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30

抑制剂 & 化合物

12

天然产物

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Cat. No. Product Name Target Signaling Pathways
T20626 Esomeprazole

Proton pump; Cysteine Protease Membrane transporter/Ion channel; Proteases/Proteasome
Esomeprazole 是奥美拉唑(omeprazole) 的S-异构体,抑制溶酶体半胱氨酸蛋白酶legumain,防止癌症转移。它是一种质子泵抑制剂(PPI)。
T9195 SHR0302

ARQ252

Apoptosis; JAK Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
SHR0302 (ARQ252) 是一种具有口服活性的 JAK 抑制剂。它对 JAK1的结合力是 JAK2的 10 倍以上,是 JAK3的 77 倍,是 Tyk2的 420 倍。它抑制JAK1-STAT3磷酸化并诱导肝星状细胞凋亡,具有抗增殖和抗炎作用。
T1394 Ibuprofen

Brufen,(±)-Ibuprofe,布洛芬,Motrin,Advil

COX Immunology/Inflammation; Neuroscience
Ibuprofen (Advil) 是一种丙酸衍生物和非甾体抗炎药 (NSAID),具有抗炎、镇痛和解热作用。它是COX-1和COX-2的抑制剂,IC50值分别为 13 和 370 μM,导致前列腺素和血栓素前体的形成减少。
T6540 Ibuprofen Lysine

布洛芬赖氨酸盐,Neoprofen

COX Immunology/Inflammation; Neuroscience
Ibuprofen Lysine (Neoprofen) 是一种非甾体抗炎药。
T4503 Talniflumate

Somalgen,他尼氟酯

Chloride channel; COX; N-Acetylglucosaminyltransferase; Anion Exchanger Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
Talniflumate (Somalgen) 是一种钙激活氯离子通道 (hCLCA1/mCLCA3) 阻滞剂,可减少动物模型和细胞培养中的粘蛋白合成和释放。它通过抑制环氧合酶,并抑制 Cl-/HCO3- 交换活性,具有抗炎作用。它还增加了远端肠梗阻综合征囊性纤维化小鼠模型的存活率。
T2486 IOWH-032

IOWH032,IOWH 032

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
IOWH-032 (IOWH032) 是一种合成 CFTR 抑制剂,可用于研究治疗霍乱、腹泻和分泌性腹泻,在T84和CHO-CFTR 细胞实验中IC50为1.01 uM。
T2686L Esomeprazole Sodium

埃索美拉唑钠,(S)-Omeprazole sodium

ATPase; Proton pump Membrane transporter/Ion channel
Esomeprazole Sodium ((S)-Omeprazole sodium) 是一种口服有效的活性质子泵抑制剂。Esomeprazole sodium 通过抑制胃壁细胞中的 H+, K+-ATPase 来降低酸分泌,在胃食管反流疾病中有研究价值。Esomeprazole 是一种外泌体抑制剂,通过抑制 V-H+-ATPases 来阻断外泌体的释放。
T83064 Anti-hepatic fibrosis agent 2

Fibrosis agent 2为针对Ewing肉瘤断点区域1 (EWSR1) 的特定抗纤维化化合物。
T2663 GTS-21 dihydrochloride

GTS 21 dihydrochloride,DMXB-A,DMBX-anabaseine

5-HT Receptor; AChR GPCR/G Protein; Neuroscience
GTS-21 dihydrochloride (DMBX-anabaseine) 是一种选择性 α7 烟碱乙酰胆碱受体激动剂,具有抗炎和增强认知的活性。它也是一种拮抗剂,对人α4β2的 Ki 为20 nM,对5-HT3A 受体的 IC50为3.1 μM。
T10409 ATX inhibitor 5

PDE Metabolism
ATX inhibitor 5 是一种有效且具有口服活性的 autotaxin (ATX) 抑制剂(IC50 : 15.3 nM),可降低 CCl4 诱导的肝纤维化水平,具有抗肝纤维化作用,。
T14076 A 839977

