Immunology & Inflammation
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CXCR3 antagonist
SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
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CXCR3 antagonist
AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3.
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CXCR3 antagonist
NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
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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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Acetylcysteine是一种是ROS抑制剂,拮抗多种蛋白酶体抑制剂的活性。它还是肿瘤坏死因子TNF的抑制剂,主要用作祛痰剂,可处理扑热息痛(对乙酰氨基酚)过量。
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- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- R Kasi, .et al. Melatonin Induces Apoptosis and Inhibits the Proliferation of Cancer Cells via Reactive Oxygen Species-mediated MAPK and mTOR Pathways, Clinical Cancer Drugs, 2020, 2019, 7(1): 44 - 56
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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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Allopurinol是嘌呤类似物;它是次黄嘌呤(人体中天然存在的嘌呤)的结构异构体,是黄嘌呤氧化酶的抑制剂。
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6-Benzylaminopurine是第一代合成细胞分裂素,可调节植物抗氧化防御系统的活性,其处理诱导植物生长发育。
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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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NOS cofactor
Biopterin是一氧化氮合酶(NOS)辅助因子四氢-L-生物蝶呤(BH4)的氧化形式。可以通过硫氧还蛋白还原酶,然后是二氢蝶呤还原酶或还原型谷胱甘肽,将L-生物蝶呤还原为BH4。在培养中对人黑素细胞具有极强的毒性(48小时后IC50 = 0.2 uM)。
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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 activator
Oltipraz抑制HIF-1alpha活性和HIF-1alpha依赖性肿瘤生长,这可能是由于S6K1抑制结合H2O2清除作用导致HIF-1alpha稳定性降低所致。
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Nrf2 activator
CDDO-EA是Nrf2/ARE的激活剂;神经保护作用。
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Nrf2 activator
NK-252是Nrf2活化剂,与OPZ相比,具有更大的Nrf2活化电位。
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Nrf2 activator
AKBA (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator.
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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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Keap1/Nrf2/ARE pathway inducer
(R)-Sulforaphane is a highly potent inducer of the Keap1/Nrf2/ARE pathway. (R)-Sulforaphane is a far more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer.
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- Isin Cakir, .et al. Sulforaphane reduces obesity by reversing leptin resistance, Elife, 2022, Mar 24 PMID: 35323110
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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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LTR antagonist
Montelukast (trade name Singulair) is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies.
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LTR antagonist
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
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Pranlukast (ONO 1078)是一种选择性的半胱氨酰白三烯受体拮抗剂。
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LTD4 receptor 拮抗剂
MK-0679 (Verlukast)是有效的白三烯D4拮抗剂。
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BLT2 receptors 拮抗剂
LY 255283是一种有效的 BLT2 receptors 拮抗剂。
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CysLT1 receptor 拮抗剂
MK-571是有效的CysLT1(LTD4)白三烯受体反向激动剂,EC50值为1.3 nM。
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- Jung-Hung Chen, .et al. Transplacental transfer of acetaminophen in pregnant rats, Biomed Pharmacother, 2022, Oct;154:113613 PMID: 36058146
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CysLT1 receptor 拮抗剂
MK-571 sodium salt是一种选择性的口服活性CysLT1受体拮抗剂。它阻断LTD4而不是LTC4与人和豚鼠肺膜的结合,Ki值分别为0.22 nM和2.1 nM。
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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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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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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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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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