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198

抑制剂 & 化合物

27

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Cat. No. Product Name Target Signaling Pathways
T8580 Bupranolol

Adrenergic Receptor GPCR/G Protein; Neuroscience
Bupranolol 是竞争性的、口服活性的、非选择性的β-adrenoceptor 拮抗剂,无固有的拟交感神经活性。
T8459 DNQX disodium salt

DNQX Disodium

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
DNQX disodium salt 是一种选择性、强竞争性的非 NMDA 谷氨酸受体 (non-NMDA glutamate receptor) 拮抗剂 (对 AMPA、kainate 和 NMDA 受体的 IC50分别为 0.5、2 和 40 μM),是一种喹恶啉衍生物。
T7304 DNQX

二硝基喹酮,FG 9041

GluR; iGluR Membrane transporter/Ion channel; Neuroscience
DNQX (FG 9041) 是喹恶啉衍生物,是一种选择性和强竞争性的非 NMDA 谷氨酸受体拮抗剂,对 AMPA、kainate 和 NMDA 受体的IC50分别为 0.5、2 和 40 μM。
T1817 GNF-2

GNF2

SARS-CoV; Bcr-Abl Angiogenesis; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors
GNF-2 是一种高选择性的非 ATP 竞争性 Bcr-Abl 抑制剂。 它抑制 Ba/F3.p210 增殖,IC50为 138 nM。
T23524 W-84 dibromide

HDMPPA

AChR Neuroscience
W-84 dibromide (HDMPPA) 是 M2胆碱受体的强变构调节剂,是一种非竞争性毒蕈碱乙酰胆碱受体拮抗剂,具有变构效应。它联合阿托品时,可有效地防止有机磷中毒。它阻碍 [3H]N-甲基东莨菪碱解离,能稳定胆碱能拮抗剂-受体复合物。
T6223 U0126-EtOH

U0126 Ethanol,U0126

Mitophagy; Influenza Virus; MEK; Autophagy Autophagy; MAPK; Microbiology/Virology
U0126-EtOH (U0126 Ethanol) 是一种非 ATP 竞争性的选择性MEK1和MEK2抑制剂,IC50分别为 72 nM 和 58 nM。U0126-EtOH 可抑制自噬和线粒体自噬。
T6893 MK-886

MK886,L 663536

Apoptosis; Leukotriene Receptor; COX; PPAR; FLAP Apoptosis; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
MK-886 (L 663536)是一种细胞可渗透的,具有口服活性的 FLAP (IC50为 30 nM) 和白三烯生物合成 (完整白细胞和人全血中的IC50分别为 3 nM 和 1.1μM) 的抑制剂。它也是一种非竞争性PPARα拮抗剂,可以诱导细胞凋亡。
T10898 Samuraciclib hydrochloride

ICEC0942 hydrochloride,CT7001 hydrochloride

Apoptosis; CDK Apoptosis; Cell Cycle/Checkpoint
Samuraciclib hydrochloride (ICEC0942 hydrochloride) 是一种具有选择性,ATP 竞争性和口服活性的CDK7抑制剂,IC50为 41 nM。它以 GI50值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长,具有抗肿瘤作用。
T10774 CFM-2

iGluR Membrane transporter/Ion channel; Neuroscience
CFM-2, a potent and selective non-competitive antagonist of AMPAR (AMPAR), exhibits anticonvulsant activity across various seizure models.
TP2058L Catestatin acetate

Catestatin acetate(142211-96-9 free base)

Endogenous Metabolite; AChR Metabolism; Neuroscience
Catestatin acetate 是 nAChR 的非竞争性拮抗剂,可抑制儿茶酚胺的释放。 Catestatin acetate 调节心脏功能和血压。
T26645 Aptiganel

CNS 1102,CNS-1102,CNS1102

NMDAR Neuroscience
Aptiganel (CNS-1102) 是一种非竞争性 NMDA 拮抗剂,是一种多肽,可用于研究急性缺血性卒中。
T2362 QNZ46

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
QNZ46 是一种 NR2C/NR2D 选择性 NMDA 受体非竞争性拮抗剂。
T22346 Indomethacin sodium hydrate

吲哚美辛钠,Indometacin Sodium

COX Immunology/Inflammation; Neuroscience
Indomethacin Sodium is the sodium salt of indomethacin, which is a non-selective, competitive, and reversible, inhibitor of cyclooxygenases 1 and 2 with analgesic-antipyretic, anti-inflammatory, and tocolytic effects.
T22692 CPCCOEt

GluR Neuroscience
CPCCOEt 是mGluR1b 的一种低亲和力、选择性、非竞争性和可逆性拮抗剂
T23588 9-CP-Ade Mesylate

