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48

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T15143	DMP-543 XR-543	Others; Potassium Channel	Membrane transporter/Ion channel; Others
	DMP-543 (XR-543) 是一种钾离子通道 (KV7 channel) 阻滞剂。DMP-543可以增强神经递质的释放。
T8840	PF-543 hydrochloride PF-543	Apoptosis; S1P Receptor; Autophagy; LPL Receptor	Apoptosis; Autophagy; GPCR/G Protein
	PF-543 hydrochloride (PF-543) 是一种选择性可逆和鞘氨醇竞争性SPHK1抑制剂，对SPHK1的选择性是 SPHK2 的 100 倍以上。它还是全血中 1-磷酸鞘氨醇形成的有效抑制剂，诱导细胞凋亡、坏死和自噬。
T29188	YM-543 trimethylamine ASP 543,ASP-543,ASP543
	YM-543, a sodium-glucose transporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.
T6085	PF-543 Sphingosine Kinase 1 Inhibitor II,PF 543	Apoptosis; S1P Receptor; Autophagy; LPL Receptor	Apoptosis; Autophagy; GPCR/G Protein
	PF-543 (Sphingosine Kinase 1 Inhibitor II) 是一种选择性可逆和鞘氨醇竞争性 SPHK1抑制剂，可诱导细胞凋亡、坏死和自噬。它对 SPHK1的选择性是 SPHK2 的 100 倍以上。它还抑制全血中 1-磷酸鞘氨醇形成，IC50为 26.7 nM。
T70390	YM-543 choline
	YM-543, also known as ASP-543, is a selective SGLT2 inhibitor. Sodium-glucose cotransporter 2 (SGLT2) is a specifically expressed transporter in the kidney that plays an important role in renal glucose reabsorption, and its inhibition may present a novel therapeutic strategy for treating diabetes. YM543 potently and selectively inhibited mouse and human SGLT2 activities at nanomolar ranges. In vivo single oral administration of YM543 dose-dependently and significantly reduced blood glucose level...
T12436	PF-543 Citrate Sphingosine Kinase 1 Inhibitor II Citrate	S1P Receptor	GPCR/G Protein
	PF-543 Citrate is an inhibitor of sphingosine-competitive SPHK1(IC50 of 2 nM ).
TP2452	Collagen type IV alpha1 (531-543) Hep III peptide,Gefyfdlrlkgdk
	Collagen type IV alpha1 (531-543) is a protein that in humans is encoded by the COL4A1 gene on chromosome 13. It is ubiquitously expressed in many tissues and cell types. COL4A1 is a subunit of type IV collagen and plays a role in angiogenesis.
T68922	YM543 free base
	YM543 free base 为口服有效的钠-葡萄糖协同转运蛋白(SGLT) 2抑制剂，主要用于降低血糖水平，适用于糖尿病研究。
T20954	Varlitinib Tosylate Varlitinib-Tosylate,ARRY-334543 Tosylate,ARRY-543 Tosylate
	Varlitinib Tosylate is a selective and potent inhibitor of ErbB1(EGFR) and ErbB2(HER2).
T82354	GAD65 (524-543)
	GAD65 (524-543) 是具有生物活性的肽，属于谷氨酸脱羧酶 65 (GAD65) 氨基酸片段 524-543。作为胰岛抗原的关键片段之一，该肽在自发性自身免疫性糖尿病非肥胖糖尿病 (NOD) 小鼠模型中，可诱导增殖性 T 细胞反应。GAD65 (524-543) 对T细胞克隆BDC2.5具有特异性刺激作用，但可能存在亲和力较低的问题。此外，p524-543免疫可增强NOD小鼠对通过BDC2.5 T细胞过继转移诱导的1型糖尿病的敏感性。
T21919	UCF 101	Apoptosis	Apoptosis
	UCF 101 是竞争性的促凋亡蛋白酶Omi/HtrA2选择性抑制剂。它对 MI/R 损伤具有明显的心脏保护作用，还具有一定的神经保护作用。它在 543 nm 处具有天然的红色荧光，可用于监视其进入哺乳动物细胞的能力。
T70389	BMS986126
	BMS-986122 is a IRAK4 Inhibitor. BMS-986126 attenuates Disease in Murine Lupus Models and Demonstrates Steroid Sparing Activity. BMS-986126 inhibited TLR7- and TLR9-dependent responses using cells derived from lupus patients, suggesting that inhibition of IRAK4 has the potential for therapeutic benefit in treating lupus.
