Immunology & Inflammation
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LTA4 hydrolase 抑制剂
SC 57461A是体外有效的重组人白三烯A4水解酶抑制剂(Askonas等,2002)。
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SIK/TBK-1/IKKe 抑制剂
MRT67307是一种强效双IKK?和TBK1抑制剂,IC50分别为160和19 nM。
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SIK2 inhibitor
ARN-3236 is potent, orally active and selective SIK2 inhibitor. ARN-3236 inhibited the growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μmol/L.
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SIK inhibitor
YKL-06-061 is a potent and selective SIK (salt-inducible kinase) inhibitor.
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SIK inhibitor
HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.
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arginase 抑制剂
BEC HCl是一种缓慢结合的竞争性精氨酸酶抑制剂,精氨酸酶II和大鼠精氨酸酶I的Ki分别为0.31 μM(pH7.5)和0.4-0.6 μM。
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Arginase 抑制剂
CB-1158,也称为INCB01158,是一种有效的口服活性精氨酸酶抑制剂,IC50 = 89nM。
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arginase 抑制剂
CB-1158,也称为INCB01158,是一种有效的口服精氨酸酶抑制剂,IC50 = 89 nM。
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Arginase inhibitor
nor-NOHA acetate is a specific and reversible arginase inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia.
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arginases I and II inhibitor
Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.
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L-PGDS 抑制剂
AT-56是脂环素型前列腺素D合酶(L-PGDS)的口服活性抑制剂(Ki = 75μM,IC50 = 95μM)。
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HPGDS 抑制剂
HPGDS inhibitor 1是一种新的选择性造血前列腺素d合酶(HPGDS)抑制剂,IC50值为0.7 nM。
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hPGDS 抑制剂
SAR191801是一种hPGDS抑制剂,在荧光偏振分析或EIA分析中,IC50为12 nM。
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H-PGDS 抑制剂
HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM.
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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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NOX2 inhibitor
GSK2795039 is a NADPH oxidase 2 (NOX2) inhibitor with a mean pIC50 of 6 in different cell-free assays. GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption. GSK2795039 reduces apoptosis.
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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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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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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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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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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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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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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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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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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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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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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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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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COX-1 抑制剂
Ibuprofen (Advil)是一种非甾体抗炎药(NSAID),靶向COX-1,IC50为13 μM。
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- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347