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14

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
T13147 ICAM-1-IN-1

Integrin Cytoskeletal Signaling
ICAM-1-IN-1 是选择性的 ICAM-1和 E-selectin 抑制剂,IC50值分别为5和7 nM。
T12783 RWJ 50271

Integrin Cytoskeletal Signaling
RWJ 50271 是具有口服活性的选择性LFA-1/ICAM-1相互作用抑制剂,抑制 LFA-1/ICAM-1 介导的细胞粘附,在细胞HL60中的IC50值为 5.0 μM。
T23796 BIRT-377

BIRT377,BIRT 377

IL Receptor; Integrin Cytoskeletal Signaling; Immunology/Inflammation
BIRT-377 是 ICAM-1 和 LFA-1 的负变构和口服生物利用度抑制剂(Ki = 25.8 nM)。 BIRT-377 抑制 IL-2 的产生,可用于有关炎症和免疫疾病的研究。
T0468 Lidocaine

Lignocaine,Alphacaine,Xylocaine,利多卡因

Apoptosis; ERK; NF-κB; MEK; Sodium Channel; Histamine Receptor Apoptosis; GPCR/G Protein; Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Neuroscience; NF-κB
Lidocaine (Alphacaine) 是一种酰胺衍生物,抑制涉及复杂电压和依赖性的钠通道,可用于研究室性心律失常。它通过调节 miR-145 表达和进一步抑制 MEK/ERK 和 NF-κB 信号通路来减少胃癌细胞的生长,迁移和侵袭。
T38976 MUC1, mucin core

MUC1, mucin core

MUC1, mucin core is a type I transmembrane glycoprotein that is characterized by its overexpression and abnormal glycosylation in carcinoma cells. It specifically binds to domain 1 of ICAM-1.
T64233 Alicaforsen

Alicaforsen 是一种 20 个碱基长度的反义寡核苷酸,对 ICAM-1 的产生表现出抑制作用。其中 ICAM-1 是一种重要的粘附分子,能够参与白细胞向炎症部位迁移和转运的过程。
T76841 Enlimomab

Enlimomab (BI-RR 0001) 是一种针对人 ICAM-1的小鼠 IgG2a 单抗,可抑制白细胞粘附到血管内皮,从而减少白细胞外渗漏和炎症性组织损伤。Enlimomab 具有抗炎作用,可用于中风研究。
T78548 3-Hydroxyxanthone

3-Hydroxy-xanthen-9-one

Integrin Cytoskeletal Signaling
3-Hydroxyxanthone (3-Hydroxy-xanthen-9-one) 是一种具有抗炎活性的氧杂蒽酮化合物。它能抑制人脐静脉内皮细胞(HUVEC)中NADPH催化的脂质过氧化,并且阻止TNF-α所诱导的ICAM-1表达。
T38339 R-8507

R-8507 is a small molecule antagonist of the TNF-α type 1 receptor (TNF-αRI). It inhibits the expression of intercellular adhesion molecule-1 (ICAM-1) induced by TNF-α and IL-1β with EC50 values of 2.45 and 3.79 μM, respectively, in an ELISA using A549 lung epithelial cells.{|Gururaja2007|} It also disrupts the interaction of the TNF-αRI with receptor interacting protein 1 (RIP1) and TNF-αR-associated death domain protein (TRADD), preventing internalization of the receptor complex.
T36385 Ansatrienin A

Ansatrienin A is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis. In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 64 nM), which is a measure of bone resorption, and pp60c-srcM kinase (IC50 = 100 nM). It also inhibits TNF-α-induced expression of intercellular adhesion molecule-1 (ICAM-1; IC50 = 570 nM). Early in vitro studies showed that ansatrienin A potentiates the chemotherapeutic action of 5-fl...
T36650 Ansatrienin B

Ansatrienin B is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis., In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 21 nM), which is a measure of bone resorption, and pp60c-src kinase (IC50 = 50 nM). It is an inhibitor of translation at the protein synthesis stage by specific inhibition of L-leucine incorporation (IC50 = 58 nM in A549 cells). It also inhibits TNF-α-induced expression of intercellul...
T35494 (±)11(12)-EET

(±)11(12)-EET is a fully racemic version of the R/S enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes.[1][2][3[]A higher proportion of 11(R),12(S)-EET is produced by the CYP450 isoforms CYP2C23 and CYP2C24 while CYP2B2 produces a higher proportion of 11(S),12(R)-EET.[3]11(12)-EET has been shown, along with 8(9)-EET to play a role in the recovery of depleted calcium pools in cultured smooth muscle cells[4] It also inhibits basolateral 18-pS potassium channels in t...
T35463 (±)14(15)-EET

(±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET

(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage o...
T62111 Antioxidant agent-5