T50082	Org 25543	Chloride channel	Membrane transporter/Ion channel
	Org 25543 是一种 N-酰基氨基酸的开发，它选择性地抑制甘氨酸转运蛋白 2 以在大鼠慢性疼痛模型中产生镇痛作用。
T21712	BAY 41-8543	Others; Guanylate cyclase	GPCR/G Protein; Others
	BAY 41-8543 是一种不依赖一氧化氮的可溶性鸟苷酸环化酶 (sGC) 刺激剂，具有抗血小板作用。它在大鼠的肺和全身血管床中具有血管舒张活性，有用于心血管疾病的研究潜力。
T7742	GW 284543 hydrochloride	MEK	MAPK
	GW 284543 hydrochloride 是 MEK5 的选择性抑制剂。
T22345	INCB054329 INCB-054329,INCB-54329,INCB-54329	Epigenetic Reader Domain	Chromatin/Epigenetic
	INCB054329 是一种结构不同的溴结构域和末端外结构域 (BET) 抑制剂，可抑制 BRD2-BD1、BRD2-BD2、BRD3-BD1、BRD3-BD2、BRD4-BD1、BRD4-BD2、BRDT-BD1 和 BRDT-BD2，IC50 值为分别为 44 nM、5 nM、9 nM、1 nM、28 nM、3 nM、119 nM 和 63 nM。
T22126	Org 25543 hydrochloride	GlyT	Neuroscience
	Org 25543 hydrochloride 是一种有效的选择性甘氨酸转运蛋白 2 型 (GlyT2) 抑制剂（hGlyT2 的 IC50 = 16 nM）。在 CHO 细胞的甘氨酸摄取测定中，对 GlyT1 或 56 种其他常见生物靶标 (≥ 100 μM) 没有显示活性。
T23145	PHA 543613	Others; AChR	Neuroscience; Others
	PHA 543613 是一种特异性 α7 nAChR 激动剂 (Ki = 8.8 nM) ，可用于阿尔茨海默病和精神分裂症认知缺陷的研究。
T10783	CGS 15435	PPAR	DNA Damage/DNA Repair; Metabolism
	CGS 15435是一种有效的血栓素(TxA2)合成酶抑制剂(IC50: 1 nM)。CGS 15435作用于 PGI2合成酶、环氧合酶和脂合酶比作用于血栓素合成酶选择性低得多。
T7610	GW284543 UNC10225170	MEK	MAPK
	GW284543 (UNC10225170) 是一个选择性的MEK5抑制剂，可降低 pERK5，并下调内源性 MYC 蛋白。
T5124	SRT 1720 dihydrochloride[925434-55-5(free base)]	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SRT 1720 dihydrochloride[925434-55-5(free base)] 是 SIRT1 (EC1.5: 0.16 μM) 的选择性激活剂，对 SIRT2 (EC1.5: 37 μM) 和 SIRT3 (EC1.5: 300 μM) 的活性较低。
T77653	Z26395438	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Z26395438 是一种 IC50 值为 1.6 μM 的 Sirtuin-1 的抑制剂。
T6790	BMS-911543 BMS911543	Tyrosine Kinases; Histone Methyltransferase; JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	BMS-911543 是一种选择性 JAK2抑制剂，IC50值为 1.1 nM，对 JAK1、JAK3 和 TYK2 的选择性相对较弱，IC50值分别为 75、360 和 66 nM。
T2506	AZD-5438 AZD5438	CDK	Cell Cycle/Checkpoint
	AZD-5438 有效抑制 CDK1,CDK2,CDK9，IC50值分别为 16 nM, 6 nM, 20 nM，但它对 GSK3β，CDK5，CDK6 的抑制作用较弱。
T30517	BMS-354326 BMS354326,BMS 354326,CHEMBL306448,BDBM50144532
	BMS-354326 is a bio-active chemical.
T34571	SCH 54388 W 873,SCH54388,W-873,SCH-54388,BRN 3051738
	SCH 54388 is a biochemical.
T33261	MDK-5432 AMPA stabilizer (R,R)-2a,MDK 5432
	MDK-5432, also known as AMPA stabilizer (R,R)-2a, is the most potent AMPA stabilizer.
T70420	PHA 543613 hydrochloride
	PHA-543613 hydrochloride acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.
T26148	RU 25434 RU-25434,RU25434
	RU 25434 is a semi-synthetic aminoglycoside antibiotic.
T33952	PF-1543 PF1543
	PF-1543 is a bio-active chemical.
T24036	WJ35435 WJ 35435,WJ-35435
	WJ35435 is a histone deacetylase and topoisomerase I dual inhibitor.
T23354	SID 7969543	Others	Others
	Selective steroidogenic factor-1 (SF-1, NR5A1) inhibitor
T37480	NPC-15437 (hydrochloride)
	NPC-15437 (盐酸盐) 是一种 PKC 的选择性抑制剂，与酶的调节域相互作用。
T31042	CP-195543 UNII-YB1F0V77MK,CP 195543
	CP-195543 is an effective leukotriene B4 antagonist for the treatment of inflammatory diseases.
T71579	GOE-5438
