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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T78707 IL--IN-2

IL--IN-2为大麻酚衍生物,该化合物作为IL-抑制剂表现出优良效力,兼具抗炎及镇痛特性。
T77675 TNKS-2-IN-1

PARP; Wnt/beta-catenin; Antibiotic Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Microbiology/Virology; Stem Cells
TNKS-2-IN-1 是一种 TNKS-2 抑制剂。TNKS-2-IN-1 对 TNKS-1 和 TNKS-2有抑制作用,IC50 分别为 259 nM 和 1100 nM。TNKS-2-IN-1 具有抗菌活性,对大肠杆菌和金黄色葡萄球菌具有抑制作用。TNKS-2-IN-1 抑制 NLRP3 炎症小体 (IC505μM)通过抑制ATP刺激的J1A.774细胞释放IL-
T28958 TG6-129

TG6 129

Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation
TG6-129 是有效的EP2受体选择性拮抗剂,可降低 butaprost 诱导的 P388D1 巨噬细胞中炎症因子的表达。
T77579 JC2-11

IL Receptor; Dehydrogenase; ROS; Caspase; NOD-like Receptor (NLR); AIM2 Apoptosis; Immunology/Inflammation; Metabolism; Proteases/Proteasome
JC2-11 是一种对炎症有抑制作用的化合物。JC2-11 对含有募集结构域的蛋白质 NLRC 4、黑色素瘤 2 中缺失 (AIM 2) 和非典型 (NC) 炎症小体有抑制作用,通过破坏活性氧的产生和 caspase-1 的活性来抑制炎症小体的活化。JC2-11 减少了炎症小体中 caspase-1 (p20) 的分泌、gasdermin D (GSDMD) 的裂解、IL- 和乳酸脱氢酶 (LDH) 的释放。
T38361 GSK717

IL Receptor; NOD Immunology/Inflammation; NF-κB
GSK717 是 NOD2(核苷酸结合寡聚结构域 2) 的选择性抑制剂。它抑制壁酰二肽 (MDP) 诱导的 NOD2 介导的信号转导,抑制 MDP 刺激的 HEK293/hNOD2 细胞分泌 IL-8 (IC50为 400 nM)。
T79256 DPP-4-IN-8

DPP-4-IN-8 (compound 27) 是一种高效的选择性DPP4抑制剂,具有 0.96 μM 的 Ki。该化合物能够抑制 Caco-2 和 HepG-2 细胞中的 DPP4 二肽酶活性,并剂量依赖性地降低 TNF-α、IL-6 和 IL- 的表达水平[1]。
T38106 JC-171

JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin- (IL-) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL- production in primary macrophages dose dependently[1]. ...
T61621 IMMH001

IMMH001, also known as SYL930, is an orally active compound that exhibits potent selectivity as an agonist for the S1P1 receptor, which is the sphingosine-1-phosphate receptor 1. This compound effectively reduces the levels of various chemokines and proinflammatory cytokines, such as IL-, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 finds utility in research focused on rheumatoid arthritis (RA) [1] [2].
T63943 COX-2-IN-10

COX-2-IN-10 是 COX-2 的有效抑制剂。COX-2-IN-10 对 IL-6、TNF-α 和 IL- 的产生表现出抑制作用。COX-2-IN-10 能够浓度依赖性地抑制 PGE2 的产生,其 IC50 值为 2.54 μM。COX-2-IN-10 在 mRNA 和蛋白水平上抑制 iNOS 和 COX-2 的表达。
T62221 NLRP3-IN-8

NLRP3-IN-8 (compound 27) 是具有口服活性的、与 NLRP3直接结合的 NLRP3炎性体抑制剂,对 IL- 的 IC50值为1.23 μM. NLRP3-IN-8 对肝微粒体具有良好的代谢稳定性 (t1/2= 138.63 min),几乎没有毒性 (against L02: IC50> 100 μM) 。
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- 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...
T9655 NBC 6

