86
12
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9214 |
ELOVL6-IN-1
|
Others | Others |
ELOVL6-IN-1 是一种选择性 ELOVL6抑制剂,口服具有活性。它对丙二酰辅酶 a (Ki:994 nM) 和对棕榈酰辅酶 a 具有非竞争性抑制 ELOVL6 作用。它能够剂量依赖性的一种小鼠 ELOVL6(IC50:0.350 μM)。 | |||
T22748 |
DQP 1105
|
NMDAR | Neuroscience |
DQP 1105 是一种高效非竞争性NMDA 受体拮抗剂。DQP-1105 抑制含有 GluN2C (IC50:7.0 Μm) 和 GluN2D (IC50:2.7 Μm) 的受体 。 IC50值至少比重组 GluN2B-、GluN2A-、GluA1- 或 GluK2 受体低 50 倍。 | |||
T2013 |
Ponalrestat
|
Reductase | Endocrinology/Hormones; Metabolism |
Ponalrestat 是一种口服有效的,选择性的和非竞争性的醛糖还原酶抑制剂,对 ALR2选择性选择性较高,Ki 为 7.7 nM, 对 ALR1 的选择性较弱,Ki 为 60 μM。Ponalrestat 抑制葡萄糖向山梨糖醇的转化。 | |||
T12103 |
MR-L2
|
PDE | Metabolism |
MR-L2 是可逆的、非竞争性的长型异构体磷酸二酯酶 -4激活剂,可以激活代表性的 PDE4 长型异构体 (PDE4A4、PDE4B1、PDE4C3、PDE4D5)。它可抑制 PGE2- 诱导的 MDCK 细胞囊肿形成,其EC50=1.2 µM。 | |||
T11696 |
Ivachtin
Caspase-3 Inhibitor VII |
Caspase | Apoptosis; Proteases/Proteasome |
Ivachtin (Caspase-3 Inhibitor VII) 是一种非肽,非竞争性和可逆的caspase-3抑制剂,IC50为 23 nM。它是其余胱天蛋白酶的适度抑制剂。 | |||
T8461 |
SKI V
|
Apoptosis; PI3K; S1P Receptor | Apoptosis; GPCR/G Protein; PI3K/Akt/mTOR signaling |
SKI V 是一种非竞争性非脂质鞘氨醇激酶抑制剂,对 GST-hSK 的IC50为 2 μM。 它减少有丝分裂的第二信使鞘氨醇-1-磷酸的形成,可诱导细胞凋亡并具有抗肿瘤活性。它还抑制PI3K,对 hPI3k 的IC50为 6 μM。 | |||
T2694 |
KN-62
|
CaMK; P2X Receptor; Autophagy | Autophagy; Membrane transporter/Ion channel; Neuroscience |
KN-62 是一种选择性的、可逆的钙调蛋白依赖性蛋白激酶 II (CaMK-II) 抑制剂,直接与 CaMK-II 酶的钙调蛋白结合位点结合,对大鼠脑 CaMK-II 的IC50值为 0.9 μM。它是非竞争性的P2X7受体拮抗剂,IC50约为 15 nM。 | |||
T6259 |
Dizocilpine
地佐环平,MK-801 |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
Dizocilpine (MK-801) 是一种选择性非竞争性NMDA 受体拮抗剂,Kd=37.2 nM,是一种抗惊厥剂。它通过与 NMDA 相关离子通道内的一个位点结合而起作用,从而阻止 Ca2+的流动。 | |||
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。 | |||
T4190 |
Ticlopidine
PCR 5332,Ticlid,噻氯匹定 |
ATPase; Adiponectin receptor | GPCR/G Protein; Membrane transporter/Ion channel |
Ticlopidine (PCR 5332) 是抗血栓前药。它是CYP2C19人肝细胞色素的抑制剂,抑制 CYP2C9 及 CYP3A4。他是变构CD39的非竞争性抑制剂,能够阻断 NTPDase 同工酶,对NTPDase2和NTPDase3的IC50分别为 170 µM 和 149 µM。 | |||
T3320 |
Dizocilpine Maleate
(+)-Mk-801 Hydrogen Maleate,MK 801,地卓亚平马来酸盐,Dizocilpine hydrogen maleate,地佐环平马来酸盐,(+)-MK 801 maleate,(+)-MK 801 (Maleate) |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
Dizocilpine Maleate (MK 801) 是一种选择性和非竞争性的 NMDA 受体拮抗剂,Kd 值为 37.2 nM。它用于治疗 NMDA 受体可能发挥重要作用的多种神经退行性疾病或疾病。 | |||
T1979 |
AVN-944
VX-944 |
Dehydrogenase | Metabolism |
AVN-944 (VX-944) 是一种选择性的、非竞争性 IMPDH 抑制剂,对IMPDH1和IMPDH2的Ki=为6-10nM。 | |||
T3444 |
Merimepodib
美泊地布,VX-497,VI-21497 |