9-Cyclopentyladenine monomethanesulfonate,9 CP Ade Mesylate,9CPAde Mesylate

AChR Neuroscience
9-CP-Ade Mesylate (9 CP Ade Mesylate)是一种具有细胞渗透性的、稳定性和非竞争性的腺苷酸环化酶 (adenylate cyclase) 抑制剂。
T2380 BIBR 1532

Apoptosis; Telomerase Apoptosis; DNA Damage/DNA Repair
BIBR 1532 是一种选择性端粒酶非竞争性抑制剂,IC50值为 100 nM。
T12205 Ned 19

Calcium Channel Membrane transporter/Ion channel; Metabolism
Ned 19 is a selective membrane-permeant non competitive antagonist of NAADP and strongly inhibits tumor growth and vascularization as well as lung metastases in mice.
T5053 Eprobemide

LIS 630,依普贝胺

MAO; Monoamine Oxidase Metabolism; Neuroscience
Eprobemide (LIS 630) 是一种非竞争性的、可逆的单胺氧化酶 A 抑制剂。
T14988 CMPD1

MAPK MAPK
CMPD1 是非 ATP 竞争性 p38 MAPK 介导的 MK2磷酸化选择性抑制剂(Ki:330 nM)。
T23048 N20C hydrochloride

盐酸N20C,2-((3,3-diphenylpropyl)amino)acetamide hydrochloride

NMDAR Neuroscience
N20C hydrochloride (2-((3,3-diphenylpropyl)amino)acetamide hydrochloride) 是一种非竞争性 NMDA 受体开放通道阻滞剂。
T7515 MTEP hydrochloride

3-((2-Methyl-1,3-thiazol-4-yl)ethyn-yl)pyridine hydrochloride,3-[2-(2-甲基-4-噻唑基)乙炔基]吡啶盐酸盐,MTEP

GluR Neuroscience
MTEP hydrochloride (MTEP) 是非竞争性的mGlu5拮抗剂,IC50和Ki 分别为 5 和16 nM,有抗帕金森病样作用。
T6083 AZD8330

ARRY-424704,ARRY-704

ERK; MEK MAPK
AZD8330 (ARRY-704) 是非竞争性的 MEK1/MEK2抑制剂,IC50为 7 nM。
T6636 Refametinib

BAY 86-97661,瑞法替尼//瑞美替尼,BAY 869766,RDEA119

MEK MAPK
Refametinib (RDEA119) 是可口服的、非 ATP 竞争和选择性的 MEK1/MEK2变构抑制剂,IC50分别为 19 和 47 nM。
T25276 Crilvastatin

PMD387,PMD 387,PMD-387

HMG-CoA Reductase Metabolism
Crilvastatin (PMD 387) 是一种新型非竞争性羟甲基戊二酰辅酶 A 还原酶抑制剂,具有降胆固醇活性,可抑制遗传性高胆固醇血症大鼠的胆固醇吸收。
T8458 CNQX disodium

iGluR Membrane transporter/Ion channel; Neuroscience
CNQX disodium 是一种有效的、竞争性的 AMPA /海藻酸酯受体 (AMPA/kainate receptor) 拮抗剂,IC50分别为 0.3 μM 和 1.5 μM。它能够阻止大鼠恐惧增强的表达,是一种竞争性的非 NMDA 受体拮抗剂。
T8685 SP-146

Aurora Kinase Cell Cycle/Checkpoint; Chromatin/Epigenetic
SP-146 是一种选择性、有效且非 ATP 竞争性的 Aurora B 抑制剂(IC50:0.316 nM)。
T24906L Tuna AI acetate

Angiotensin-converting Enzyme (ACE) Metabolism
Tuna AI acetate 是一种源自金枪鱼肌肉的非竞争性血管紧张素转换酶 (ACE) 抑制剂。
T6546 IPA-3

IPA3,IPA 3

PAK Cytoskeletal Signaling
IPA-3 是一种选择性的非 ATP 竞争性 Pak1 抑制剂,IC50 为 2.5 μM。
T3067 Tideglusib

NP-12,NP031112

GSK-3 PI3K/Akt/mTOR signaling; Stem Cells
Tideglusib (NP031112) 是不可逆的 GSK-3抑制剂,能够抑制 GSK-3βWT (IC50:5 nM) 和 GSK-3βC199A (IC50:60 nM)。
T0245 RS 61443

RS61443,吗替麦考酚酯,Mycophenolate mofetil,TM-MMF

Dehydrogenase Metabolism
RS 61443 (Mycophenolate mofetil) 是一种免疫抑制剂,一种非竞争性、选择性和可逆的肌苷一磷酸脱氢酶 (IMPDH) 抑制剂。
T6287 Tariquidar