NLRP3-IN-NBC6 是一种有效的选择性 NLRP3炎性小体抑制剂 ,IC50为574 nM,其作用独立于 Ca2+。NLRP3-IN-NBC6 抑制 Nigericin 诱导的 THP-1 细胞炎症反应和 Imiquimod 诱导的 LPS-primed 的骨髓源性巨噬细胞 (BMDMs) 释放 IL-
T68738 (±)-γ-Tocopherol

(±)-γ-Tocopherol is a form of vitamin E with antioxidant and anti-inflammatory properties. It traps and detoxifies reactive nitrogen oxide species, including nitrogen dioxide, in cell-free assays. It also reduces the synthesis of prostaglandin E2 (PGE2) induced by LPS in RAW 264.7 macrophages and by IL- in A549 cells. (±)-γ-Tocopherol inhibits LPS-induced nitrite release and inducible nitric oxide synthase (iNOS) expression in RAW 264.7 cells and reduces COX-2 activity in A549 cells pretreated...
T37590 ML 3403

p38 MAPK inhibitor (IC50 = 0.38 μM). Inhibits the release of IL- and TNF-α in a peripheral blood mononuclear cell (PBMC) assay (IC50 values are 0.039 and 0.16 μM respectively). Laufer et al (2003) Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J.Med.Chem. 46 3230 PMID:12852754 |Kammerer et al (2007) Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-...
T79304 Semapimod

CPSI-2364,CNI-1493 free base

Semapimod是一种抑制促炎细胞因子产生的化合物,具有抑制TNF-α、IL-IL-6功能。它通过抑制巨噬细胞的p38 MAPK以及一氧化氮的生成发挥作用,并且能够抑制TLR4信号传导(IC50约为0.3 μM)。Semapimod对于治疗各类炎症和自身免疫性疾病显示出潜在效用。
T82526 Drotrecogin alfa (activated)

Drotrecogin alfa activated (DrotAA)为重组人活化蛋白C(APC)。该化合物能够抑制由烟雾引起的大鼠肺微血管通透性上升及促炎细胞因子IL-水平增加,具有抗凝血与抗炎作用,并促进纤溶过程。Drotrecogin alfa activated主要用于重症脓毒症的实验研究。
T73852 Ac-YVAD-CHO acetate

Ac-YVAD-CHO(L-709049)醋酸盐是一种高效、可逆、特异的四肽白介素转化酶(ICE)抑制剂,小鼠和人类的Ki值分别为3.0 nM和0.76 nM。它同时也能抑制caspase-1,从而抑制成熟IL-lβ的产生。
T72017 6(5H)-Phenanthridinone

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimenta...
T36042 17(R)-HDHA

Resolvins are a group of polyhydroxylated metabolites of docosahexaenoic acid (DHA) found in the inflammatory exudates of aspirin-treated experimental animals. 17(R)-HDHA is the primary oxygenation product of DHA when exposed to aspirin-inhibited cyclooxygenase-2. 17(R)-HDHA serves as a precursor to resolvins and has intrinsic biological activity, such as the inhibition of TNFα-induced IL- expression in human glioma cells.
T36517 Resveratrol-3-O-sulfate sodium

Resveratrol-3-O-sulfate is a metabolite of resveratrol . In U-937 cells stimulated with LPS, resveratrol-3-O-sulfate (1 μM) decreases the expression of IL-1α, IL-, and IL-6 by 61.2, 76.6, and 42.2%, respectively, and decreases the release of TNF-α and IL-6 to similar levels as resveratrol. It has antioxidant activity in a Trolox assay, dose-dependently decreases growth of Caco-2 colorectal adenocarcinoma cells when used at concentrations ranging from 10 to 100 μM, and induces apoptosis at conc...
T83866 LCC-12 formate

LCC-12是一种铜(II)螯合剂,为二甲双胍的衍生物。作为单体,它能结合铜(II)并在20 µM的浓度下减少氢过氧化物依赖的NADH向NAD+的氧化。在10 µM的浓度下,LCC-12降低一次性人类细胞因子激活的单核衍生的巨噬细胞(MDMs)中IL-IL-2IL-6、IL-8和TNF-α的细胞因子水平,以及JAK2、STAT2IL-1受体相关激酶4(IRAK4)的水平。此外,同样浓度的LCC-12减少了细胞因子激活的MDMs中CD80+和CD86+的数量。每日0.3 mg/kg的剂量可提高LPS或盲肠结扎穿孔模型小鼠的存活率。
T68321 AS1940477

AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-, and IL-6 at low concentrations (LPS/TNFα, IC(50)=0.45n M; PHA/TNFα, IC(50)=0.40 nM). In addition, equivalent c...
T36629 Givinostat

Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL- production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL- secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1...
T82189 HMGB1-IN-2

HMGB1-IN-2 (compound 15) 是一种针对高度保守的核蛋白 HMGB1 的抑制剂,其在 RAW264.7 细胞中展现出 NO 抑制活性,IC50 为 20.2 μM。 HMGB1-IN-2 (30 μM) 能够减少 IL-、TNF-α、caspase-1 p20 的表达,并抑制 NF-κB p65 的磷酸化作用,显示出抗凋亡特性。在脓毒症急性肾损伤模型的小鼠中,HMGB1-IN-2(15 mg/kg;腹腔注射)可有效减轻肾脏伤害。此外,HMGB1-IN-2 对 Huh7 细胞和 A549 细胞的 IC50 分别为 77.0 μM 和 82.0 μM。
T83962 C 101248

C 101248是一种选择性且强效的小鼠和人类串联孔道卤素抑制K+通道1(THIK-1, IC50= 50 nM)抑制剂,对K2P家族成员TREK-1和TWIK-2以及Kv2.1无活性。C 101248能够阻断小鼠海马微胶质细胞中THIK-1 K+电流的整细胞膜片钳记录中的音调和ATP激发的电流。C 101248通过防止NLRP3依赖性IL-的释放,从而减少在分离的微胶质细胞中的神经炎症。
T83895 NCI 126224

NSC 126224

NCI 126224 是一种 toll-like receptor 4 (TLR4) 的拮抗剂。它在 RAW 264.7 巨噬细胞中,选择性抑制由 TLR4 激动剂 LPS 引起的一氧化氮 (NO) 产生(IC50 = 0.31 µM),而对 TLR7/8 激动剂 R-848、TLR1/2 激动剂 Pam3CSK4 以及 TLR3 激动剂 poly(I:C) 的影响较小;但对于相同细胞中由 TLR2/6 激动剂 FSL-1 引起的 NO 产生,其抑制作用在 0.6 µM 时亦显现。此外,NCI 126224 在 BV-2 微胶质细胞的报告实验中抑制了 LPS 引起的 NF-κB 活性,并在 RAW 264.7 巨噬细胞中降低了 LPS 引起的 IL- 和 TNF-α 水平(IC50s = 5.92, 0.42, 和 1.54 µM,分别)。
T83773 Prostaglandin E2 Inhibitor 3

PGE2 Inhibitor 3

Prostaglandin E2抑制剂3是一种microsomal prostaglandin E合酶-1 (mPGES-1; IC50 = 0.2 µM)的抑制剂,相较于COX-1、COX-2、5-lipoxygenase (5-LO)和soluble epoxide hydrolase (sEH),在10 µM的无细胞试验中表现出对mPGES-1的选择性。在10 µM和1 µM的浓度下,该抑制剂能抑制A549细胞中IL-诱导的PGE2生成以及在J774A.1巨噬细胞中,LPS诱导的IL-6和PGE2生成。同时,它还能抑制由钙离子载体A23187单独或结合花生四烯酸和A23187诱导的5-LO产物形成,包括白三烯B4 (LTB4) 和5-H(p)ETE(IC50s分别为4.9和5.2 µM)。在体内,10 mg/kg剂量的Prostaglandin E2抑制剂3能防止在zymosan诱导的小鼠腹膜炎模型中白细胞渗入腹腔液中。
T37052 Tetranactin

Tetranactin is a macrotetrolide and a monovalent cation ionophore that has been found in S. aureus and has antibacterial, insecticidal, and mitogenic activities. It exhibits an equilibrium permeability ratio 1,000-fold greater for lithium than sodium or cesium ions accross bilayer membranes at low voltages. Tetranactin inhibits the growth of Gram-positive bacteria and C. miyabeanus and R. solani fungi when used at concentrations less than 0.9 μg/ml. Tetranactin (0.5-1.5 μg per insect) dose-depen...
T36486 Benpyrine

Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research[1]. Benpyrine (5-20 μM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IκBα in RAW264.7 cells (stimulated with 10 ng/mL TNF-α or 1 μg/mL LPS). Benpyrine abo...
T38309 LL-37 amide (trifluoroacetate salt)

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. ...

