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31

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T16967 T-00127_HEV1

PI4K PI3K/Akt/mTOR signaling
T-00127_HEV1 是有效的phosphatidylinositol 4-kinase III beta 抑制剂,IC50为 60 nM
T17260 WWL70

Lipase; MAGL Metabolism
WWL70 是选择性 α/β 水解酶结构域 6 抑制剂,其IC50=70 nM
T2098 A 77-01

A77-01

ALK; TGF-beta/Smad Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
A 77-01 是 TGF-βI 型受体家族 ALK5抑制剂(IC50:25 nM)。
T16530 BF738735

Antiviral; PI4K Immunology/Inflammation; PI3K/Akt/mTOR signaling
BF738735 是有效的磷脂酰肌醇 4-激酶 IIIβ 抑制剂,IC50为 5.7 nM
T1671 Mirabegron

YM178,米拉贝隆

Adrenergic Receptor GPCR/G Protein; Neuroscience
Mirabegron (YM178) 是选择性的肾上腺素受体激动剂,EC50=22.4 nM
T13253 Umibecestat

CNP520

BACE Neuroscience
Umibecestat 是一种β-位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂,对人 BACE-1 和小鼠 BACE-1 的 IC50 分别为 11 nM 和 10 nM,可用于阿尔茨海默病的研究。
T0154 Nebivolol hydrochloride

R 065824 hydrochloride,盐酸奈必洛尔,Nebivolol HCl,R-65824

Apoptosis; Adrenergic Receptor Apoptosis; GPCR/G Protein; Neuroscience
Nebivolol hydrochloride (R 065824 hydrochloride) 是一种β1-肾上腺素受体选择性抑制剂,IC50为0.8 nM
T22694 CRANAD 2

Others Others
CRANAD 2 是一种特异性近红外 (NIR) 荧光探针,可用于检测 Aβ 斑块。它可透过血脑屏障,且对 Aβ 聚集体有高亲和性,其 Kd=38 nM
T1800 GW788388

GW 788388

ALK; TGF-beta/Smad Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
GW788388 是一种 ALK5抑制剂(IC50:18 nM)。它也抑制 TGF-β II 型受体和激活素 II 型受体的活性,但对 BMP II 型受体无影响。
T0277 Metaproterenol hemisulfate

Orciprenaline sulfate,Metaproterenol Sulfate,硫酸奥西那林

Adrenergic Receptor GPCR/G Protein; Neuroscience
Metaproterenol hemisulfate (Orciprenaline sulfate) 是一种 β2-肾上腺素能受体 (β2AR) 激动剂(IC50=68 nM),是一种直接作用的拟交感神经药,具有抗炎活性。
T1527 Gliclazide

格列齐特,S1702,SE1702

Potassium Channel Membrane transporter/Ion channel
Gliclazide (SE1702) 是一种有效的全细胞的 β 细胞 ATP 敏感型钾流阻断剂,IC50为 184 nM,用作降糖药。
T6496 Vactosertib

TEW-7197,EW-7197

ALK; TGF-beta/Smad Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
Vactosertib (EW-7197) 是有效的、具有 ATP 竞争性的、具有口服活性的激活素受体样激酶 5 (ALK5) 抑制剂(IC50:12.9 nM)。它还以纳摩尔浓度抑制 ALK2 和 ALK4 (IC50为 17.3 nM),表现出强大的抗转移活性和抗癌作用。
T6870 L-685458

L-685,458

Apoptosis; Gamma-secretase Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells
L-685458 (L-685,458) 是一种过渡状态模拟 γ-分泌酶抑制剂,抑制淀粉样 β-蛋白前体 γ-分泌酶活性,选择性高于其他检测的天冬氨酸蛋白酶 50-100 倍。它抑制 γ-分泌酶介导的 APP-C99 和 Notch-100 的裂解,可研究阿尔茨海默病和癌症。
T2265 Bimiralisib

5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine,PQR309,PI3K-IN-2

Others; PI3K; S6 Kinase; mTOR MAPK; Others; PI3K/Akt/mTOR signaling
Bimiralisib (PI3K-IN-2) 是一种有效的,可渗透脑的 mTOR/PI3K 抑制剂,是一种 mTORC1和 mTORC2抑制剂。它能够抑制 PI3Kα,PI3Kδ,PI3Kβ,PI3Kγ和 mTOR,IC50分别为 33 nM,451 nM,661 nM,708 nM 和 89 nM
T22245 Arformoterol Tartrate

(R,R)-Formoterol tartrate,酒石酸福莫特罗

Adrenergic Receptor GPCR/G Protein; Neuroscience
Arformoterol Tartrate ((R,R)-Formoterol tartrate) 是一种长效 β2-肾上腺素能受体 (β2-AR) 激动剂,Kd=2.9 nM。它是一种 Formoterol 的 (R,R)-对映异构体,可用于慢性阻塞性肺疾病 (COPD) 的研究。
T6604 Nepicastat hydrochloride