Dehydrogenase; Antiviral; HCV Protease; HBV | Immunology/Inflammation; Metabolism; Microbiology/Virology; Proteases/Proteasome |
Merimepodib (VX-497) 是一种新型非竞争性肌苷一磷酸脱氢酶抑制剂,具有广谱抗病毒活性。 | |||
T23353 |
(E/Z)-SIB-1893
SIB 1893 |
Others; GluR | Neuroscience; Others |
(E/Z)-SIB-1893 (SIB 1893)是 (E)-SIB-1893 和 (Z)-SIB-1893 的消旋体。(E)-SIB-1893 是一种选择性的、非竞争性的 mGluR5 拮抗剂,具有抗惊厥活性 。 | |||
T22425 |
Sevoflurane
七氟烷,Fluoromethyl |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Sevoflurane (Fluoromethyl) 是一种 5-HT3 受体的非竞争性抑制剂,是一种低溶性吸入麻醉剂。 | |||
TP1888L1 |
[Ala113]-MBP (104-118) acetate
|
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
[Ala113]MBP(104-118) acetate 是一种蛋白激酶 C (PKC) 的非竞争性肽抑制剂,IC50 范围为 28-62 μM。 | |||
T3120 |
K858 (Racemic)
K858 Racemic,K858 |
Apoptosis; Kinesin | Apoptosis; Cytoskeletal Signaling |
K858 Racemic (K858) 是一种选择性有丝分裂驱动蛋白 Eg5 抑制剂,以 ATP 非竞争性方式起作用,IC50值为 1.3 μM。 | |||
T8457 |
NPS2390
|
GluR | Neuroscience |
NPS2390 是钙敏感受体抑制剂,也是 mGluR1 和 mGluR5 的非竞争性拮抗剂。 | |||
T22703 |
CYM-5520
CYM 5520 |
S1P Receptor; LPL Receptor | GPCR/G Protein |
CYM-5520 是一种选择性的变构鞘氨醇 1-磷酸受体 2 (S1PR2) 激动剂,EC50为 480 nM。它可以在 S1PR2 受体中与 S1P 结合,可用于骨质疏松症研究。 | |||
T3591 |
URB602
|
Lipase; Antibacterial | Metabolism; Microbiology/Virology |
URB602 是选择性单酰基甘油脂肪酶 (MGL) 抑制剂,非竞争性抑制大鼠脑 MGL,IC50为 28±4 μM。 | |||
T14194 |
β-NETA
α-NETA |
AChE | Neuroscience |
β-NETA(α-NETA) 是胆碱乙酰转移酶(ChA;IC50=76 μM) 和胆碱酯酶 (ChE;IC50=40 µM)的非竞争性抑制剂,对乙酰胆碱酯的作用微弱 (AChE;IC50=1 mM)。 | |||
T28754 |
Sepin-1
Sepin 1,Sepin1,2H-Benzimidazole, 2,2-dimethyl-5-nitro-, 1,3-dioxide |
Others | Others |
Sepin-1 是一种分离酶的非竞争性抑制剂,IC50 为 14.8 µM。 Sepin-1可以通过抑制细胞增殖和诱导细胞凋亡来抑制小鼠和人类癌细胞系乳腺癌异种移植瘤的生长。 | |||
T10852 |
CNS-5161 hydrochloride
CNS 5161A |
NMDAR | Neuroscience |
CNS-5161 hydrochloride (CNS 5161A) 是一种新型 NMDA 离子通道拮抗剂,与 NMDA 受体/离子通道位点相互作用,产生对谷氨酸作用的非竞争性阻断。 | |||
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 | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others |
IMT1B (LDC203974) 是一种特异性的、具有口服活性的、非竞争性的线粒体 RNA 聚合酶 (POLRMT) 别构抑制剂,能够抑制线粒体 DNA (mtDNA) 的表达,具有抗肿瘤活性。 | |||
T14844 |
BX430
|
P2X Receptor; Calcium Channel | Membrane transporter/Ion channel; Metabolism; Neuroscience |
BX430 是一种有效的选择性非竞争性变构人 P2X4 受体通道拮抗剂,IC50 为 0.54 μM。它具有物种特异性,可用于治疗慢性疼痛和心血管疾病。 | |||
T21584 |
CP 465022
|
iGluR | Membrane transporter/Ion channel; Neuroscience |
CP 465022 hydrochloride 是强效的、选择性的AMPA 受体非竞争性拮抗剂,具有抗惊厥活性。CP 465022 hydrochloride 在大鼠皮层神经元中抑制Kainate 诱导的反应 (IC50= 25 nM)。 | |||
T8976 |
PD-089828
