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34

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T39607	NLRP3 modulators 1 NLRP3 modulators 1
	NLRP3 modulators 1 (WO2017184746A1, compound 107) is a potent modulator of NLRP3, capable of agonizing or partially agonizing the activity of NLRP3. This compound proves valuable in investigating conditions, diseases, or disorders where a reduction in LRP3 activity plays a role in the pathology.
T11362	gamma-Secretase Modulators γ-Secretase Modulators,Amyloid-β production inhibitor	Others	Others
	gamma-Secretase Modulators serves as a useful treatment for Alzheimer's disease by inhibiting the production of Amyloid-β. Specifically, it acts as a gamma-Secretase Modulators with an IC50 value.
T38423	CL097 CL097	Reactive Oxygen Species; TLR	Immunology/Inflammation; Metabolism; NF-κB
	CL097 是 TLR7 和 TLR8 的有效激动剂。 CL097 诱导巨噬细胞中的促炎细胞因子和 NADPH 氧化酶引发，从而增加 fMLF 刺激的 ROS 产生。
T7839	Lasofoxifene Tartrate CP-336156,酒石酸拉索昔芬	Estrogen Receptor/ERR	Endocrinology/Hormones
	Lasofoxifene Tartrate (CP-336156) 是一种非甾体类的雌激素受体选择性调节剂 (SERM)。
T27854	LSN2463359 LSN-2463359,LSN 2463359	GluR	Neuroscience
	LSN2463359是 mGlu5受体的正变构调节剂。
T7136	AZD-6280	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	AZD-6280 是一种新型的亚型选择性 GABAAα2/3 受体阳性调节剂，用于治疗广泛性焦虑症。
T67734	MCUF-651	Guanylate cyclase	GPCR/G Protein
	MCUF-651是鸟苷酸环化酶A 受体的正变构调节剂, EC50=0.45 μM。
T8991	BMS986187	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	BMS986187 是一种有效的δ-阿片受体选择性正变构调节剂 (PAM)，其 EC50= 0.03 μM，pKB= 6.02 (~1 μM)。BMS986187 对 μ 受体无明显 PAM 活性 (EC50=3 μM)。
TP1330	Cyclo(RADfK)	Integrin	Cytoskeletal Signaling
	Cyclo(RADfK) 是选择性 α(v)β(3) 整合素配体，广泛用于新血管生成的研究、治疗和诊断。它是 cyclo (-RGDfK-) 的阴性对照， RGD 肽。 RGD 肽是细胞粘附的调节剂，并被整合素家族的几个成员识别。
T3295	1-Methyl-1H-pyrazol-3-amine	Others	Others
	1-Methyl-1H-pyrazol-3-amine 是一种吡唑类化合物。它已被用于合成各种化合物，如药物、染料和聚合物。它也是合成某些药物的重要中间体。它还被用于新药的开发，以及酶抑制剂和受体调节剂的研究。
T37734	AMPA receptor modulator-2	GluR	Neuroscience
	AMPA receptor modulator-2 是 AMPA 受体的有效调节剂，在 TARPγ2 依赖性 AMPA 受体上的pIC50为 10.1。
T11409	GLP-26	HBV	Microbiology/Virology
	GLP-26 是一种HBV 衣壳组装调节剂，抑制 Hep AD38 系统中的 HBV DNA 复制，IC50值为3 nM。在 1 μM 时，使 cccDNA 降低> 90％。它破坏前基因组 RNA 的衣壳化，导致核衣壳解体，并减少 cccDNA 库。
T29124	VU0240382 VU-0240382,VU 0240382
	VU0240382 is a selective positive allosteric modulators of metabotropic glutamate receptor subtype 5.
T26328	VU0455691 VU 0455691,VU-0455691
	VU0455691 is a selective M1 Muscarinic Receptor Allosteric Modulators.
T29125	VU0359516 VU 0359516,VU-0359516
	VU0359516 is a mGluR4 positive allosteric modulators.
T27449	GSK1331268 GSK 1331268,GSK-1331268
	GSK1331268 is a selective, orally bioavailable positive modulators of mGluR2.
T26706	AZ4800 AZ-4800,AZ 4800
	AZD4800 is a gamma secretase modulators.
T29138	VU0463841 VU 0463841,VU-0463841
	VU0463841 is a mGlu5 negative allosteric modulators.
T27448	GSK1331258 GSK 1331258,GSK-1331258
	GSK1331258 is a selective, orally bioavailable positive modulators of mGluR2.
T27496	GSK9772 GSK-9772,GSK 9772
	GSK9772 is a transrepression-selective liver X receptor modulators with anti-inflammatory activity.
T29121	VU0080241 VU-0080241,VU 0080241
	VU0080241 is a positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4).
T29127	VU0361747 VU-0361747,VU 0361747
	VU0361747 is a positive allosteric modulators (PAM) of metabotropic glutamate receptor subtype 5 (mGlu5).
T27289	Etacstil GW 5638,GW-5638,GW5638,DPC974,DPC 974,DPC-974
