Immunology & Inflammation
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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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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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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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CXCR4 拮抗剂
Plerixafor 8HCl (DB06809)是CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导调节的趋化性， IC50分别为44 nM和5.7 nM。
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- Mei Zheng, .et al. CXCL12 inhibits hair growth through CXCR4, Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. Bone marrow cell homing to sites of acute tibial fracture: 89Zr-oxine cell labeling with positron emission tomographic imaging in a mouse model, EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. Bone marrow cell trafficking analyzed by 89Zr-oxine positron emission tomography in a murine transplantation model, Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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CXCR4 拮抗剂
AMD 070是CXCR4趋化因子受体拮抗剂。
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- Uchida D, .et al. Effect of a novel orally bioavailable CXCR4 inhibitor, AMD070, on the metastasis of oral cancer cells, Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. Enhancement of the CXCL12/CXCR4 axis due to acquisition of resistance in pancreatic cancer: effect of CXCR4 antagonists, BMC Cancer, 2016, 16: 305 PMID: 27175473
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CXCR4 拮抗剂
AMD 3465 Hexahydrobromide是一种有效的选择性CXCR4拮抗剂。
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- Kentaro Suzuki, .et al. C-terminal-modifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
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CXCR2 ligand
SRT3109是一种CXCR2配体，用于治疗趋化因子介导的疾病和状况。
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CXCR4 拮抗剂
WZ811是4型C-X-C趋化因子受体（CXCR4）拮抗剂（EC50 = 0.3 nM）。在体外抑制CXCR4/基质细胞衍生因子1（SDF-1）介导的cAMP调节（EC50 = 1.2 nM）。
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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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SIRT1 activator
SRT3190是一种强效cxcr2配体。
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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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CXCR4 拮抗剂
AMD3100 (Plerixafor)是用于增殖造血干细胞的免疫刺激剂，并且是用于动员造血干细胞进行移植的趋化因子受体-4拮抗剂。
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- Hitoshi Maeda, .et al. Cell-penetrating albumin enhances the sublingual delivery of antigens through macropinocytosis, Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. Brain vascular damage-induced lymphatic ingrowth is directed by Cxcl12b/Cxcr4a, Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. Effects of local vs systemic administration of CXCR4 inhibitor AMD3100 on orthodontic tooth movement in rats, Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. Positive effects of selenium supplementation on selenoprotein S expression and cytokine status in a murine model of acute liver injury, J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. Stromal cell-derived factor 1 (SDF1) attenuates platelet-derived growth factor-B (PDGF-B)-induced vascular remodeling for adipose tissue expansion in obesity, Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. Role of Prx1-expressing skeletal cells and Prx1-expression in fracture repair, Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. C-terminal?Cmodifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. Cell-penetrating mechanism of intracellular targeting albumin: Contribution of macropinocytosis induction and endosomal escape, J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. LPS-induced CXCR7 expression promotes gastric Cancer proliferation and migration via the TLR4/MD-2 pathway, Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. The role of conventional antibodies targeting the CD4 binding site and CD4-induced epitopes in the control of HIV-1 CRF01_AE viruses, Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. Microbe-dependent lymphatic migration of neutrophils modulates lymphocyte proliferation in lymph nodes, Nat Commun, 2015, 6: 7139 PMID: 25972253
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CXCR1/CXCR2 拮抗剂
SCH-527123 (Navarixin)是人CXCR1和CXCR2受体的强效选择性拮抗剂，IC50分别为42 nM和3 nM。
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- Ruijie Zhang, .et al. Combined inhibition of IL-6 and IL-8 pathways suppresses ovarian cancer cell viability and migration and tumor growth, Int J Oncol, 2022, May;60(5):50 PMID: 35315502
