Immunology & Inflammation
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COX-2 抑制剂
FK3311是一种可渗透细胞且可口服的磺酰苯胺,可作为选择性COX-2抑制剂和NSAID。
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COX-2 抑制剂
伐地考昔(Valdecoxib),也称为SC-65872,是一种非甾体类抗炎药(NSAID),用于治疗骨关节炎,类风湿性关节炎以及痛经和月经症状。 它是一种选择性的环氧合酶2(COX-2)抑制剂,IC50为5nM。
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COX-2 抑制剂
Parecoxib是一种有效的选择性COX-2抑制剂。
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COX 抑制剂
Diflunisal是具有止痛和抗炎活性的水杨酸衍生物。
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COX 抑制剂
Amfenac Sodium Monohydrate是一种非甾体止痛消炎药,带有乙酸部分。COX1和COX2的IC50值分别为250 nM和150 nM。
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COX 抑制剂
Ampiroxicam是一种非选择性的环氧合酶抑制剂,被用作抗炎药。
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COX-2 抑制剂
Carprofen通过抑制COX-2和其他炎症性前列腺素来减轻炎症,不干扰COX-1活性。
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COX and lipo-oxygenase 抑制剂
Timegadine被发现是一种有效的竞争性环加氧酶(COX)和脂加氧酶抑制剂,IC50的范围从5 nM(洗兔血小板)到20μM(大鼠脑)。在马血小板匀浆的细胞溶质级分和洗涤过的兔血小板中,脂氧化酶的浓度为100μM和100μM。
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COX 抑制剂
Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
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COX-2 抑制剂
Firocoxib is a non-steroidal anti-inflammatory drug of the COX-2 inhibitor class, currently approved for use in dogs and horses.
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COX-2 抑制剂
Aceclofenac is a cyclooxygenase-2 inhibitor used to treat osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
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COX 抑制剂
Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
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COX-2 抑制剂
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect.
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NSAID and COX-2 抑制剂
Deracoxib is an NSAID and COX-2 inhibitor used to treat osteoarthritis. It induces cell cycle arrest and apoptosis in mammary tumor cells, decreases platelet aggregation, and lowers inflammatory responses.
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COX-2 抑制剂
Bromfenac Sodium Sesquihydrate is a nonsteroidal anti-inflammatory drug (NSAID), which inhibits cyclooxygenase II (COX-2).
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COX 抑制剂
Dipyrone, also known as Anador and NSC-73205, is a nonsteroidal anti-inflammatory drug used to treat pain (postoperative, colic, cancer, and migraine).
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CCR2/CCR5 抑制剂
Cenicriviroc是用于治疗HIV感染的实验性候选药物.Cenicriviroc是CCR2和CCR5受体的抑制剂,可使其充当阻止病毒进入人体细胞的进入抑制剂。
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CCR5 entry 抑制剂
Aplaviroc是一种CCR5进入抑制剂,用于治疗HIV感染。
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CCR2/5 receptors 抑制剂
Cenicriviroc(TAK-652,TBR-652)是CCR2和CCR5受体的抑制剂,可使其充当防止病毒进入人细胞的进入抑制剂
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CCR8 抑制剂
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations.
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TLR4 抑制剂
TAK-242的S对映体。TAK-242(Resatorvid),Toll样受体(TLR)4信号转导的小分子抑制剂。TAK-242用于治疗败血症和败血性休克。
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MD2-TLR4 inhibitor
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
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TLR4 inhibitor
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases.
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TLR inhibitor
AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.