|
EGFR; FGFR; PDGFR; Src | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
PD-089828 是受体酪氨酸激酶 FGFR1、PDGFRβ 和 EGFR 的竞争性抑制剂,IC50分别为0.15、1.76 和 5.47 µM。它也是非受体酪氨酸激酶 c-Src 的非竞争性抑制剂,IC50 为 0.18 µM。 | |||
T3483 |
FTIDC
|
GluR | Neuroscience |
FTIDC 是非竞争性和选择性的口服变构代谢型谷氨酸受体 1 拮抗剂,对人 mGluR1a 的IC50为 5.8 nM。 | |||
T12425 |
PF-06424439 methanesulfonate
|
Acyltransferase; Transferase | Metabolism |
PF-06424439 methanesulfonate 是一种口服有效咪唑并吡啶二酰基甘油酰基转移酶 2 (DGAT2)选择性抑制剂,IC50是14 nM。PF-06424439 methanesulfonate 具有缓慢可逆,时间依赖性的特点,其相对于酰基-CoA 底物以非竞争性模式抑制 DGAT2。 | |||
T1220 |
Ethidium bromide
EtBr,Homidium bromide,EB,溴化乙啶 |
AChR | Neuroscience |
Ethidium bromide (EB) 是一种可用作分子生物实验学中的荧光标记(核酸染色),如琼脂糖凝胶电泳。Ethidium bromide 的λEx 为300-360 nm,λEm为590 nm。 | |||
T14884 |
CBR-5884
|
Others; Dehydrogenase | Metabolism; Others |
CBR-5884 是一种磷酸甘油酸脱氢酶抑制剂,IC50为 33 μM。 它抑制癌细胞中的丝氨酸合成,选择性地抑制黑素瘤和乳腺癌细胞系的增殖,对具有高丝氨酸生物合成活性的癌细胞系有选择性毒性。 | |||
T68599 |
Orphenadrine
Orphenadrine (free base) |
Sodium Channel; NMDAR; AChR | Membrane transporter/Ion channel; Neuroscience |
Orphenadrine 是一种非竞争性的 N-甲基-D-天冬氨酸(NMDA)受体拮抗剂,以浓度依赖性方式抑制克隆的 HERG 通道,在 HEK 细胞中产生0.85μM 的 IC。Orphenadrine 是中枢和外周毒蕈碱受体的拮抗剂,通过孔残基 Y652或 F656突变阻断衰减。 Orphenadrine 具有抗痉挛、镇痛和抗胆碱能活性,对在体外和体内对谷氨酸神经毒性具有保护作用。Orphenadrine 对钠离子通道具有抑制作用,可用来治疗帕金森。 | |||
T32033 |
GYKI-46903 HCl
GYKI-46,903,GYKI 46,903,GYKI 46903,GYKI46,903,GYKI-46903,GYKI46903 |
Others | Others |
GYKI-46903 is a noncompetitive 5-HT3 receptor antagonist. | |||
T70467 |
Alinastine
|
Others | Others |
Alinastine is a noncompetitive histamine H1 receptor antagonist. | |||
T25516 |
I-A09
I-A-09,IA 09 |
Others | Others |
I-A09 is a noncompetitive mPTPB inhibitor. | |||
T27452 |
GSK1723980
|
Others | Others |
GSK1723980 is a novel noncompetitive rTbIPMK inhibitor. | |||
T24604 |
PDAT
Propyl Dimethyl Amino Tryptamine |
Others | Others |
PDAT is a noncompetitive Indolethylamine N-methyltransferase inhibitor. | |||
T27674 |
JNJ-27141491
JNJ 27141491 |
Others | Others |
JNJ-27141491 is a potent, noncompetitive antagonist of human CCR2. | |||
T28614 |
RPC425 free base
RPC425,RPC-425,RPC 425 |
Others | Others |
RPC425 is a noncompetitive inhibitors of the Betaine-γ-Aminobutyric Acid Transporter 1 (BGT1). | |||
T13429 |
α-2,3-sialyltransferase-IN-1
Lith-O-Asp analog |
Others | Others |
α-2,3-sialyltransferase-IN-1 is a noncompetitive inhibitor of α-2,3-sialyltransferase(IC50 of 6 μM). | |||
T38068 |
Aptiganel hydrochloride
|
Others | Others |