A839977,A-839977

P2X Receptor; Calcium Channel Membrane transporter/Ion channel; Metabolism; Neuroscience
A 839977是一种选择性 P2X7 受体拮抗剂,具有抗炎和镇痛活性, 可抑制 P2X7 受体的 BzATP 诱发的钙内流,可用于研究肾纤维化 .
T15647 Tipelukast

MN 001,KCA 757

Leukotriene Receptor GPCR/G Protein
Tipelukast (KCA 757) 是一种新型可口服的白三烯受体 (leukotriene receptor) 拮抗剂,是具有抗炎活性,可减少纤维化,下调 TIMP-1、1 型胶原蛋白。Tipelukast 可用于研究哮喘疾病。
T11411 GLPG1205

GPR; Others Endocrinology/Hormones; GPCR/G Protein; Others
GLPG1205是一种有效的、具有口服活性的 GPR84(G 蛋白偶联受体)拮抗剂,具有抗炎活性 。GLPG1205显示出良好的PK/PD 特征,可用于研究肺纤维化。
T76956 Vixarelimab

RG-6536,RO-7622888,KPL-716

Interleukin Immunology/Inflammation
Vixarelimab (KPL-716) 是一种人源的抗 oncostatin M (OSM)单克隆抗体,对 OSM 受体的β链有亲和力,对 IL-31 和 OSM 的信号传导有抑制作用。Vixarelimab 可用于研究重度结节性痒疹和特发性肺纤维化。
T25136 Aztreonam lysine

Corus 1020,Corus1020,Corus-1020,Aztreonam lysinate

Aztreonam lysine is an inhaled anti-pseudomonal treatment for people who have pulmonary Pseudomonas aeruginosa infection with cystic fibrosis (CF).
T70622 Selonsertib HCl

Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis ...
T74996 FXR agonist 3

FXR agonist3 是一种抗 NASH 试剂,通过激活 FXR 起作用。FXR agonist3 抑制 COL1A1、TGF-β1、α-SMA 和 TIMP1的表达,具有抗纤维化活性。FXR agonist3 显著减轻肝脏脂肪变性和炎症,改善肝纤维化水平。
T78944 VDR agonist 2

VDR agonist 2(化合物16i)作为VDR(vitamin D receptor)激动剂,能有效抑制TGF-β1诱导的肝星状细胞(HSC)活化,并在体外和体内展现出显著的抗肝纤维化效果。
T80526 L-K6L9

L-K6L9 对于囊性纤维化患者的铜绿假单胞菌 (P. aeruginosa) 表现出显著的抗菌 (antimicrobial) 活性和抗生物膜 (anti-biofilm) 能力。该化合物的抗酶解性质保证了其在体内的稳定性,且不引发细菌的耐药性。
T61586 TGFβ-IN-2

TGFβ-IN-2 (Compound 9d) effectively inhibits the accumulation of total collagen induced by TGF-β in NRK-49F cells, with an IC 50 value of 4.31 μM. It also suppresses the in vitro protein expression of COL1A1, α-SMA, and p-Smad3, which are induced by TGF-β. Additionally, TGFβ-IN-2 shows promise as a potential anti-fibrosis compound for in vivo applications through oral administration [1].
T64008 Thi-DPPY

Thi-DPPY 是一种有效的、口服具有活力的 JAK3 抑制剂,能够作用于 BTK (IC50: 62.4 nM)、JAK (IC50: 1.38 nM)。Thi-DPPY 能够抗 HBE 细胞的增殖。Thi-DPPY 在体内具有抗炎作用。Thi-DPPY 对特发性肺纤维化(IPF)表现出研究潜力。
T62301 J-1063

J-1063 是一种选择性、口服具有活力的、有效的 ALK5 抑制剂 (IC50: 0.039 μM)。 J-1063 能够抑制炎症浸润,胶原沉积,肝细胞坏死,表现出抗肝纤维化作用。J-1063 具有潜力进行肝纤维化的研究。
T73155 BMS-986339

