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23

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
T15758 Linopirdine

利诺吡啶,DuP 996

Potassium Channel; TRP/TRPV Channel Membrane transporter/Ion channel
Linopirdine (DuP 996) 是一种口服有效的,选择性 M 型 K+电流 (IM;Kv7;KCNQ Channels) 抑制剂,IC50为 2.4 μM。Linopirdine 是TRPV1激活剂。Linopirdine 是一种公认的认知增强药物,可增加大鼠脑组织中乙酰胆碱的释放。
T71857 GTP-14564

FLT; Tyrosine Kinases Angiogenesis; Tyrosine Kinase/Adaptors
GTP-14564是一种新型酪氨酸激酶抑制剂,对 wt-FLT3和ITD-FLT3也具有抑制作用。GTP-14564 在 3μ m 处抑制表达 ITD-FLT3 的白细胞介素-3 非依赖性 Ba/F1 的生长,而需要高 30 倍的 GTP-14564 浓度来抑制表达野生型 FLT3 的 Ba/F3 的 FLT3 配体依赖性生长 (wt-FLT3)。
T50077 m-Nisoldipine

3-methyl 5-(2-methylpropyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

Others Others
m-Nisoldipine (3-methyl 5-(2-methylpropyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate) 是一种二氢吡啶类钙通道阻滞剂,尼索地平的衍生物,阻断心脏和平滑肌细胞中的 L-型钙通道,用于治疗高血压和心绞痛。
T27229 E-4177

E4177

E-4177 is an angiotensin type 1 receptor antagonist. In rat adrenal cortex and liver, E4177 competitively inhibited the specific binding of 125I-[Sar1,Ile8]Ang II, with IC50 being (5.2 +/- 1.0) x 10(-8) M for the adrenal cortex and (1.2 +/- 0.3) x 10(-7)
T76885 Sonelokimab

Sonelokimab (ALX 0761; M 1095) 是三价纳米抗体,特异性结合人白介素(IL)-17A、IL-17F及人血清白蛋白VHH,由单价骆驼来源纳米抗体构成,展现于斑块型银屑病研究中的应用潜力。
T79647 VEGFR/PARP-IN-1

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
VEGFR/PARP-IN-1 (Compound 14b) 是一款针对VEGFR和PARP两个靶点的双重抑制剂,其对VEGFR和PARP的IC50值分别为191 nM和60.9 nM。该化合物能够抑制DNA损伤修复机制,诱导apoptosis,并使细胞在G2/M期阻滞。此外,VEGFR/PARP-IN-1对BRCA野生型乳腺癌细胞表现出较强的抗增殖效果,尤其是在MDA-MB-231和MCF-7细胞系上,其IC50值分别为4.1 μM和3.5 μM,是潜在的抗肿瘤和抗转移药物。
T36132 3β-OH-7-Oxocholenic Acid

3β-OH-7-Oxocholenic acid is a bile acid.1 It is also a metabolite of 7β-hydroxy cholesterol in rats. Conjugated forms of 3β-OH-7-oxocholenic acid have been found in the urine of patients with Neimann-Pick disease type C.2,3 |1. Norii, T., Yamaga, N., and Yamasaki, K. Metabolism of 7β-hydroxycholesterol-4-14C in rat. Steroids 15(3), 303-326 (1970).|2. Alvelius, G., Hjalmarson, O., Griffiths, W.J., et al. Identification of unusual 7-oxygenated bile acid sulfates in a patient with Niemann-Pick dise...
T37178 Norhyodeoxycholic Acid

Norhyodeoxycholic acid (NHDCA) is a synthetic bile acid and a derivative of hyodeoxycholic acid .1,2 NHDCA is an intermediate in the synthesis of 3β-sulfooxy-7β-hydroxy-24-nor-5-cholen-23-oic acid, which has been used as an internal standard for the quantification of δ5-bile acid conjugates that have been identified in patients with Niemann-Pick disease type C1.3 |1. Schteingart, C.D., and Hofmann, A.F. Synthesis of 24-nor-5β-cholan-23-oic acid derivatives: A convenient and efficient one-carbon ...
T38309 LL-37 amide (trifluoroacetate salt)