Potent and noncompetitive NMDA receptor antagonist (IC50 = 36 nM). Exhibits >70-fold selectivity for NMDA receptor over σ receptor. Neuroprotective in a rat model of focal ischemia. | |||
T11171 |
eIF4A3-IN-2
|
Others | Others |
eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 inhibitor with an IC50 of 110 nM. | |||
TQ0233L |
Traxoprodil Mesylate
|
Others | Others |
Traxoprodil Mesylate is a potent noncompetitive N-methyl-D-aspartate (NMDA) receptors antagonist and has selective for the NR2B subunit. | |||
T14774 |
Bragsin1
|
Others | Others |
Bragsin1 is a potent and selective and noncompetitive ArfGEF BRAG2 inhibitor, inhibits Arf GTPase activation(IC50 : 3 μM),and with anti-cancer activity. | |||
T28893 |
SX-517
SX 517 |
Others | Others |
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. | |||
T27604 |
INCB-9471 HCl
INCB 9471,INCB-9471,INCB9471,INCB-009471,INCB 009471,INCB009471 |
Others | Others |
INCB-9471 HCl, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5, has potent inhibitory activity against monocyte migration and HIV-1 infection. | |||
T10552 |
Bitopertin (R enantiomer)
RO4917838 (R enantiomer),RG1678 (R enantiomer),Bitopertin R enantiomer |
GlyT | Neuroscience |
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). | |||
T38050 |
CP-609754
|
Transferase | Metabolism |
CP-609754 是高效的、可逆的法尼基转移酶抑制剂,对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。 | |||
T61430 |
S-2E
|
Others | Others |
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 such as familial hypercholesterolemia and mixed hyperlipidemia [1] [2]. | |||
T80183 |
Muscarinic toxin 7
|
||
Muscarinic toxin 7,一种肽类毒素,特异性地针对毒蕈碱M1受体表现出选择性和非竞争性的拮抗活性。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S2391 |
L-Chicoric Acid
(-)-Chicoric acid,trans-Caffeoyltartaric acid,Chicoric acid,L-菊苣酸,dicaffeoyltartaric acid,菊苣酸 |
Others; HIV Protease | Microbiology/Virology; Others; Proteases/Proteasome |
L-Chicoric Acid (trans-Caffeoyltartaric acid) 是一种二咖啡酰酒石酸,是一种选择性可逆的 HIV-1 整合酶抑制剂,IC50约为 100 nM。它还可抑制 HIV-1 复制。 | |||
T16535 |
Picrotoxinin
|
Chloride channel; GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Picrotoxinin 是一种氯离子通道阻断剂和 GABAA 的非竞争性拮抗剂,对 α1β2γ2L GABAA 的 IC50 为 1.15 μM。 Picrotoxinin 具有惊厥作用。 | |||
T3S2072 |
3-Butylidenephthalide
Butylidene phthalide,n-Butylidenephthalide,丁烯基苯酞,丁烯基苯酞;丁烯基酞内酯 |
Parasite; Glucosidase | Metabolism; Microbiology/Virology |
3-Butylidenephthalide (Butylidene phthalide) 是从 Ligusticum chuanxiongHort 鉴定出的一种邻苯二甲酸酐衍生物,有杀虫活性。 | |||