BMS-986339 是一种具有口服活性的FXR 激动剂。BMS-986339 可与 His298 和 ASN287 残基形成氢键。BMS-986339 可用于原发性胆汁性肝硬化 (PBC)、原发性硬化性胆管炎 (PSC)、非酒精性脂肪性肝炎 (NASH),和抗纤维化研究。
T10964L DB1976 dihydrochloride

DB1976 hydrochloride,DB1976 2HCl

Apoptosis; NF-κB Apoptosis; NF-κB
DB1976 dihydrochloride (DB1976 2HCl) ,一种转录因子 PU.1 抑制剂,具有潜在抗炎活性,可在体内实验中减缓小鼠的炎症和纤维化,改善了葡萄糖稳态和血脂异常。DB1976 dihydrochloride 促进细胞凋亡,可用于研究代谢功能障碍和非酒精性脂肪性肝炎。
T36408 Rhein-13C4

Rhein-13C4

Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically i...
T79731 MLKL-IN-6

Necroptosis Apoptosis
MLKL-IN-6(compound P28)是一种针对Mixed Lineage Kinase domain-like(MLKL)的混合谱系激酶抑制剂,具有抗纤维化的潜力。它能够抑制MLKL的磷酸化和寡聚化,从而抑制细胞坏死、免疫细胞死亡,并减少粘附因子的表达。MLKL-IN-6展现出低细胞毒性,并可抑制肝星状细胞的激活,从而降低肝纤维化标志物的水平。
T71303 Flufenamic Acid-d4

Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear...
T37861 Talabostat

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...
T36673 CC 401 dihydrochloride

High affinity JNK inhibitor (Ki values are 25-50 nM). Inhibits JNK via competitive binding of the ATP-binding site of active, phosphorylated JNK. Exhibits > 40-fold selectivity for JNK over p38, ERK, IKK2, protein kinase C, Lck and ZAP70. Hepatoprotective. Also inhibits HCMV replication. Uehara et al (2004) c-Jun N-terminal kinase mediates hepatic injury after rat liver transplantation. Transplantation. 78 324 PMID:15316358 |Uehara et al (2005) JNK mediates hepatic ischemia reperfusion injury. J...
T36618 Rupatadine

Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu...

化合物

Esomeprazole
Cat.No: T20626
Synonym:
Target: Proton pump, Cysteine Protease
SHR0302
Cat.No: T9195
Synonym: ARQ252
Target: Apoptosis, JAK
Ibuprofen
Cat.No: T1394
Synonym: Brufen,(±)-Ibuprofe,布洛芬,Motrin,Advil
Target: COX
Ibuprofen Lysine
Cat.No: T6540
Synonym: 布洛芬赖氨酸盐,Neoprofen
Target: COX
Talniflumate
Cat.No: T4503
Synonym: Somalgen,他尼氟酯
Target: Chloride channel, COX, N-Acetylglucosaminyltransferase, Anion Exchanger
IOWH-032
Cat.No: T2486
Synonym: IOWH032,IOWH 032
Target: CFTR, Autophagy
Esomeprazole Sodium
Cat.No: T2686L
Synonym: 埃索美拉唑钠,(S)-Omeprazole sodium
Target: ATPase, Proton pump
Anti-hepatic fibrosis agent 2
Cat.No: T83064
Synonym:
Target:
GTS-21 dihydrochloride
Cat.No: T2663
Synonym: GTS 21 dihydrochloride,DMXB-A,DMBX-anabaseine
Target: 5-HT Receptor, AChR
ATX inhibitor 5
Cat.No: T10409
Synonym:
Target: PDE
A 839977
Cat.No: T14076
Synonym: A839977,A-839977
Target: P2X Receptor, Calcium Channel
Tipelukast
Cat.No: T15647
Synonym: MN 001,KCA 757
Target: Leukotriene Receptor
GLPG1205
Cat.No: T11411
Synonym:
Target: GPR, Others
Vixarelimab
Cat.No: T76956
Synonym: RG-6536,RO-7622888,KPL-716
Target: Interleukin
Aztreonam lysine
Cat.No: T25136
Synonym: Corus 1020,Corus1020,Corus-1020,Aztreonam lysinate
Target:
Selonsertib HCl
Cat.No: T70622
Synonym:
Target:
FXR agonist 3
Cat.No: T74996
Synonym:
Target:
VDR agonist 2
Cat.No: T78944
Synonym:
Target:
L-K6L9
Cat.No: T80526
Synonym:
Target:
TGFβ-IN-2
Cat.No: T61586
Synonym:
Target:
Thi-DPPY
Cat.No: T64008
Synonym:
Target:
J-1063
Cat.No: T62301
Synonym:
Target:
BMS-986339
Cat.No: T73155
Synonym:
Target:
DB1976 dihydrochloride
Cat.No: T10964L
Synonym: DB1976 hydrochloride,DB1976 2HCl
Target: Apoptosis, NF-κB
Rhein-13C4
Cat.No: T36408
Synonym: Rhein-13C4
Target:
MLKL-IN-6
Cat.No: T79731
Synonym:
Target: Necroptosis
Flufenamic Acid-d4
Cat.No: T71303
Synonym:
Target:
Talabostat
Cat.No: T37861
Synonym:
Target:
CC 401 dihydrochloride
Cat.No: T36673
Synonym:
Target:
Rupatadine
Cat.No: T36618
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6569 Mimosine