	GOE-5438 is a calcium antagonist that has been shown to inhibit the excitation and contraction of single cardiomyocytes.
T62440	TCMDC-125431
	TCMDC-125431 是一种新型的疟原虫钙动力学抑制剂，而对血红素结晶的抑制作用较低。
T32463	L 685434 L 685,434,L-685434,L-685,434,L685434,L685,434
	L 685434 is a pseudopeptide that can against HIV protease.
TP2159	Urocortin, rat TFA (171543-83-2 free base) Urocortin (Rattus norvegicus) (TFA),Rat urocortin TFA,Urocortin, rat TFA	Others	Others
	Urocortin, rat TFA is a neuropeptide and a potent endogenous CRFR agonist (Kis: 0.97 nM, 1.5 nM, and 13 nM for mouse CRF2β, rat CRF2α, and human CRF1).
T11403L	Gln-AMS TFA (209543-57-7 free base) Gln-AMS TFA	Others	Others
	Gln-AMS(TFA) inhibits glutaminyl-tRNA synthetase (GlnRS) with a Ki of 1.32 μM. Gln-AMS (TFA) is a type Ia aminoacyl-tRNA synthetase (AARS) inhibitor.
T30992	CN009543V CN 009543V,CN-009543V
	CN009543V is an enhancer of tyrosine phosphorylation of EGFR via downstream signaling pathways.
T27485	GSK-625433
	GSK-625433, a homochiral inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase, has the ability to inhibit the polymerase of both HCV genotypes 1a and 1b.
T11649	INCB054329 Racemate	Others	Others
	INCB054329 Racemate is an inhibitor of BET protein.
T11910	LY285434	Others	Others
	LY285434 is a suitable angiotensin II receptor antagonist.
T24361	L 754394 L754394,L-754,394,L 754,394,L-754394,L754,394
	L 754394 is an effective and specific inhibitor of the HIV-1 protease.
T25826	MMV024101 MMV-024101,TCMDC 134293,TCMDC134293,TCMDC-134293,MMV 024101
	MMV024101 is a PI4K inhibitor. MMV024101 exhibits submicromolar potency against P. falciparum NF54 (IC50 =543 nM), low aqueous solubility (<5 μM), and rapid clearance by mouse liver microsomes with only 2% of parent compound remaining after 30 min of incu
T75381	Bodipy TMR-X muscimol
	Bodipy TMR-X muscimol为标记有Bodipy的Muscimol（Ex=543 nm, Em=572 nm），是GABAA受体的激动剂。该化合物适用于可视化可逆脑失活的扩散研究。
T37472	TAMRA-Amyloid-β (1-42) Peptide (trifluoroacetate salt)
	TAMRA-Amyloid-β (1-42) peptide is a fluorescently labeled peptide. Amyloid-β (1-42) (Aβ42) is a neurotoxic 42-residue protein fragment found in amyloid plaques in postmortem cerebral cortex from patients with Alzheimer's disease. Aggregation of Aβ42 results in the formation of neurotoxic fibrils or globular oligomers. TAMRA-Amyloid-β (1-42) peptide is a labeled form of Aβ42 containing carboxytetramethyl rhodamine (TAMRA), which displays excitation/emission maxima of 543/572 nm, respectively.
T36836	(4′-Hydroxy)phenoxybenzoic Acid
	(4′-Hydroxy)phenoxybenzoic acid is a pyrethroid insecticide metabolite.1,2 1.Akhtar, M.H., Mahadevan, S., and Russell, F.Cleavage of 3-phenoxybenzoic acid by chicken microsomal preparationsJ. Environ. Sci. Health B.28(5)527-543(1993) 2.Maloney, S.E., Maule, A., and Smith, A.R.Microbial transformation of the pyrethroid insecticides: Permethrin, deltamethrin, fastac, fenvalerate, and fluvalinateAppl. Environ. Microbiol.54(11)2874-2876(1988)