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. ...
T37702 Pancuronium (bromide hydrate)

Pancuronium is an aminosteroid antagonist of muscle-type nicotinic acetylcholine receptors (nAChRs) with an IC50value of 14.8 nM using patch clamp electrophysiology in BOSC23 cells expressing mouse nAChRs.1It acts as a non-depolarizing neuromuscular blocking agent.2Pancuronium enhances anesthesia induced by isoflurane , reducing immobilization with an ED50value of 1.62 μg/kg.3 1.Liu, M., and Dilger, J.P.Site selectivity of competitive antagonists for the mouse adult muscle nicotinic acetylcholin...
T37201 CAY10787

CAY10787 is an oxysterol and a negative allosteric modulator of GABAAreceptors.1,2It reduces GABA-induced currents in HEK cells expressing α1β1γ2or α4β3γ2subunit-containing GABAAreceptors (IC50s = 1.5 and 1 μM, respectively).2CAY10787 (500 nM) reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.In vivo, CAY10787 (2, 10, and 50 mg/kg) increases latency to nocifensive behaviors in t...
T35814 Urocortin III (human) (trifluoroacetate salt)

Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively)....
T36055 Nitisinone-13C6

Nitisinone-13C6

Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg/kg. Nitisinone (3 mg/kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (F...
T36779 NG 25 (hydrochloride hydrate)

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectiv...
T37847 Zonisamide-13C2,15N

Zonisamide-13C2,15N

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...
T37187 D-erythro/L-threo Lysosphingomyelin (d18:1)

D-erythro/L-threo Lysosphingomyelin (d18:1)

Lysosphingomyelin is an endogenous bioactive sphingolipid and a constituent of lipoproteins.1,2It is produced by the removal of the acyl group from sphingomyelin by a deacylase and acts as a precursor in the biosynthesis of sphingosine-1-phosphate . D-erythroLysosphingomyelin is an agonist of the S1P receptors S1P1, S1P2, and S1P3(EC50s = 167.7, 368.1, and 482.6 nM, respectively, for the human receptors).3It is also an agonist of the orphan receptor ovarian cancer G protein-coupled receptor 1 (O...
T36373 Urocortin II (mouse) (trifluoroacetate salt)

Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF...
T36321 C6 Urea Ceramide

C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It inhibits proliferation of, and induces apoptosis and autophagy in HT-29, but not non-cancerous RIE-1, cells when used at concentrations of 5 and 10 μM. C6 urea ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the ...
T35790 Palmitic acid-1,2,3,4-13C4

Palmitic Acid-13C (C1, C2, C3, and C4 labeled)

Palmitic acid-13C (C1, C2, C3, and C4 labeled) is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids, respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellula...
T35775 HT-2 Toxin-13C22

HT-2 Toxin-13C22

HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human...
T37297 Ru360

Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial ce...
T37736 N-cis-hexadec-9Z-enoyl-L-Homoserine lactone

N-(2-oxotetrahydrofuran-3S-yl) Palmitoleyl Amide,N-cis-hexadec-9Z-enoyl-L-Homoserine lactone

Quorum sensing is a regulatory process used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of whic...
T37741 N-hexadecanoyl-L-Homoserine lactone

C16-HSL,N-palmitoyl-L-Homoserine,N-hexadecanoyl-L-Homoserine lactone

Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which...

