452	GSK1723980
	GSK1723980 is a novel noncompetitive rTbIPMK inhibitor.
T24604	PDAT	Propyl Dimethyl Amino Tryptamine
	PDAT is a noncompetitive Indolethylamine N-methyltransferase inhibitor.
T26673	AT-076	AT 076
	AT-076 is a noncompetitive antagonist of the κ-opioid receptor (Ki = 1.14 nM) and nociceptin receptor (Ki = 1.75 nM) and a competitive antagonist of the μ-opioid receptor (Ki = 1.67 nM) and δ-opioid receptor (Ki = 19.6 n...
T13429	α-2,3-sialyltransferase-IN-1	Lith-O-Asp analog	Others
	α-2,3-sialyltransferase-IN-1 is a noncompetitive inhibitor of α-2,3-sialyltransferase(IC50 of 6 μM).		Others
TQ0233L	Traxoprodil Mesylate
	Traxoprodil Mesylate is a potent noncompetitive N-methyl-D-aspartate (NMDA) receptors antagonist and has selective for the NR2B subunit.
T70467	Alinastine
	Alinastine is a noncompetitive histamine H1 receptor antagonist.
T11171	EIF4A3-IN-2		Others
	eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 inhibitor with an IC50 of 110 nM.		Others
T14774	Bragsin1		Others
	Bragsin1 is a potent and selective and noncompetitive ArfGEF BRAG2 inhibitor, inhibits Arf GTPase activation(IC50 : 3 μM),and with anti-cancer activity.		Others
T61430	S-2E
	S-2E is a compound that functions as an orally active, noncompetitive inhibitor of both HMG-CoA reductase and acetyl-CoA carboxylase. It exhibits an anti-hyperlipidemic action, making it suitable for studying conditions ...
T28893	SX-517	SX 517
	SX-517 is a potent noncompetitive boronic acid CXCR1/2 antagonist. SX-517 inhibits CXCL1-induced Ca(2+) flux (IC50 = 38 nM) in human PMNs.
T38050	CP-609754		Transferase
	CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 n...		Transferase
T10552	Bitopertin (R enantiomer)	RO4917838 (R enantiomer),RG1678 (R enantiomer),Bitopertin R enantiomer	GlyT
	Bitopertin R enantiomer (RG1678 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a noncompetitive glycine reuptake inhibitor and inhibits glycine uptake at human GlyT1 (IC50: 25 nM).		GlyT

Compounds

Synonym: Caspase-3 Inhibitor VII

Target: Apoptosis, PI3K, S1P Receptor

Target: CaMK, P2X Receptor, Autophagy

Ticlopidine

T4190

Synonym: PCR 5332,Ticlid

Target: ATPase, Adiponectin receptor

ML141

T2463

Synonym: CID-2950007

Target: Apoptosis, CDK, Ras

Dizocilpine Maleate

T3320

Synonym: (+)-Mk-801 Hydrogen Maleate,MK 801,Dizocilpine hydrogen maleate,(+)-MK 801 maleate,(+)-MK 801 (Maleate)

Target: NMDAR, iGluR

Merimepodib

T3444

Synonym: VX-497,VI-21497

Target: Dehydrogenase, Antiviral, HCV Protease, HBV

Target: Dehydrogenase

Target: S1P Receptor, LPL Receptor

URB602

T3591

Synonym:

Target: Lipase, Antibacterial

[Ala113]-MBP (104-118) acetate

Synonym: Fluoromethyl

Target: 5-HT Receptor

K858 (Racemic)

T3120

Synonym: K858 Racemic,K858

Target: Apoptosis, Kinesin

CNS-5161 hydrochloride

Synonym: EtBr,Homidium bromide,EB

Target: AChR

IMT1B

T8842

Synonym: 3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-,LDC203974

Target: Others, DNA/RNA Synthesis

Target: P2X Receptor, Calcium Channel

PD-089828

T8976

Synonym:

Target: EGFR, FGFR, PDGFR, Src

Sepin-1

T28754

Synonym: Sepin 1,Sepin1,2H-Benzimidazole, 2,2-dimethyl-5-nitro-, 1,3-dioxide

Target: Others

PF-06424439 methanesulfonate

T12425

Synonym:

Target: Acyltransferase, Transferase

CBR-5884

T14884

Synonym:

Target: Others, Dehydrogenase

Orphenadrine

T68599

Synonym: Orphenadrine (free base)