Leucenine,NSC 69188,含羞草素,Leucenol,L-Mimosine

Others Others
Mimosine (Leucenol) 是一种酪氨酸类似物,具有抗癌和抗炎等活性。它可通过其强大的铁结合活性作为抗氧化剂,是一种 Fe(III) 螯合剂。它作用于人类白血病细胞,通过金属离子螯合、线粒体激活和诱导活性氧产生来诱导细胞凋亡。
T4S1102 Liensinine diperchlorate

莲心碱高氯酸盐,莲心碱二高氯酸盐,Liensinine-Perchlorate

Mitophagy; Others; Autophagy Autophagy; Others
Liensinine Diperchlorate 是从芙蕖种子胚中提取的一种异喹啉生物碱。它通过阻断自噬小体-溶酶体融合来抑制晚期自噬,具有抗心律不齐、抗高血压、抗肺纤维化和血管平滑肌松弛等生物学活性。
TN1936 Mogroside III-E

罗汉果皂苷ⅢE

IL Receptor; TNF; TLR Apoptosis; Immunology/Inflammation
Mogroside IIIe 是一种葫芦烷型化合物,从罗汉果中分离得到,可抑制 NO 的释放,具有抗肺纤维化作用。
T3795 Corilagin

Apoptosis; TLR; Reverse Transcriptase; Antibacterial; Autophagy Apoptosis; Autophagy; Immunology/Inflammation; Microbiology/Virology
Corilagin 是一种鞣酸,有抑制 RNA 肿瘤病毒逆转录酶的活性。它抑制金黄色葡萄球菌的生长,MIC 为 25 μg/mL。它有抗肿瘤活性,可用于肝癌和卵巢癌。
T6S1049 Wilforine

ATPase Membrane transporter/Ion channel
Wilforine 是一倍半萜吡啶化合物,T. wilfordii 植物中的重要生物活性化合物,可有效治疗特发性肺纤维化。它具有抗炎和杀虫活性。
TN3469 Aucuparin

2,6-dimethoxy-4-phenylphenol

NADPH-oxidase Immunology/Inflammation
Aucuparin (2,6-dimethoxy-4-phenylphenol) 是一种植物抗菌素,具有抗炎活性。 在博来霉素 (BLM) 诱导的肺纤维化小鼠模型中,Aucuparin 抑制肺纤维化。 在经ABTS 和FRAP 测定显示出明显的清除活性。 Aucuparin 对fmlp 诱导的人中性粒细胞产生超氧化物具有明显的抑制作用,其IC50为17.0μM。
T5S0896 Loureirin A

龙血素 A,龙血素A

Akt; PI3K Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
Loureirin A 是一种黄酮类物质,从龙血树中分离得到,能够降低Akt 的磷酸化,具有抗血小板聚集作用。
T5S0018 Betulonic acid