化合物

Linopirdine
Cat.No: T15758
Synonym: 利诺吡啶,DuP 996
Target: Potassium Channel, TRP/TRPV Channel
GTP-14564
Cat.No: T71857
Synonym:
Target: FLT, Tyrosine Kinases
m-Nisoldipine
Cat.No: T50077
Synonym: 3-methyl 5-(2-methylpropyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Target: Others
E-4177
Cat.No: T27229
Synonym: E4177
Target:
Sonelokimab
Cat.No: T76885
Synonym:
Target:
VEGFR/PARP-IN-1
Cat.No: T79647
Synonym:
Target: PARP
3β-OH-7-Oxocholenic Acid
Cat.No: T36132
Synonym:
Target:
Norhyodeoxycholic Acid
Cat.No: T37178
Synonym:
Target:
LL-37 amide (trifluoroacetate salt)
Cat.No: T38309
Synonym:
Target:
Pancuronium (bromide hydrate)
Cat.No: T37702
Synonym:
Target:
CAY10787
Cat.No: T37201
Synonym:
Target:
Urocortin III (human) (trifluoroacetate salt)
Cat.No: T35814
Synonym:
Target:
Nitisinone-13C6
Cat.No: T36055
Synonym: Nitisinone-13C6
Target:
NG 25 (hydrochloride hydrate)
Cat.No: T36779
Synonym:
Target:
Zonisamide-13C2,15N
Cat.No: T37847
Synonym: Zonisamide-13C2,15N
Target:
D-erythro/L-threo Lysosphingomyelin (d18:1)
Cat.No: T37187
Synonym: D-erythro/L-threo Lysosphingomyelin (d18:1)
Target:
Urocortin II (mouse) (trifluoroacetate salt)
Cat.No: T36373
Synonym:
Target:
C6 Urea Ceramide
Cat.No: T36321
Synonym:
Target:
Palmitic acid-1,2,3,4-13C4
Cat.No: T35790
Synonym: Palmitic Acid-13C (C1, C2, C3, and C4 labeled)
Target:
HT-2 Toxin-13C22
Cat.No: T35775
Synonym: HT-2 Toxin-13C22
Target:
Ru360
Cat.No: T37297
Synonym:
Target:
N-cis-hexadec-9Z-enoyl-L-Homoserine lactone
Cat.No: T37736
Synonym: N-(2-oxotetrahydrofuran-3S-yl) Palmitoleyl Amide,N-cis-hexadec-9Z-enoyl-L-Homoserine lactone
Target:
N-hexadecanoyl-L-Homoserine lactone
Cat.No: T37741
Synonym: C16-HSL,N-palmitoyl-L-Homoserine,N-hexadecanoyl-L-Homoserine lactone
Target:
Cat. No. Product Name Target Signaling Pathways
T83192 Acetyllycoposerramine M

Acetyllycoposerramine M 是一种从石松(Lycopodium japonicum)中分离出的石松碱类生物碱。该化合物对乙酰胆碱酯酶无抑制作用。
T75538 Alismanol M

Alismanol M,一种法尼酯 X 受体 (FXR) 激动剂,具有 50.25 μM 的 EC50 值。作为一种源自东方红根茎的原丹类三萜化合物,Alismanol M 主要应用于胆汁淤积与非酒精性脂肪性肝炎的研究。
T4700 1,3,5-Trihydroxy-4-prenylxanthone

1,3,5-Trihydroxy-4-prenylxanthone is a relatively potent inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 3.0 μM; it shows in vitro inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 valu
T36563 (E)-Guggulsterone

Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hy...
T35779 Oosporein

Oosporein is a mycotoxin that has been found inBeauveriaand has diverse biological activities.1,2It is cytotoxic to Sf9 and Sf21 insect cells with 50% cytotoxic concentration (CC50) values of 4.23 and 10.43 μM, respectively.3Oosporin induces lethality in day-old cockerels (LD50= 6.12 mg/kg).4It inhibits Na+/K+-, Ca2+-, and Mg2+-ATPase activities by 27, 52, and 100%, respectively, in equine erythrocyte ghosts when used at a concentration of 200 μg/ml.2Oosporein inhibits herpes simplex 1 (HSV-1), ...

天然产物

Acetyllycoposerramine M
Cat.No: T83192
Synonym:
Target:
Alismanol M
Cat.No: T75538
Synonym:
Target:
1,3,5-Trihydroxy-4-prenylxanthone
Cat.No: T4700
Synonym:
Target:
(E)-Guggulsterone
Cat.No: T36563
Synonym:
Target:
Oosporein
Cat.No: T35779
Synonym:
Target:
TargetMol Loading
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