Nepicastat HCl,内匹司他盐酸盐,RS-25560-197 hydrochloride,SYN-117 hydrochloride,Nepicastat (SYN-117) HCl

Hydroxylase Metabolism
Nepicastat hydrochloride (RS-25560-197 hydrochloride) 是一种选择性的,有效的,口服活性的多巴胺 β 羟化酶(dopamine-beta-hydroxylase)抑制剂,对牛和人多巴胺 β 羟化酶的IC50分别为IC50=8.5 nM 和IC50=9 nM。Nepicastat HCl 可以穿过血脑屏障。
T1349 5-Fluorouridine

Others; DNA/RNA Synthesis Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others
5-Fluorouridine 是一种 5-fluorouracil 的代谢物,具有抗癌作用。它对 L1210 细胞的生长具有细胞毒性作用,其作用的 IC50值为 2 nM。它能抑制人结肠癌细胞 rRNA 的合成。
T4978 Sarpogrelate hydrochloride

盐酸沙格雷酯,MCI-9042

5-HT Receptor GPCR/G Protein; Neuroscience
Sarpogrelate hydrochloride (MCI-9042) 是一种选择性5-HT2R 拮抗剂,可用于研究与血栓形成有关的血管疾病,对 5-HT2A、5-HT2B 和 5-HT2C 受体的pKi 值分别为 8.52、6.57 和 7.43。
T0866 Propafenone

Rythmol,普罗帕酮,Propafenonum

Potassium Channel; MRP; Sodium Channel Immunology/Inflammation; Membrane transporter/Ion channel
Propafenone (Propafenonum) 是钠通道阻滞剂,它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ,具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡,从而抑制食管癌增殖。
T63013 Ruboxistaurin

Ruboxistaurin (LY333531) 是一种选择性的、口服具有活力的 PKC beta 抑制剂,其 Ki 值为 2 nM。Ruboxistaurin 以 ATP 依赖性的方式竞争性抑制 PKC beta I (IC50: 4.7 nM)。Ruboxistaurin 能够作用于 PKC beta II (IC50: 5.9 nM)。
T24380 L-796568 free base

L-796568 free base is a β3 adrenergic receptor agonist potentially for the treatment of obesity. L-796568 is a potent full beta(3) agonist (EC50: 3.6 nM). It has 600-fold selectivity over the human beta(1) and beta(2) receptors.
T12467 PI4KIII beta inhibitor 3

PI3K PI3K/Akt/mTOR signaling
PI4KIII beta inhibitor 3 is a novel and high effective inhibitor of PI4KIIIβ (IC50 of 5.7 nM).
T10014 (1α,1'S,4β)-Lanabecestat

(1α,1'S,4β)-AZD3293

Others Others
(1α,1'S,4β)-Lanabecestat is a Beta site APP Cleaving Enzymel (BACE1) inhibitor, and has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively.
T29034 U75302

U 75302,U-75302

U75302 is an antagonist of thymosin beta-4 (TB4) receptor with a Ki value of 159 nM on guinea pig lung membranes.
T27786 L-796568 dihydrochloride

L 796568,L-796568,L796568

L-796568, is a β3 adrenergic receptor agonist. L-796568 is a potent full beta(3) agonist (EC(50) = 3.6 nM, 94% activation) with >600-fold selectivity over the human beta(1) and beta(2) receptors, which also displays good oral bioavailability in several
T11243 Ethyl tosylcarbamate

Others Others
Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877).
T60633 Nepicastat

Nepicastat (SYN117) 是一种选择性的,有效的,口服的多巴胺 β 羟化酶抑制剂,可穿过血脑屏障(BBB)。Nepicastat (SYN117) 对牛和人多巴胺 β 羟化酶产生浓度依赖性抑制作用,IC50值分别为8.5 nM 和 9 nM
T31828 AZD4694

Flutafuranol,AZD 4694,NAV-4694,AZD-4694,NAV 4694,NAV4694

Flutafuranol, also known as AZD 4694 and NAV4694, is a bio-active chemical. AZD4694 shows high affinity for beta-amyloid fibrils in vitro (K(d) = 2.3 +/- 0.3 nM). The fluorine-18 labeled AZD4694 may have potential for PET-visualization of cerebral beta-am
T72261 Metallo-β-lactamase-IN-9

Metallo-β-lactamase-IN-9 (Compound 23) 是一种高效的泛金属-β-内酰胺酶 (MBL) 抑制剂,其对 NDM-1、VIM-1 和 IMP-1 的抑制活性表现在 IC50 值上,分别为 35 nM、269 nM 和 369 nM
T74786 BIBD-124

BIBD-124 通过与淀粉样蛋白 (Aβ) 斑块结合,展现出优异的亲和力,其 IC50 值达到了 9.51 nM。作为一种放射性示踪剂,[18F]BIBD-124 能够针对 Aβ 斑块进行高效的标记。
T36296 BIO5192 hydrate

BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2]. The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days...