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TLR4 抑制剂
VGX-1027通过抑制Toll样受体4(TLR4)信号传导来显示免疫调节和抗炎活性。
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TLR 抑制剂
TLR2-IN-C29是TLR2/1和TLR2/6信号传导的抑制剂。
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- Qian-Lu Wang, .et al. ROCK1 regulates sepsis-induced acute kidney injury via TLR2-mediated endoplasmic reticulum stress/pyroptosis axis, Mol Immunol, 2021, Oct;138:99-109 PMID: 34365196
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CXCR4 抑制剂
MSX-122是口服可生物利用的CXCR4抑制剂(IC50 =?10 nM),具有潜在的抗肿瘤和抗病毒活性。CXCR4抑制剂MSX-122与趋化因子受体CXCR4结合,阻止基质衍生因子-1(SDF-1)与CXCR4受体和受体激活结合,这可能导致肿瘤细胞增殖和迁移减少。
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CXCL8/CXCR1/2 抑制剂
Reparixin是两种CXCL8受体CXCR1/2的有效抑制剂,它抑制CXCR2介导的细胞迁移(IC50 = 100 nM),而它强烈地阻断CXCR1介导的趋化性(IC50 = 1 nM)。
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- Naour AL, .et al. Tumor cells educate mesenchymal stromal cells to release chemoprotective and immunomodulatory factors, J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. N-acetyl cysteine improves the effects of corticosteroids in a mouse model of chlorine-induced acute lung injury, Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
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CXCL8 receptor 抑制剂
Reparixin L-lysine salt是CXCL8受体的抑制剂,也抑制CXCR1和CXCR2的活化,已显示在各种损伤模型中减弱了炎症反应。
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Dihydropyrimidinase 抑制剂
Dihydromyricetin (Ampeloptin)是具有良好性能的天然抗氧化剂。
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xanthine oxidase 抑制剂
Febuxostat (TEI-6720)是黄嘌呤氧化酶的非嘌呤抑制剂(Ki = 1.2 nM)。
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xanthine oxidase inhibitor
Allopurinol sodium是次黄嘌呤(体内天然存在的嘌呤)的结构异构体,是黄嘌呤氧化酶的抑制剂。
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NOS inhibitor
Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a number of pathological states.
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NOS inhibitor
L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor.
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GPR3 激动剂/NOS/ NADPH oxidases 抑制剂
Diphenyleneiodonium是一种有效的不可逆的巨噬细胞抑制剂NOS2(iNOS)和内皮细胞NOS3(eNOS)抑制剂。
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INOS 抑制剂
1400W Dihydrochloride是一种缓慢,紧密结合,有效和高度选择性的诱导型一氧化氮合酶抑制剂(Kd = 7 nM)。对nNOS和eNOS具有选择性(Ki值分别为2和50μM)。细胞可渗透并在体内具有活性。
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iNOS 抑制剂
GW274150是有效且高度选择性的iNOS抑制剂,可减少实验性肾脏缺血/再灌注损伤。
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Nrf2 inhibitor
Nrf2-IN-1 (Compound 4f) is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2), acts as a promising agent in acute myeloid leukemia (AML) therapy.
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Nrf2 抑制剂
RTA-408是一种合成的三萜类化合物,可有效激活抗氧化转录因子Nrf2并抑制促炎转录因子NF-kB。
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Nrf2 抑制剂
Brusatol是一种生化物质,从Brucea javanica植物中分离出来,可抑制Nrf2。
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NRF2 抑制剂
ML-385是核因子红系2相关因子2(Nrf2)的抑制剂,IC50值为1.9μM。
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MALT1 inhibitor
MLT-748 is a potent, selective and allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM.
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MALT1 inhibitor
MLT-747 is a potent, selective, allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 14 nM.
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MALT1 抑制剂
MI 2直接与MALT1结合并在体外和体内抑制活化的B细胞样弥漫性大B细胞淋巴瘤(ABC-DLBCL)。
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PD-1/PD-L1 interaction 抑制剂
PD1-PDL1 inhibitor 2 是PD-1/PD-L1相互作用抑制剂。
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PD1-PDL1 inhibitor 1 是PD-1/PD-L1相互作用抑制剂。
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NADPH-oxidase 抑制剂
Apocynin (Acetovanillone)是NADPH氧化酶抑制剂。
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- Liling Su, .et al. Disruption of mitochondrial redox homeostasis as a mechanism of antimony-induced reactive oxygen species and cytotoxicity, Ecotoxicol Environ Saf, 2022, Jun 1;237:113519 PMID: 35453021
- Shimizu S, .et al. Angiotensin II, a stress-related neuropeptide in the CNS, facilitates micturition reflex in rats, Br J Pharmacol, 2018, Sep;175(18):3727-3737 PMID: 29981238
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NOX1 抑制剂
ML 171是一种有效的、选择性的NADPH-oxidase抑制剂,对NOX1、NOX2、NOX3、NOX4和xanthine oxidase的IC50分别为0.25 μM, 5 μM, 3μM, 5 μM 和 5.5 μM。
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NOX1/4 抑制剂
GKT137831是针对NOX1和NOX4酶的一流抑制剂。
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- Chia-Hui Huang, .et al. Arsenic Trioxide-Induced p38 MAPK and Akt Mediated MCL1 Downregulation Causes Apoptosis of BCR-ABL1-positive Leukemia Cells, Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
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Nox inhibitor
APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury.
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