Antioxidant agent-5 (compound D-6) 是一种有效的抗氧化剂。Antioxidant agent-5 能够抑制 oxLDL 诱导的 ROS 水平升高和 NF-κB 核转位。Antioxidant agent-5 对 oxLDL (氧化型低密度脂蛋白)诱导的 VECs 细胞凋亡 (apoptosis) 及 ICAM-1 和 VCAM-1 的表达表现出抑制作用。Antioxidant agent-5 可以激活 Nrf2/HO-1 抗氧化通路,对 oxLDL 诱导的内皮损伤表现出保护活性。

化合物

ICAM-1-IN-1
Cat.No: T13147
Synonym:
Target: Integrin
RWJ 50271
Cat.No: T12783
Synonym:
Target: Integrin
BIRT-377
Cat.No: T23796
Synonym: BIRT377,BIRT 377
Target: IL Receptor, Integrin
Lidocaine
Cat.No: T0468
Synonym: Lignocaine,Alphacaine,Xylocaine,利多卡因
Target: Apoptosis, ERK, NF-κB, MEK, Sodium Channel, Histamine Receptor
MUC1, mucin core
Cat.No: T38976
Synonym: MUC1, mucin core
Target:
Alicaforsen
Cat.No: T64233
Synonym:
Target:
Enlimomab
Cat.No: T76841
Synonym:
Target:
3-Hydroxyxanthone
Cat.No: T78548
Synonym: 3-Hydroxy-xanthen-9-one
Target: Integrin
R-8507
Cat.No: T38339
Synonym:
Target:
Ansatrienin A
Cat.No: T36385
Synonym:
Target:
Ansatrienin B
Cat.No: T36650
Synonym:
Target:
(±)11(12)-EET
Cat.No: T35494
Synonym:
Target:
(±)14(15)-EET
Cat.No: T35463
Synonym: (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET
Target:
Antioxidant agent-5
Cat.No: T62111
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5785 MALTOTETRAOSE

Fujioligo 450,Amylotetraose,α-1,4-Tetraglucose,麦芽四糖

TNF; Endogenous Metabolite Apoptosis; Metabolism
Maltotetraose (Fujioligo 450) 能够作为生物流体中酶联测定淀粉酶特性的底物。
TN1163 2'-Hydroxychalcone

Others Others
2'-Hydroxychalcone 是一种药物合成中间体,可用于合成黄酮类化合物。负载在纳米乳液中的2'-Hydroxychalcone 在Danio rerio 模型对副球孢子菌显示出杀真菌活性。2'-Hydroxychalcone 通过负载脂质的Hepg2细胞中的氧化应激诱导细胞毒性。2'-Hydroxychalcone 抑制通过逆转录聚合酶链反应确定的肿瘤坏死因子-α诱导ICAM-1,VCAM-1和E-选择素的稳态转录水平,因此可能会干扰其基因的转录。
TN6694 5,6-Benzoflavone

β-Naphthoflavone,beta-NF

Antioxidant oxidation-reduction
5,6-Benzoflavone (β-Naphthoflavone) 是芳烃受体的外源配体,可破坏人肝癌 HepG2 细胞中的锌稳态。5,6-Benzoflavone (β-Naphthoflavone) 具有抗炎和抗氧化活性,抑制通过 AKT/Nrf-2/HO-1-NF-kappaB 信号转导轴,抑制 LPS 诱导的炎症,抑制TNF-α诱导的ICAM-1和VCAM-1表达,可用于研究神经退行性疾病。
T3427 Polydatin

Piceid,虎杖苷,Polydotin Peceid

Apoptosis; Mitophagy; NF-κB; Autophagy Apoptosis; Autophagy; NF-κB
Polydatin (Piceid) 是从传统中药虎杖根中提取的一种天然产物,在多个实验模型中具有抗炎作用。它可抑制 G6PD,并诱导氧化和内质网应激。
T79962 Aloenin aglycone

Others Others
Aloenin aglycone (compound 13) 作为一种NF-κB抑制剂,可从芦荟渗出液中提取。它在抑制TNFα引发的NF-κB转录活性方面表现显著(IC50: 18.7 μM)。当HepG2细胞经10 ng/mL TNFα处理时,以10 μM Aloenin aglycone处理能有效下调诱导型一氧化氮合酶(iNOS)及细胞间粘附分子1ICAM-1)的基因表达。

天然产物

MALTOTETRAOSE
Cat.No: T5785
Synonym: Fujioligo 450,Amylotetraose,α-1,4-Tetraglucose,麦芽四糖
Target: TNF, Endogenous Metabolite
2'-Hydroxychalcone
Cat.No: TN1163
Synonym:
Target: Others
5,6-Benzoflavone
Cat.No: TN6694
Synonym: β-Naphthoflavone,beta-NF
Target: Antioxidant
Polydatin
Cat.No: T3427
Synonym: Piceid,虎杖苷,Polydotin Peceid
Target: Apoptosis, Mitophagy, NF-κB, Autophagy
Aloenin aglycone
Cat.No: T79962
Synonym:
Target: Others
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