XR9576,他立喹达

P-gp Membrane transporter/Ion channel; Neuroscience
Tariquidar (XR9576) 是一种特异性有效的P-糖蛋白抑制剂,Kd 为 5.1 nM。
T4354 KPT9274

KPT-9274,KPT 9274,PAK4-IN-1

NAMPT; PAK Cytoskeletal Signaling; Metabolism
KPT9274 (PAK4-IN-1) 是一种非竞争性的 PAK4 和 NAMPT 双重抑制剂(IC50= ~120 nM)。它是一种口服生物可利用的小分子。
T2443 CI-1040

PD 184352

Apoptosis; MEK Apoptosis; MAPK
CI-1040 (PD 184352) 是一种有口服活性的高度特异性MEK 小分子抑制剂,对 MEK1 的IC50值为 17 nM 。
T21152 Ac-Phe-NH2

Ac-Phe NH2,Ac Phe NH2,乙酰基苯甲酰胺,Ac Phe-NH2

Others Others
Ac-Phe-NH2 是一种非竞争性多聚泛素链延长抑制剂,Ki 值为 8 ± 1.2 mM。
T15301 Fluspirilene

Redeptin,R 6218

Calcium Channel Membrane transporter/Ion channel; Metabolism
Fluspirilene (R 6218) 是一种非竞争性 L 型钙通道拮抗剂(IC50:0.03 μM)。Fluspirilene 是一种长效抗精神病类疾病的化合物,用于治疗精神分裂症。
T26520 ABP688

ABP-688,ABP 688

GluR Neuroscience
ABP688 是一种非竞争性和选择性的 mGluR5 拮抗剂 (Ki = 1.7 nM)。 ABP688 可用作临床成像的 PET 示踪剂。
T2463 ML141

CID-2950007

Apoptosis; CDK; Ras Apoptosis; Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
ML141 (CID-2950007) 是一种高效变构,选择性可逆的 Cdc42 GTPase 非竞争性抑制剂,IC50值为200 nM。它抑制 Cdc42 野生型和 Cdc42 Q61L 突变体。
T7178 CNQX

FG9065,6-氰基-7-硝基喹喔啉-2,3-二酮

GluR; iGluR Membrane transporter/Ion channel; Neuroscience
CNQX (FG9065) 是一种竞争性、非 NMDA 谷氨酸受体拮抗剂,对 AMPA 和红藻氨酸受体的IC50分别为 0.3 和 1.5 μM。
T16964 SYM2206

SYM-2206,SYM 2206

Sodium Channel; iGluR Membrane transporter/Ion channel; Neuroscience
SYM2206 是一种亲和力较低的非竞争性 AMPA 受体拮抗剂,IC50 值为 1.6 μM。SYM2206 具有抗癌活性,可阻断 Nav1.6 介导的持续电流,降低胰腺癌细胞的存活率。
T15387 GLP-1R Antagonist 1

Glucagon Receptor GPCR/G Protein
GLP-1R Antagonist 1 (compound 5d) 是口服有效的、能透过中枢神经系统的,胰高血糖素样肽 1 受体 (GLP-1R) 的非竞争性抑制,其 IC50 值为 650 nM。
T77679 hPL-IN-2

Others Others
hPL-IN-2 是一种具有有效性、可逆性、和非竞争性胰脂肪酶 (Pancreatic lipase) 抑制剂 (IC50: 1.63 μM),可用于研究肥胖相关疾病。
T16560 Poloxin

PLK Cell Cycle/Checkpoint
Poloxin 是一种 polo 样激酶 1 的 ATP 非竞争性抑制剂,靶向 polo-box 结构域,IC50值约为 4.8 μM。
T4442 MK2-IN-1 hydrochloride

MK2 Inhibitor,MK 25

MAPK MAPK
MK2-IN-1 hydrochloride (MK 25) 是一种高效的选择性 MAPKAPK2(MK2)激酶抑制剂,其 IC50值为0.11uM。
T78554 Tyrosinase-IN-12

Tyrosinase Proteases/Proteasome
Tyrosinase-IN-12(Non-competitive tyrosinase inhibitor) 是一种有效的非竞争性酪氨酸酶抑制剂,IC50 值为 49.33 ± 2.64 µM,Ki 值为31.25 ± 0.25 µM。Tyrosinase-IN-12 具有显著的抗氧化和自由基清除活性,减少活性氧 (ROS) 的产生(IC50:25.39 ± 0.77 µM)。Tyrosinase-IN-12 可用于研究食品和水果中物质的褐变。
T9773 Thioquinapiperifil dihydrochloride