- Fu S, .et al. Inhibition of interleukin 8/C-X-C chemokine receptor 1,/2 signaling reduces malignant features in human pancreatic cancer cells, Int J Oncol, 2018, Jul;53(1):349-357 PMID: 29749433
- Fu S, .et al. Blocking Interleukin-6 and Interleukin-8 Signaling Inhibits Cell Viability, Colony-forming Activity, and Cell Migration in Human Triple-negative Breast Cancer and Pancreatic Cancer Cells, Anticancer Res, 2018, Nov;38(11):6271-6279 PMID: 30396947
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CXCR2 拮抗剂
SB265610是CXCR2 (Kd = 2.51 nM)的非肽变构反向激动剂，通过与不同于激动剂结合位点的区域结合来防止受体活化。它不与相关CXCR1受体结合。在体外和高氧诱导肺损伤的大鼠模型中，它已被证明能防止中性粒细胞趋化性。
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CXCR2 拮抗剂
SB225002是一种有效的选择性CXCR2拮抗剂，IC50为22 nM，可抑制白介素IL-8与CXCR2的结合，选择性是其他测试的7-TMR的150倍以上。
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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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CXCR2/CXCR1 拮抗剂
SCH 563705是有效的双重CXCR2（IC50 = 1.3 nM)/CXCR1（IC50 = 7.3 nM）拮抗剂。
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CXCR4 拮抗剂
在CXCR4 125I-SDF抑制结合试验中，AMD-070 HCl是一种有效的选择性CXCR4拮抗剂，IC50值为13 nM，抑制T-4型HIV-1（NL4.3株）在MT-4细胞中的复制和PBMC。
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CXCL chemokines 拮抗剂
UNBS5162是一种新型萘二甲酰亚胺，可降低实验性前列腺癌中CXCL趋化因子的表达。9种癌细胞系的平均抗增殖活性IC50值为17.9 uM；UNBS3157的水解产物。
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CXCR2 拮抗剂
AZD-5069是一种有效的选择性CXCR2拮抗剂，具有抑制COPD患者中性粒细胞向气管迁移的潜能。
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CXCR4 激动剂
ATI-2341是针对C-X-C趋化因子受体4型（CXCR4）（EC50 = 194 nM）的pepducin，是一种变构激动剂，可激活抑制性异三聚体G蛋白（Gi），从而促进cAMP生成的抑制并诱导钙动员。
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CXCR4 receptor modulator
NSC-23026是CXCR4受体调节剂。
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CXCR4 拮抗剂
USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
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GPR35/CXCR8 拮抗剂
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
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Human CXCR3 拮抗剂
PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM.
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CXCR2 激动剂
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.
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GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
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GPR35/CXCR8 agonist
Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
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CXCR3 antagonist
AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
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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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TLR7 Ligand
Toll-Like Receptor 7 Ligand II是一种细胞可渗透的羟基腺嘌呤化合物，可作为强效且高度特异性的TLR7（toll样受体7）激动剂，对TLR2/3/5/8/9没有任何可检测的活性。它在刺激体外培养物中产生TLR7依赖性细胞因子方面比R848效力高10倍。
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TLR8 激动剂
VTX-2337是一种具有潜在的免疫刺激和抗肿瘤活性的小分子Toll样受体8（TLR8）激动剂。
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- Yinwen Cheng, .et al. The anti-tumor effects of cetuximab in combination with VTX-2337 are T cell dependent, Sci Rep, 2021, Jan 15;11(1):1535 PMID: 33452311
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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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Hydroxychloroquine Sulfate是一种抗疟疾药，用于治疗系统性红斑狼疮，类风湿性关节炎和其他自身免疫性，炎性和皮肤病性疾病。还可以作为自噬和通行费样受体（TLR）7/9的抑制剂。
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Toll-like receptor modulator是一类在先天免疫系统中起关键作用的蛋白质。是一类在先天免疫系统中起关键作用的蛋白质。
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TLR7 激动剂
Gardiquimod TFA是一种化合物，可选择性作用于小鼠和人类形式的Toll样受体7（TLR7）。它起免疫反应调节剂的作用。CAS：1020412-43-4（游离碱）
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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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TLR7 激动剂
TLR7-agonist-1是一种有效且选择性的Toll样受体7（TLR7）激动剂，LEC为0.4 μM。
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TLR7 激动剂
Imiquimod (Aldara)是一种杂环咪唑并喹啉酰胺，用作免疫反应调节剂。
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- David Diaz-Carballo, .et al. Enhanced antitumoral activity of TLR7 agonists via activation of human endogenous retroviruses by HDAC inhibitors, Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Kunishita Y, .et al. TRIM21 Dysfunction Enhances Aberrant B-Cell Differentiation in Autoimmune Pathogenesis, Front Immunol, 2020, Feb 7;11:98 PMID: 32117252
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