	GW5638 is a estrogen receptor ligand. GW5638 is a prodrug of its active metabolite GW7604. GW5638 appears to act as an antagonist in these in vitro systems, although in a manner distinct from other known ER modulators. GW5638 is also classified as a pseud
T69525	MIF degrader MD13
	MIF degrader MD13 is involved in protein-protein interactions that play key roles in inflammation and cancer. Current strategies to develop small molecule modulators of MIF functions are mainly restricted to the MIF tautomerase active siteMIF degrader MD13. MD13 also exhibits antiproliferative effect in a 3D tumor spheroid model. In conclusion, we describe the first MIF-directed PROTAC (MD13) as a research tool, which also demonstrates the potential of PROTACs in cancer therapy.
T80471	α-Conotoxin MrIC
	α-Conotoxin MrIC为特异性α7nAChR偏向激动剂，仅针对II型正变构调节剂（例如PNU120596）调控的α7nAChR产生激活作用。该化合物适用于神经系统疾病研究，以及α7nAChR药理特性的探测。
T71262	AZD-8418
	AZD-8418 is an mGlu2 receptor positive allosteric modulators that attenuates nicotine-taking and nicotine-seeking behavior. Acute treatment with AZD8418 (0.37, 1.12, 3.73, 7.46, and 14.92 mg/kg) and AZD8529 (1.75, 5.83, 17.5, and 58.3 mg/kg) deceased nicotine self-administration and had no effect on food-maintained responding. Chronic treatment with AZD8418 attenuated nicotine self-administration, but tolerance to this effect developed quickly. The inhibition of nicotine self-administration by c...
T36421	Immuno-Oncology Screening Library
	The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list ...
T68473	WAY-255348
	WAY-255348 is a potent nonsteroidal progesterone receptor (PR) antagonist. WAY-255348 inhibits the activity of progesterone. WAY-255348 achieves antagonist activity by binding to and subsequently preventing progesterone-induced nuclear accumulation, phosphorylation and promoter interactions of the PR. WAY-255348 bound PR conformation was similar to that of a progesterone agonist-bound PR and distinct from steroidal antagonist-bound PR conformations. WAY-255348 inhibits PR action through a novel ...
T76230	p-fin4
	p-fin4，作为一种针对STEP Phosphatase-GluA2 AMPA受体相互作用的肽抑制剂，具有0.4 μM的Ki值。在东莨菪碱处理的大鼠模型中，p-fin4能够恢复记忆功能，并展现出抗焦虑及抗抑郁效果。该化合物是开发新型认知增强剂和/或行为调节剂的有希望的先导物。
T76229	p3Ysh-3
	p3Ysh-3 是 STEP Phosphatase-GluA2 AMPA 受体相互作用的肽抑制剂，Ki 为 1.09 μM。p3Ysh-3 在东莨菪碱处理的大鼠模型中恢复记忆缺陷并表现出抗焦虑和抗抑郁作用。p3Ysh-3 是一种很有前途的先导化合物，可用于新型认知增强剂和/或行为调节剂。
T36436	Spergualin trihydrochloride
	Spergualin trihydrochloride is a natural product that first identified as an antibiotic from culture filtrates of Bacillus laterosporus BMG162-aF2[1]. Spergualin trihydrochloride derivatives likely acts as Hsp70 modulators[1]. [1]. Srikanth Patury, et al. Pharmacological Targeting of the Hsp70 Chaperone. Curr Top Med Chem. 2009;9(15):1337-51.
T36391	Spiro-Oxanthromicin A
	Spiro-oxanthromicin A is a polyketide that has been found inStreptomyces.1It induces mislocalization of K-RAS in MDCK cells (IC50= 26.7 μM). 1.Salim, A.A., Xiao, X., Cho, K.J., et al.Rare Streptomyces sp. polyketides as modulators of K-Ras localisationOrg. Biomol. Chem.12(27)4872-4878(2014)
T28157	Nephrin
	Nephrin is a cell surface signaling receptor protein that regulates podocyte function and plays a role in β-cell survival signaling; it is a protein necessary for the proper functioning of the renal filtration barrier. Nephrin belongs to a family of highl
T36570	KUS121
	KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It red...