KF-31327

PDE Metabolism
Thioquinapiperifil dihydrochloride 是一种磷酸二酯酶(PDE-5)抑制剂(IC50: 0.074 nM),具有有效性、选择性和非竞争性,可用于研究性成熟。
T2497 MPEP hydrochloride

GluR Neuroscience
MPEP Hydrochloride 是一种有效且高度特异性的非竞争性拮抗剂,作用于 mGlu5 受体亚型,IC50为 36 nM,有抗焦虑和抗抑郁活性。
TP1887L1 [Ala107]-MBP (104-118) acetate

[Ala107]-MBP (104-118) acetate(99026-77-4 free base)

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
[Ala107]-MBP (104-118) acetate ([Ala107]-MBP )(99026-77-4 free base) 是牛髓鞘碱性蛋白 (MBP) 的合成肽类似物。 PKC 的非竞争性抑制剂 (IC50 = 46 - 145 mM)。
T10066 2',5'-Dideoxyadenosine

Adenylyl cyclase; Adrenergic Receptor; AChR GPCR/G Protein; Neuroscience
2',5'-Dideoxyadenosine 是一种非竞争性腺苷酸环化酶抑制剂,通过结合 P 位点,IC50为 3 µM。它是核苷类似物,在心脏中发挥强大的抗肾上腺素作用。
T7157 XY1

N-2-萘基-N'-[2-氧代-2-(1-吡咯烷基)乙基]脲

Histone Methyltransferase Chromatin/Epigenetic
XY1是 SGC707的类似物,SGC707是选择性PRMT3抑制剂,IC50值为31 nM。
T73331 GSK3-IN-3

Mitophagy; GSK-3 Autophagy; PI3K/Akt/mTOR signaling; Stem Cells
GSK3-IN-3 是一种线粒体自噬 (mitophagy) 诱导剂和GSK-3 抑制剂(IC50 : 3.01 μM),可诱导帕金依赖性线粒体自噬。 GSK3-IN-3 具有非 ATP 和非底物竞争性,对 6-OHDA 有神经保护作用。