化合物

Cat.No: T15143

Synonym: XR-543

Target: Others, Potassium Channel

PF-543 hydrochloride

Cat.No: T8840

Synonym: PF-543

Target: Apoptosis, S1P Receptor, Autophagy, LPL Receptor

YM-543 trimethylamine

Cat.No: T29188

Synonym: ASP 543,ASP-543,ASP543

Cat.No: T6085

Synonym: Sphingosine Kinase 1 Inhibitor II,PF 543

Target: Apoptosis, S1P Receptor, Autophagy, LPL Receptor

YM-543 choline

Cat.No: T70390

PF-543 Citrate

Cat.No: T12436

Synonym: Sphingosine Kinase 1 Inhibitor II Citrate

Target: S1P Receptor

Collagen type IV alpha1 (531-543)

Cat.No: TP2452

Synonym: Hep III peptide,Gefyfdlrlkgdk

YM543 free base

Cat.No: T68922

Varlitinib Tosylate

Cat.No: T20954

Synonym: Varlitinib-Tosylate,ARRY-334543 Tosylate,ARRY-543 Tosylate

GAD65 (524-543)

Cat.No: T82354

Cat.No: T21919

Target: Apoptosis

Cat.No: T70389

Cat.No: T50082

Target: Chloride channel

Cat.No: T21712

Target: Others, Guanylate cyclase

GW 284543 hydrochloride

Cat.No: T7742

Target: MEK

Cat.No: T22345

Synonym: INCB-054329,INCB-54329,INCB-54329

Target: Epigenetic Reader Domain

Org 25543 hydrochloride

Cat.No: T22126

Target: GlyT

Cat.No: T23145

Target: Others, AChR

Cat.No: T10783

Target: PPAR

Cat.No: T7610

Synonym: UNC10225170

Target: MEK

SRT 1720 dihydrochloride[925434-55-5(free base)]

Cat.No: T5124

Target: Sirtuin

Cat.No: T77653

Target: Sirtuin

Cat.No: T6790

Synonym: BMS911543

Target: Tyrosine Kinases, Histone Methyltransferase, JAK

Cat.No: T2506

Synonym: AZD5438

Target: CDK

Cat.No: T30517

Synonym: BMS354326,BMS 354326,CHEMBL306448,BDBM50144532

Cat.No: T34571

Synonym: W 873,SCH54388,W-873,SCH-54388,BRN 3051738

Cat.No: T33261

Synonym: AMPA stabilizer (R,R)-2a,MDK 5432

PHA 543613 hydrochloride

Cat.No: T70420

Cat.No: T26148

Synonym: RU-25434,RU25434

Cat.No: T33952

Synonym: PF1543

Cat.No: T24036

Synonym: WJ 35435,WJ-35435

Cat.No: T23354

Target: Others

NPC-15437 (hydrochloride)

Cat.No: T37480

Cat.No: T31042

Synonym: UNII-YB1F0V77MK,CP 195543

Cat.No: T71579

Cat.No: T62440

Cat.No: T32463

Synonym: L 685,434,L-685434,L-685,434,L685434,L685,434

Urocortin, rat TFA (171543-83-2 free base)

Cat.No: TP2159

Synonym: Urocortin (Rattus norvegicus) (TFA),Rat urocortin TFA,Urocortin, rat TFA

Target: Others

Gln-AMS TFA (209543-57-7 free base)

Cat.No: T11403L

Synonym: Gln-AMS TFA

Target: Others

Cat.No: T30992

Synonym: CN 009543V,CN-009543V

Cat.No: T27485

INCB054329 Racemate

Cat.No: T11649

Target: Others

Cat.No: T11910

Target: Others

Cat.No: T24361

Synonym: L754394,L-754,394,L 754,394,L-754394,L754,394

Cat.No: T25826

Synonym: MMV-024101,TCMDC 134293,TCMDC134293,TCMDC-134293,MMV 024101

Bodipy TMR-X muscimol

Cat.No: T75381

TAMRA-Amyloid-β (1-42) Peptide (trifluoroacetate salt)

Cat.No: T37472

(4′-Hydroxy)phenoxybenzoic Acid

Cat.No: T36836

Cat. No.	Product Name	Target	Signaling Pathways
TN1270	LPRP-Et-97543 (3R)-5,7-Dihydroxy-6-methyl-3-(4'-hydroxybenzyl)chroman-4-one	Others	Others
	(3R)-5,7-Dihydroxy-6-methyl-3-(4'-hydroxybenzyl)chroman-4-one is a natural product

天然产物

Cat.No: TN1270

Synonym: (3R)-5,7-Dihydroxy-6-methyl-3-(4'-hydroxybenzyl)chroman-4-one

Target: Others

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