化合物

NLRP3 modulators 1

Cat.No: T39607

Synonym: NLRP3 modulators 1

gamma-Secretase Modulators

Cat.No: T11362

Synonym: γ-Secretase Modulators,Amyloid-β production inhibitor

Target: Others

Cat.No: T38423

Synonym: CL097

Target: Reactive Oxygen Species, TLR

Lasofoxifene Tartrate

Cat.No: T7839

Synonym: CP-336156,酒石酸拉索昔芬

Target: Estrogen Receptor/ERR

Cat.No: T27854

Synonym: LSN-2463359,LSN 2463359

Target: GluR

Cat.No: T7136

Target: GABA Receptor

Cat.No: T67734

Target: Guanylate cyclase

Cat.No: T8991

Target: Opioid Receptor

Cat.No: TP1330

Target: Integrin

1-Methyl-1H-pyrazol-3-amine

Cat.No: T3295

Target: Others

AMPA receptor modulator-2

Cat.No: T37734

Target: GluR

Cat.No: T11409

Target: HBV

Cat.No: T29124

Synonym: VU-0240382,VU 0240382

Cat.No: T26328

Synonym: VU 0455691,VU-0455691

Cat.No: T29125

Synonym: VU 0359516,VU-0359516

Cat.No: T27449

Synonym: GSK 1331268,GSK-1331268

Cat.No: T26706

Synonym: AZ-4800,AZ 4800

Cat.No: T29138

Synonym: VU 0463841,VU-0463841

Cat.No: T27448

Synonym: GSK 1331258,GSK-1331258

Cat.No: T27496

Synonym: GSK-9772,GSK 9772

Cat.No: T29121

Synonym: VU-0080241,VU 0080241

Cat.No: T29127

Synonym: VU-0361747,VU 0361747

Cat.No: T27289

Synonym: GW 5638,GW-5638,GW5638,DPC974,DPC 974,DPC-974

MIF degrader MD13

Cat.No: T69525

α-Conotoxin MrIC

Cat.No: T80471

Cat.No: T71262

Immuno-Oncology Screening Library

Cat.No: T36421

Cat.No: T68473

Cat.No: T76230

Cat.No: T76229

Spergualin trihydrochloride

Cat.No: T36436

Spiro-Oxanthromicin A

Cat.No: T36391

Cat.No: T28157

Cat.No: T36570

Cat. No.	Product Name	Target	Signaling Pathways
T3406	Kuromanin chloride Glucocyanidin chloride,Chrysontemin,矢车菊素-3-O-葡萄糖苷,Chrysontemin chloride,Cyanidin 3-O-glucoside chloride	NF-κB	NF-κB
	Kuromanin chloride (Chrysontemin chloride) 是从桑叶中获得，能够提高血糖浓度、维持脂质代谢平衡，表现出降低肥胖的作用。
T5S2343	Acetylshikonin 乙酰紫草素,Acetyl shikonin	Others; P450; AChE	Metabolism; Neuroscience; Others
	Acetylshikonin 来源于紫草根，具有抗癌、抗炎作用。它是一种 AChE 抑制剂，具有很强的抗凋亡活性。它是一种非选择性的细胞色素 P450抑制剂，对所有 P450 亚型抑制的 IC50值范围为 1.4-4.0 μM。
TN4174	Guajadial	Glucokinase	Metabolism
	Guajadial shows α-glucosidase inhibitory activities significantly and its activity was better than that of Acarbose.Guajadial may act as Selective Estrogen Receptors Modulators (SERMs), therefore holding significant potential for anticancer therapy, it ex
T4S1616	Sanggenon D 桑根酮D,Sanggenone D	NOS; COX; GABA Receptor	Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
	Sanggenone D represents a new scaffold of positive GABAA receptor modulators, it also inhibits COX-2 activity (IC 50 = 73-100 μM). Sanggenone D has anti-inflammatory activity, it can inhibit NO production from lipopolysaccharide (LPS)-induced RAW 264.7 ce
T37219	N-Palmitoyl Glycine
	The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100...

天然产物

Kuromanin chloride

Cat.No: T3406

Synonym: Glucocyanidin chloride,Chrysontemin,矢车菊素-3-O-葡萄糖苷,Chrysontemin chloride,Cyanidin 3-O-glucoside chloride

Target: NF-κB

Cat.No: T5S2343

Synonym: 乙酰紫草素,Acetyl shikonin

Target: Others, P450, AChE

Cat.No: TN4174

Target: Glucokinase

Cat.No: T4S1616

Synonym: 桑根酮D,Sanggenone D

Target: NOS, COX, GABA Receptor

N-Palmitoyl Glycine

Cat.No: T37219

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