化合物

Bupranolol
Cat.No: T8580
Synonym:
Target: Adrenergic Receptor
DNQX disodium salt
Cat.No: T8459
Synonym: DNQX Disodium
Target: NMDAR, iGluR
DNQX
Cat.No: T7304
Synonym: 二硝基喹酮,FG 9041
Target: GluR, iGluR
GNF-2
Cat.No: T1817
Synonym: GNF2
Target: SARS-CoV, Bcr-Abl
W-84 dibromide
Cat.No: T23524
Synonym: HDMPPA
Target: AChR
U0126-EtOH
Cat.No: T6223
Synonym: U0126 Ethanol,U0126
Target: Mitophagy, Influenza Virus, MEK, Autophagy
MK-886
Cat.No: T6893
Synonym: MK886,L 663536
Target: Apoptosis, Leukotriene Receptor, COX, PPAR, FLAP
Samuraciclib hydrochloride
Cat.No: T10898
Synonym: ICEC0942 hydrochloride,CT7001 hydrochloride
Target: Apoptosis, CDK
CFM-2
Cat.No: T10774
Synonym:
Target: iGluR
Catestatin acetate
Cat.No: TP2058L
Synonym: Catestatin acetate(142211-96-9 free base)
Target: Endogenous Metabolite, AChR
Aptiganel
Cat.No: T26645
Synonym: CNS 1102,CNS-1102,CNS1102
Target: NMDAR
QNZ46
Cat.No: T2362
Synonym:
Target: NMDAR, iGluR
Indomethacin sodium hydrate
Cat.No: T22346
Synonym: 吲哚美辛钠,Indometacin Sodium
Target: COX
CPCCOEt
Cat.No: T22692
Synonym:
Target: GluR
9-CP-Ade Mesylate
Cat.No: T23588
Synonym: 9-Cyclopentyladenine monomethanesulfonate,9 CP Ade Mesylate,9CPAde Mesylate
Target: AChR
BIBR 1532
Cat.No: T2380
Synonym:
Target: Apoptosis, Telomerase
Ned 19
Cat.No: T12205
Synonym:
Target: Calcium Channel
Eprobemide
Cat.No: T5053
Synonym: LIS 630,依普贝胺
Target: MAO, Monoamine Oxidase
CMPD1
Cat.No: T14988
Synonym:
Target: MAPK
N20C hydrochloride
Cat.No: T23048
Synonym: 盐酸N20C,2-((3,3-diphenylpropyl)amino)acetamide hydrochloride
Target: NMDAR
MTEP hydrochloride
Cat.No: T7515
Synonym: 3-((2-Methyl-1,3-thiazol-4-yl)ethyn-yl)pyridine hydrochloride,3-[2-(2-甲基-4-噻唑基)乙炔基]吡啶盐酸盐,MTEP
Target: GluR
AZD8330
Cat.No: T6083
Synonym: ARRY-424704,ARRY-704
Target: ERK, MEK
Refametinib
Cat.No: T6636
Synonym: BAY 86-97661,瑞法替尼//瑞美替尼,BAY 869766,RDEA119
Target: MEK
Crilvastatin
Cat.No: T25276
Synonym: PMD387,PMD 387,PMD-387
Target: HMG-CoA Reductase
CNQX disodium
Cat.No: T8458
Synonym:
Target: iGluR
SP-146
Cat.No: T8685
Synonym:
Target: Aurora Kinase
Tuna AI acetate
Cat.No: T24906L
Synonym:
Target: Angiotensin-converting Enzyme (ACE)
IPA-3
Cat.No: T6546
Synonym: IPA3,IPA 3
Target: PAK
Tideglusib
Cat.No: T3067
Synonym: NP-12,NP031112
Target: GSK-3
RS 61443
Cat.No: T0245
Synonym: RS61443,吗替麦考酚酯,Mycophenolate mofetil,TM-MMF
Target: Dehydrogenase
Tariquidar
Cat.No: T6287
Synonym: XR9576,他立喹达
Target: P-gp
KPT9274
Cat.No: T4354
Synonym: KPT-9274,KPT 9274,PAK4-IN-1
Target: NAMPT, PAK
CI-1040
Cat.No: T2443
Synonym: PD 184352
Target: Apoptosis, MEK
Ac-Phe-NH2
Cat.No: T21152
Synonym: Ac-Phe NH2,Ac Phe NH2,乙酰基苯甲酰胺,Ac Phe-NH2
Target: Others
Fluspirilene
Cat.No: T15301
Synonym: Redeptin,R 6218
Target: Calcium Channel
ABP688
Cat.No: T26520
Synonym: ABP-688,ABP 688
Target: GluR
ML141
Cat.No: T2463
Synonym: CID-2950007
Target: Apoptosis, CDK, Ras
CNQX
Cat.No: T7178
Synonym: FG9065,6-氰基-7-硝基喹喔啉-2,3-二酮
Target: GluR, iGluR
SYM2206
Cat.No: T16964
Synonym: SYM-2206,SYM 2206
Target: Sodium Channel, iGluR
GLP-1R Antagonist 1
Cat.No: T15387
Synonym:
Target: Glucagon Receptor
hPL-IN-2
Cat.No: T77679
Synonym:
Target: Others
Poloxin
Cat.No: T16560
Synonym:
Target: PLK
MK2-IN-1 hydrochloride
Cat.No: T4442
Synonym: MK2 Inhibitor,MK 25
Target: MAPK
Tyrosinase-IN-12
Cat.No: T78554
Synonym:
Target: Tyrosinase
Thioquinapiperifil dihydrochloride
Cat.No: T9773
Synonym: KF-31327
Target: PDE
MPEP hydrochloride
Cat.No: T2497
Synonym:
Target: GluR
[Ala107]-MBP (104-118) acetate
Cat.No: TP1887L1
Synonym: [Ala107]-MBP (104-118) acetate(99026-77-4 free base)
Target: PKC
2',5'-Dideoxyadenosine
Cat.No: T10066
Synonym:
Target: Adenylyl cyclase, Adrenergic Receptor, AChR
XY1
Cat.No: T7157
Synonym: N-2-萘基-N'-[2-氧代-2-(1-吡咯烷基)乙基]脲
Target: Histone Methyltransferase
GSK3-IN-3
Cat.No: T73331
Synonym:
Target: Mitophagy, GSK-3
Cat. No. Product Name Target Signaling Pathways
T11054 DL-Norvaline

2-Aminopentanoic acid,DL-正缬氨酸

Arginase; Endogenous Metabolite Immunology/Inflammation; Metabolism
DL-Norvaline (2-Aminopentanoic acid) 是精氨酸酶的非竞争性抑制剂,是L-norvaline 的代谢物。
T3419 Chelerythrine chloride

白屈菜红碱,盐酸白屈菜红碱

Apoptosis; BCL; PKC; Autophagy Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling
Chelerythrine chloride 是一种可渗透细胞的蛋白激酶 C 抑制剂,对磷酸盐受体具有竞争性,而对 ATP 是非竞争性的。它诱导细胞凋亡和自噬。
T1680 Tolazoline hydrochloride

Imidaline hydrochloride,苯甲唑啉盐酸盐,Imidaline (hydrochloride),Benzidazol hydrochloride,Tolazoline HCl,NSC35110 (hydrochloride)