Target: Sodium Channel, NMDAR, AChR

GYKI-46903 HCl

T32033

Synonym: GYKI-46,903,GYKI 46,903,GYKI 46903,GYKI46,903,GYKI-46903,GYKI46903

Synonym: JNJ 27141491

Target:

RPC425 free base

T28614

Synonym: RPC425,RPC-425,RPC 425

Target:

I-A09

T25516

Synonym: I-A-09,IA 09

Synonym: Propyl Dimethyl Amino Tryptamine

α-2,3-sialyltransferase-IN-1

T13429

Synonym: Lith-O-Asp analog

Bitopertin (R enantiomer)

T10552

Synonym: RO4917838 (R enantiomer),RG1678 (R enantiomer),Bitopertin R enantiomer

Target: GlyT

カタログ番号	製品名	別名	ターゲット
T6S2391	L-Chicoric Acid	(-)-Chicoric acid,trans-Caffeoyltartaric acid,Chicoric acid,dicaffeoyltartaric acid	Others , HIV Protease
	L-Chicoric Acid (trans-Caffeoyltartaric acid) has been shown to inhibit hyaluronidase and HIV-1 integrase, and to possess phagoeytosis stimulatory activity in vitro and in vivo and antiviral acitivy. L-Chicoric acid may ...		Others , HIV Protease
T16535	Picrotoxinin		Chloride channel , GABA Receptor
	Picrotoxinin is a blocker of chloride channel and a noncompetitive antagonist of GABAA with an IC50 of 1.15 μM for α1β2γ2L GABAA. Picrotoxinin shows convulsant properties.		Chloride channel , GABA Receptor
T3S2072	3-Butylidenephthalide	Butylidene phthalide,n-Butylidenephthalide	Parasite , Glucosidase
	1. 3-Butylidenephthalide (Butylidene phthalide) has antihyperglycemic effect is due to inhibition of α-glucosidase at the intestinal level, inhibited the activity of yeast-α-glucosidase (IC(5) 2.35 mM) in a noncompetitiv...		Parasite , Glucosidase
T3865	Beta-Eudesmol	Beta-Selinenol	TRP/TRPV Channel , AChR
	beta-Eudesmol (Beta-Selinenol) is a noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). It is a sesquiterpene that has been found in a variety of plants, including Cannabis, and has diverse biologica...		TRP/TRPV Channel , AChR
TN1928	Methyl rosmarinate		MMP , Anti-infection , Tyrosinase
	Methyl rosmarinate is a noncompetitive tyrosinase inhibitor which is isolated from Rabdosia serra, with an IC50 of 0.28 mM for mushroom tyrosinase.Methyl rosmarinate shows antioxidative, and antifungal activities. It has...		MMP , Anti-infection , Tyrosinase
T8182	Guanfu base A	Guan-fu base A	P450 , Potassium Channel , HER
	Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.		P450 , Potassium Channel , HER
TN1544	D-Menthol	Menthol,(+)-MENTHOL	Calcium Channel , 5-HT Receptor , AChR
	D-Menthol ((+)-MENTHOL) is a common compound in pharmaceutical and commercial products and a popular additive to cigarettes, it attenuates α±7 mediated Ca 2+ transients in the cell body and neurite, suggests that menthol...		Calcium Channel , 5-HT Receptor , AChR
T2940	6-Hydroxyflavone	6-HF	GABA Receptor
	6-Hydroxyflavone (6-HF) is a noncompetitive inhibitors of cytochrome P450 2C9. It is a flavone, a type of chemical compound. It is reported in leaves of Barleria prionitis Linn. (a common Acanthaceae from India). 6-Hydro...		GABA Receptor
T38241	2-Aminoimidazole
	2-Aminoimidazole is a potent antibiofilm agent and adjuvant to antimicrobial treatments, which effectively disrupts bacterial self-protection mechanisms by inhibiting biofilm formation and genetically-encoded antibiotic ...
T16011	Manumycin A		Prostaglandin Receptor
	Manumycin A is an antibiotic. Manumycin A induces apoptosis and exerts antitumor activity. Manumycin A inhibits exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A acts as a ...		Prostaglandin Receptor
T82241	Halichondrin B
	Halichondrin B, sourced from the sponge Halichondria okadai, serves as a noncompetitive inhibitor of Vinca-alkaloid binding to tubulin, with an IC 50 for tubulin polymerization ranging from 1.2-1.4 μM, and exhibits anti-...