路路通酸,(+)-Betulonic acid,Betunolic acid,Liquidambaric acid

Parasite; HSV Microbiology/Virology
Betulonic acid (Liquidambaric acid) 是一种在许多植物中存在的三萜类天然产物,具有抗肿瘤,抗炎,抗寄生虫和抗病毒的活性。
T2S2043 Dracorhodin perchlorate

Dracorhodin perochlorate,血竭素高氯酸盐,Dracohodin perochlorate

Apoptosis; Others Apoptosis; Others
Dracorhodin perchlorate 是来源于中药血竭的一种天然产物。它抑制细胞生长,并以剂量和时间依赖性方式诱导成纤维细胞凋亡,将细胞周期阻滞在 G1 期,可作为抗乳腺癌的候选药物。
T3753 Sinapinic Acid

Sinapic acid,芥子酸,Synapoic acid

Apoptosis; RAAS; Reactive Oxygen Species; HDAC Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Endocrinology/Hormones; Immunology/Inflammation; Metabolism; NF-κB
Sinapinic Acid (Synapoic acid) 是从 Hydnophytum formicarumJack. 根中分离到的酚类,是HDAC 抑制剂,对ACE-I 的活性也有抑制作用。它有抗肿瘤活性,诱导肿瘤细胞凋亡,具有抗氧化、抗糖尿病的作用。
T4S0797 Berberine

小檗碱,Berberin,Umbellatine,黄连素

Reactive Oxygen Species; Topoisomerase; Endogenous Metabolite; Antibacterial; Antibiotic; Autophagy Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB
Berberine (Umbellatine) 是从中草药黄连中分离出来的一种生物碱抗生素。它诱导活性氧生成并抑制 DNA 拓扑异构酶,具有抗肿瘤特性。
T10554 Bixin

Others Others
Bixin is isolated from the seeds of Bixa orellana and possesses anti-tumor, anti-inflammatory, and antioxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation, and ROS generation.

天然产物

Mimosine
Cat.No: T6569
Synonym: Leucenine,NSC 69188,含羞草素,Leucenol,L-Mimosine
Target: Others
Liensinine diperchlorate
Cat.No: T4S1102
Synonym: 莲心碱高氯酸盐,莲心碱二高氯酸盐,Liensinine-Perchlorate
Target: Mitophagy, Others, Autophagy
Mogroside III-E
Cat.No: TN1936
Synonym: 罗汉果皂苷ⅢE
Target: IL Receptor, TNF, TLR
Corilagin
Cat.No: T3795
Synonym:
Target: Apoptosis, TLR, Reverse Transcriptase, Antibacterial, Autophagy
Wilforine
Cat.No: T6S1049
Synonym:
Target: ATPase
Aucuparin
Cat.No: TN3469
Synonym: 2,6-dimethoxy-4-phenylphenol
Target: NADPH-oxidase
Loureirin A
Cat.No: T5S0896
Synonym: 龙血素 A,龙血素A
Target: Akt, PI3K
Betulonic acid
Cat.No: T5S0018
Synonym: 路路通酸,(+)-Betulonic acid,Betunolic acid,Liquidambaric acid
Target: Parasite, HSV
Dracorhodin perchlorate
Cat.No: T2S2043
Synonym: Dracorhodin perochlorate,血竭素高氯酸盐,Dracohodin perochlorate
Target: Apoptosis, Others
Sinapinic Acid
Cat.No: T3753
Synonym: Sinapic acid,芥子酸,Synapoic acid
Target: Apoptosis, RAAS, Reactive Oxygen Species, HDAC
Berberine
Cat.No: T4S0797
Synonym: 小檗碱,Berberin,Umbellatine,黄连素
Target: Reactive Oxygen Species, Topoisomerase, Endogenous Metabolite, Antibacterial, Antibiotic, Autophagy
Bixin
Cat.No: T10554
Synonym:
Target: Others
TargetMol Loading
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