Adrenergic Receptor GPCR/G Protein; Neuroscience
Tolazoline hydrochloride (NSC35110(hydrochloride)) 是一种 α 肾上腺素受体抑制剂。
T3379 Decanoic Acid

Decoic acid,CAPRIC ACID,Caprynic acid,癸酸

GluR; iGluR Membrane transporter/Ion channel; Neuroscience
Decanoic Acid (Caprynic acid) 是中链甘油三酯中的成分,是非竞争性和可透过血脑屏障的 AMPA 受体抑制剂,具有抗癫痫作用。
TJS0851 Plantagoside

Others Others
Plantagoside 是α-mannosidase 的非竞争性特异性抑制剂(IC50:5 μM),分离自Plantago asiatica 种子中。
T8319 Butyl isobutyl phthalate

ButylIsobutylPhthalate,邻苯二甲酸-1-丁酯-2-异丁酯

Glucosidase Metabolism
Butyl isobutyl phthalate (ButylIsobutylPhthalate) 是一种非竞争性 α-葡萄糖苷酶抑制剂,IC50=38 μM,可以从海带的根状茎中分离得到。它具有降血糖作用,可用于糖尿病相关的研究。
T8044 Ajmalicine

阿吗里新,Lamuran,Delta-Yohimbine,Raubasine,Ajmalicin

Adrenergic Receptor GPCR/G Protein; Neuroscience
Ajmalicine (Raubasine) 是一种有效的抗肾上腺素 (adrenolytic) 剂,优先阻断 α1-肾上腺素受体 (α1-adrenoceptor)。Ajmalicine 是一种可逆性但非竞争性尼古丁受体 (nicotine receptor) 完全抑制剂,IC50 为 72.3 μM。Ajmalicine 还可用于降压、蛇毒,具有镇静活性。
T6680 Staurosporine

Antibiotic AM-2282,星形孢菌素,AM-2282,CGP 41251,星孢菌素

Apoptosis; PKA; Antibacterial; Antibiotic; Src; PKC; Antifungal Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors
Staurosporine (AM-2282) 是一种蛋白激酶抑制剂,对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6/15/2/3/3000 nM),具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。
T25192 Butyrolactone I

Olomoucin,丁酸内酯I

CDK Cell Cycle/Checkpoint
Butyrolactone I (Olomoucin) 是 CDK 和 cdc2 激酶家族的 ATP 竞争性抑制剂。 Butyrolactone I 在非小细胞肺、小细胞肺和前列腺癌细胞系中显示出抗肿瘤作用。
TN4660 Niranthin

Anti-infection; HBV; PAFR; Topoisomerase DNA Damage/DNA Repair; GPCR/G Protein; Microbiology/Virology
Niranthin 是一种木脂素,具有广泛的药理活性。它是L. donovaniIB 拓扑异构酶的非竞争性抑制剂,可用于研究耐药利什曼病的治疗。
TN1343 8-Geranyloxypsoralen

8-香叶草氧基补骨脂素

Anti-infection; P450; BACE Metabolism; Microbiology/Virology; Neuroscience
8-Geranyloxypsoralen 是一种呋喃香豆素,分离自葡萄柚,是 P450 3A4 的有效抑制剂(IC50:3.93 μM)。
T6S0659 Rhynchophylline

钩藤碱,Rhynchophyllin,Rhyncophylline,Mitrinermine,Mitrinermin

Calcium Channel; NF-κB Membrane transporter/Ion channel; Metabolism; NF-κB
Rhynchophylline (Mitrinermine) 是一种生物碱类化合物,从钩藤中分离得到,具有很高的生物活性,被广泛用于抗炎、神经保护等方面的研究。
T0962 L-Hyoscyamine

Daturine,Hyoscyamine,L-莨菪碱,L-天仙子胺

AChR Neuroscience
L-Hyoscyamine (Daturine) 是从山莨菪中提取的一种托烷生物碱,是竞争性的毒蕈碱受体拮抗剂。它是 Atropine 的左旋异构体。
T4S1619 L-Hyoscyamine sulfate

Hyoscyamine sulfate hydrate,Levsin Sulfate,Hyoscyamine Sulphate,硫酸天仙子胺水合物,L-莨菪碱硫酸盐

AChR Neuroscience
L-Hyoscyamine sulfate (Levsin Sulfate) 是来自山莨菪的一种托烷生物碱,是竞争性的毒蕈碱受体拮抗剂。它是 Atropine 的左旋异构体。
TN3013 4,5-Dimethoxycanthin-6-one