T3865 |
beta-Eudesmol
β-桉叶醇,Beta-Selinenol,beta-桉叶醇 |
TRP/TRPV Channel; AChR | Membrane transporter/Ion channel; Neuroscience |
beta-Eudesmol (Beta-Selinenol) 是天然的含氧倍半萜烯,可激活hTRPA1,EC50值为 32.5 μM。Beta-Eudesmol 有增加食欲的功效。 | |||
TN1928 |
Methyl rosmarinate
|
MMP; Anti-infection; Tyrosinase | Microbiology/Virology; Proteases/Proteasome |
Methyl rosmarinate 是一种非竞争性 tyrosinase 抑制剂,从 Rabdosia serra 中分离得到的,对蘑菇酪氨酸酶作用的 IC50值为 0.28 mM,也能抑制a-glucosidase。 | |||
T8182 |
Guanfu base A
Guan-fu base A,关附甲素 |
P450; Potassium Channel; HER | Angiogenesis; JAK/STAT signaling; Membrane transporter/Ion channel; Metabolism; Tyrosine Kinase/Adaptors |
Guanfu base A 是一种生物碱,分离自 Aconitum coreanum,是非竞争性 CYP2D6抑制剂,对人肝微粒体 (HLM) 的 Ki 为 1.20 μM,对人重组体 (rCYP2D6) 的 Ki 为 0.37 μM。它也是 CYP2D 的有效竞争抑制剂。它还能抑制 HERG 通道电流。Guan-fu base A 具有抗心律失常的作用。 | |||
TN1544 |
D-Menthol
Menthol,(+)-MENTHOL,D-薄荷醇 |
Calcium Channel; 5-HT Receptor; AChR | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience |
D-Menthol ((+)-MENTHOL) 是药物和商业产品中的一种常见化合物,也是一种流行的香烟添加剂,它可以减弱细胞体和神经突中 α±7 介导的 Ca 2+ 瞬变,表明薄荷醇以非竞争性方式抑制 α±7-nACh 受体. | |||
T2940 |
6-Hydroxyflavone
6-羟基黄酮,6-HF |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
6-Hydroxyflavone (6-HF) 是天然存在的黄酮化合物,具有抗炎作用。它对牛血红蛋白糖基化具有抑制作用。它能激活 AKT、ERK 1/2、JNK 信号通路,有效促进成骨细胞分化。它能抑制 LPS 诱导的 NO 的产生。 | |||
TN7359 |
HU-331
Cannabidiol Hydroxy Quinone |
Others | Others |
Cannabidiol hydroxyquinone (HU-331) is potentially an active metabolite of cannabidiol that could play a role in inducing apoptosis. It functions by inhibiting the ATPase activity of topoisomerase IIα through a noncompetitive mechanism. | |||
T38241 |
2-Aminoimidazole
|
Others | Others |
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 resistance traits. Additionally, 2-Aminoimidazole acts as a weak noncompetitive inhibitor of human arginase I, with a Ki value of 3.6 mM[1][2][3]. | |||
T82241 |
Halichondrin B
|
||
Halichondrin B,源自海绵 Halichondria okadai,为非竞争性Vinca-alkaloid 微管蛋白结合抑制剂,微管蛋白聚合 IC50 值为1.2-1.4 μM,表现出抗肿瘤活性。 | |||
T16011 |
Manumycin A
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
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 selective, competitive inhibitor of |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMIJ-0160 |
Dextrorphan-d3 Tartrate
Dextromethorphan EP Impurity B-d3 Tartrate |
||
Dextrorphan-d3 Tartrate 是 Dextrorphan Tartrate 的氘代化合物。Dextrorphan Tartrate 的 CAS 号为 77-07-6。Dextrorphan tartrate 是一种非竞争性 NMDA 谷氨酸受体拮抗剂。 |