化合物

T-00127_HEV1
Cat.No: T16967
Synonym:
Target: PI4K
WWL70
Cat.No: T17260
Synonym:
Target: Lipase, MAGL
A 77-01
Cat.No: T2098
Synonym: A77-01
Target: ALK, TGF-beta/Smad
BF738735
Cat.No: T16530
Synonym:
Target: Antiviral, PI4K
Mirabegron
Cat.No: T1671
Synonym: YM178,米拉贝隆
Target: Adrenergic Receptor
Umibecestat
Cat.No: T13253
Synonym: CNP520
Target: BACE
Nebivolol hydrochloride
Cat.No: T0154
Synonym: R 065824 hydrochloride,盐酸奈必洛尔,Nebivolol HCl,R-65824
Target: Apoptosis, Adrenergic Receptor
CRANAD 2
Cat.No: T22694
Synonym:
Target: Others
GW788388
Cat.No: T1800
Synonym: GW 788388
Target: ALK, TGF-beta/Smad
Metaproterenol hemisulfate
Cat.No: T0277
Synonym: Orciprenaline sulfate,Metaproterenol Sulfate,硫酸奥西那林
Target: Adrenergic Receptor
Gliclazide
Cat.No: T1527
Synonym: 格列齐特,S1702,SE1702
Target: Potassium Channel
Vactosertib
Cat.No: T6496
Synonym: TEW-7197,EW-7197
Target: ALK, TGF-beta/Smad
L-685458
Cat.No: T6870
Synonym: L-685,458
Target: Apoptosis, Gamma-secretase
Bimiralisib
Cat.No: T2265
Synonym: 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine,PQR309,PI3K-IN-2
Target: Others, PI3K, S6 Kinase, mTOR
Arformoterol Tartrate
Cat.No: T22245
Synonym: (R,R)-Formoterol tartrate,酒石酸福莫特罗
Target: Adrenergic Receptor
Nepicastat hydrochloride
Cat.No: T6604
Synonym: Nepicastat HCl,内匹司他盐酸盐,RS-25560-197 hydrochloride,SYN-117 hydrochloride,Nepicastat (SYN-117) HCl
Target: Hydroxylase
5-Fluorouridine
Cat.No: T1349
Synonym:
Target: Others, DNA/RNA Synthesis
Sarpogrelate hydrochloride
Cat.No: T4978
Synonym: 盐酸沙格雷酯,MCI-9042
Target: 5-HT Receptor
Propafenone
Cat.No: T0866
Synonym: Rythmol,普罗帕酮,Propafenonum
Target: Potassium Channel, MRP, Sodium Channel
Ruboxistaurin
Cat.No: T63013
Synonym:
Target:
L-796568 free base
Cat.No: T24380
Synonym:
Target:
PI4KIII beta inhibitor 3
Cat.No: T12467
Synonym:
Target: PI3K
(1α,1'S,4β)-Lanabecestat
Cat.No: T10014
Synonym: (1α,1'S,4β)-AZD3293
Target: Others
U75302
Cat.No: T29034
Synonym: U 75302,U-75302
Target:
L-796568 dihydrochloride
Cat.No: T27786
Synonym: L 796568,L-796568,L796568
Target:
Ethyl tosylcarbamate
Cat.No: T11243
Synonym:
Target: Others
Nepicastat
Cat.No: T60633
Synonym:
Target:
AZD4694
Cat.No: T31828
Synonym: Flutafuranol,AZD 4694,NAV-4694,AZD-4694,NAV 4694,NAV4694
Target:
Metallo-β-lactamase-IN-9
Cat.No: T72261
Synonym:
Target:
BIBD-124
Cat.No: T74786
Synonym:
Target:
BIO5192 hydrate
Cat.No: T36296
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T4721 β-Nicotinamide mononucleotide

β-NM,β烟酰胺单核苷酸,烟酰胺单核苷酸

Others; Endogenous Metabolite Metabolism; Others
β-Nicotinamide mononucleotide (β-NM) 是烟酰胺磷酸核糖转移酶 (NAMPT) 反应的产物。β-nicotinamide mononucleotide 的作用包括其在细胞生化功能、心脏保护、糖尿病、肥胖相关并发症和阿尔茨海默病中的作用。
TJS0341 7-Amino-4-(trifluoromethyl)coumarin

香豆素151,Coumarin 151,AFC,7-氨基-4-(三氟甲基)香豆素

5-HT Receptor GPCR/G Protein; Neuroscience
7-Amino-4-(trifluoromethyl)coumarin (Coumarin 151) 是一种荧光标记物,其激发和发射波长分别为400和500 nm,可用来灵敏的检测蛋白酶。

天然产物

β-Nicotinamide mononucleotide
Cat.No: T4721
Synonym: β-NM,β烟酰胺单核苷酸,烟酰胺单核苷酸
Target: Others, Endogenous Metabolite
7-Amino-4-(trifluoromethyl)coumarin
Cat.No: TJS0341
Synonym: 香豆素151,Coumarin 151,AFC,7-氨基-4-(三氟甲基)香豆素
Target: 5-HT Receptor
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