Methylnigakinone

P450; Antibacterial; PDE Metabolism; Microbiology/Virology
4,5-Dimethoxycanthin-6-one 从 Picrasma quassioides BENNET (Simaroubaceae)是一种从 Picrasma quassioides BENNET (Simaroubaceae) 中分离得到生物碱。4,5-Dimethoxycanthin-6-one 是一种有效的、非竞争性的 CYP1A2 介导的 phenacetin O-deethylation 抑制剂(IC50 : 1.7 μM, Ki : 2.6 μM),对环磷酸腺苷(cAMP)磷酸二酯酶有很强的抑制作用。4,5-Dimethoxycanthin-6-one 具有抗菌活性,对金黄色葡萄球菌及其耐药菌株有抑制作用。4,5-Dimethoxycanthin-6-one 对肿瘤细胞株 U937 和 HepG2 具有细胞毒性。
T13752 L-(+)-Arabinose

Endogenous Metabolite Metabolism
L-(+)-Arabinose 能够选择性抑制肠道蔗糖酶,并抑制因蔗糖摄入而导致的血浆葡萄糖提高。
T39025 Adenosine 2',5'-diphosphate sodium

Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist with non-selective antagonism at recombinant and human platelet P2X1 receptors.
TN4571 Mirabijalone D

Beta Amyloid Neuroscience
Mirabijalone D is a non-competitive inhibitor based on the Dixon plot.It inhibits Aβ1-42 production by 43.7% in APPSW-N2a cells.
T2S0118 Daurinoline

Calcium Channel; 5-HT Receptor; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
Daurinoline is a non-competitive antagonist, it exerts marked relaxation effect on basilar artery of rabbits through non-competitive antagonism, it would have a protective function on microcirculation of cerebral pia mater, which may be beneficial to relieve cerebral ischemic injury. Daurinoline could significantly reverse noradrenaline induced constriction of pial arterioles and venules, and increase the number of blood vessels which were decreased by noradrenaline.
T8214 Kushenol E

苦参醇E,Flemiphilippinin D

IDO; Indoleamine 2,3-Dioxygenase (IDO) Metabolism
Kushenol E (Flemiphilippinin D) 是一种分离自Sophora flavescens 中的类黄酮,是一种IDO1的非竞争性抑制剂,其IC50=7.7 µM,Ki=为 9.5 µM,具有抗肿瘤特性。
TN3383 α-Amyrin palmitate

alpha-Amyrin palmitate

PKA Tyrosine Kinase/Adaptors
alpha-Amyrin palmitate is antiarthritic in the adjuvant model of arthritis in rats. alpha-Amyrin palmitate is a potent non-competitive inhibitor of chymotrypsin (Ki=6 microM), it also shows weak cytotoxicity against the A2780 human ovarian cancer cell line.
T8306 Epiberberine chloride

表小檗碱氯化物,Epiberberine (chloride),盐酸表小檗碱

Reactive Oxygen Species; Beta-Secretase; BACE; AChR; AChE Immunology/Inflammation; Metabolism; Neuroscience; NF-κB
Epiberberine chloride (Epiberberine (chloride)) 是一种从黄连中得到的生物碱,是一种AChE 和BChE 抑制剂,和非竞争性的BACE1抑制剂。它具有抗氧化作用,能够清除 ONOO-,可用于研究阿尔滋海默症和糖尿病。
TN2517 1,7-Dihydroxy-2,3-dimethoxyxanthone

Others Others
1,7-Dihydroxy-2,3-dimethoxyxanthone may have medicinal use in the management of inflammation, asthma and allergy, it antagonises in a non competitive but, reversible manner the contractions induced by chemical inflammatory mediators in the guinea pig trac
T73202 BChE-IN-11

BChE-IN-11 是一种有效的、选择性的、非竞争性BChE(丁基胆碱酯酶)抑制剂,其IC50为 2.1 μM。BChE-IN-11 可用于阿尔茨海默病 (AD) 的研究。
T75513 BChE-IN-12

BChE-IN-12 (compound 12) 为一种高效BChE非竞争性抑制剂,其IC50值为2.3 μM。该化合物可从白芨(Bletilla striata)中分离提取,适用于阿尔兹海默症(AD)的研究。
T37774 Thielavin A

Thielavin A is a fungal metabolite originally isolated from T. terricola that is related to thielavin B . Thielavin A inhibits COX, blocking both the conversion of arachidonic acid to prostaglandin H2 and the conversion of PGH2 to PGE2 . Thielavin A also inhibits glucose-6-phosphatase in rat liver microsomes (IC50 = 4.6 μM). It is a non-competitive inhibitor of α-glucosidase from S. cerevisiae (IC50 = 23.8 μM; Ki = 27.8 μM).
T69254 Ajmalicine hydrochloride

Raubasine hydrochloride

Ajmalicine (Raubasine) hydrochloride 是一种有效的抗肾上腺素 (adrenolytic) 剂,优先阻断 α1-肾上腺素受体 (α1-adrenoceptor)。Ajmalicine hydrochloride 是一种可逆性但非竞争性尼古丁受体 (nicotine receptor) 完全抑制剂,其 IC50为 72.3 μM。Ajmalicine hydrochloride 还可用于降压、蛇毒,具有镇静活性。

天然产物

DL-Norvaline
Cat.No: T11054
Synonym: 2-Aminopentanoic acid,DL-正缬氨酸
Target: Arginase, Endogenous Metabolite
Chelerythrine chloride
Cat.No: T3419
Synonym: 白屈菜红碱,盐酸白屈菜红碱
Target: Apoptosis, BCL, PKC, Autophagy
Tolazoline hydrochloride
Cat.No: T1680
Synonym: Imidaline hydrochloride,苯甲唑啉盐酸盐,Imidaline (hydrochloride),Benzidazol hydrochloride,Tolazoline HCl,NSC35110 (hydrochloride)
Target: Adrenergic Receptor
Decanoic Acid
Cat.No: T3379
Synonym: Decoic acid,CAPRIC ACID,Caprynic acid,癸酸
Target: GluR, iGluR
Plantagoside
Cat.No: TJS0851
Synonym:
Target: Others
Butyl isobutyl phthalate
Cat.No: T8319
Synonym: ButylIsobutylPhthalate,邻苯二甲酸-1-丁酯-2-异丁酯
Target: Glucosidase
Ajmalicine
Cat.No: T8044
Synonym: 阿吗里新,Lamuran,Delta-Yohimbine,Raubasine,Ajmalicin
Target: Adrenergic Receptor
Staurosporine
Cat.No: T6680
Synonym: Antibiotic AM-2282,星形孢菌素,AM-2282,CGP 41251,星孢菌素
Target: Apoptosis, PKA, Antibacterial, Antibiotic, Src, PKC, Antifungal
Butyrolactone I
Cat.No: T25192
Synonym: Olomoucin,丁酸内酯I
Target: CDK
Niranthin
Cat.No: TN4660
Synonym:
Target: Anti-infection, HBV, PAFR, Topoisomerase
8-Geranyloxypsoralen
Cat.No: TN1343
Synonym: 8-香叶草氧基补骨脂素
Target: Anti-infection, P450, BACE
Rhynchophylline
Cat.No: T6S0659
Synonym: 钩藤碱,Rhynchophyllin,Rhyncophylline,Mitrinermine,Mitrinermin
Target: Calcium Channel, NF-κB
L-Hyoscyamine
Cat.No: T0962
Synonym: Daturine,Hyoscyamine,L-莨菪碱,L-天仙子胺
Target: AChR
L-Hyoscyamine sulfate
Cat.No: T4S1619
Synonym: Hyoscyamine sulfate hydrate,Levsin Sulfate,Hyoscyamine Sulphate,硫酸天仙子胺水合物,L-莨菪碱硫酸盐
Target: AChR
4,5-Dimethoxycanthin-6-one
Cat.No: TN3013
Synonym: Methylnigakinone
Target: P450, Antibacterial, PDE
L-(+)-Arabinose
Cat.No: T13752
Synonym:
Target: Endogenous Metabolite
Adenosine 2',5'-diphosphate sodium
Cat.No: T39025
Synonym:
Target:
Mirabijalone D
Cat.No: TN4571
Synonym:
Target: Beta Amyloid
Daurinoline
Cat.No: T2S0118
Synonym:
Target: Calcium Channel, 5-HT Receptor, Histamine Receptor
Kushenol E
Cat.No: T8214
Synonym: 苦参醇E,Flemiphilippinin D
Target: IDO, Indoleamine 2,3-Dioxygenase (IDO)
α-Amyrin palmitate
Cat.No: TN3383
Synonym: alpha-Amyrin palmitate
Target: PKA
Epiberberine chloride
Cat.No: T8306
Synonym: 表小檗碱氯化物,Epiberberine (chloride),盐酸表小檗碱
Target: Reactive Oxygen Species, Beta-Secretase, BACE, AChR, AChE
1,7-Dihydroxy-2,3-dimethoxyxanthone
Cat.No: TN2517
Synonym:
Target: Others
BChE-IN-11
Cat.No: T73202
Synonym:
Target:
BChE-IN-12
Cat.No: T75513
Synonym:
Target:
Thielavin A
Cat.No: T37774
Synonym:
Target:
Ajmalicine hydrochloride
Cat.No: T69254
Synonym: Raubasine hydrochloride
Target:
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