化合物

IL--IN-2
Cat.No: T78707
Synonym:
Target:
TNKS-2-IN-1
Cat.No: T77675
Synonym:
Target: PARP, Wnt/beta-catenin, Antibiotic
TG6-129
Cat.No: T28958
Synonym: TG6 129
Target: Prostaglandin Receptor
JC2-11
Cat.No: T77579
Synonym:
Target: IL Receptor, Dehydrogenase, ROS, Caspase, NOD-like Receptor (NLR), AIM2
GSK717
Cat.No: T38361
Synonym:
Target: IL Receptor, NOD
DPP-4-IN-8
Cat.No: T79256
Synonym:
Target:
JC-171
Cat.No: T38106
Synonym:
Target:
IMMH001
Cat.No: T61621
Synonym:
Target:
COX-2-IN-10
Cat.No: T63943
Synonym:
Target:
NLRP3-IN-8
Cat.No: T62221
Synonym:
Target:
Rhein-13C4
Cat.No: T36408
Synonym: Rhein-13C4
Target:
NBC 6
Cat.No: T9655
Synonym:
Target:
(±)-γ-Tocopherol
Cat.No: T68738
Synonym:
Target:
ML 3403
Cat.No: T37590
Synonym:
Target:
Semapimod
Cat.No: T79304
Synonym: CPSI-2364,CNI-1493 free base
Target:
Drotrecogin alfa (activated)
Cat.No: T82526
Synonym:
Target:
Ac-YVAD-CHO acetate
Cat.No: T73852
Synonym:
Target:
6(5H)-Phenanthridinone
Cat.No: T72017
Synonym:
Target:
17(R)-HDHA
Cat.No: T36042
Synonym:
Target:
Resveratrol-3-O-sulfate sodium
Cat.No: T36517
Synonym:
Target:
LCC-12 formate
Cat.No: T83866
Synonym:
Target:
AS1940477
Cat.No: T68321
Synonym:
Target:
Givinostat
Cat.No: T36629
Synonym:
Target:
HMGB1-IN-2
Cat.No: T82189
Synonym:
Target:
C 101248
Cat.No: T83962
Synonym:
Target:
NCI 126224
Cat.No: T83895
Synonym: NSC 126224
Target:
Prostaglandin E2 Inhibitor 3
Cat.No: T83773
Synonym: PGE2 Inhibitor 3
Target:
Tetranactin
Cat.No: T37052
Synonym:
Target:
Benpyrine
Cat.No: T36486
Synonym:
Target:
LL-37 amide (trifluoroacetate salt)
Cat.No: T38309
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6S1579 Monotropein

水晶兰苷,Monotropeine

Others Others
Monotropein (Monotropeine) 是从Morinda officinalis 中获得,能够抑制硫酸葡聚糖硫酸钠诱导的结肠炎小鼠模型中炎性因子的表达。
T6S1597 Mulberroside A

桑皮苷 A,桑皮苷A

TNF; Tyrosinase; Interleukin Apoptosis; Immunology/Inflammation; Proteases/Proteasome
Mulberroside A 是桑中的一种主要活性成分,可降低TNF-α、IL-IL-6的表达,抑制 NALP3、caspase-1 和 NF-κB 的激活以及 ERK、JNK 和 p38 的磷酸化 。它抑制蘑菇酪氨酸酶,具有抗炎和抗细胞凋亡作用。
T6S0139 Neobavaisoflavone

Apoptosis; DNA/RNA Synthesis Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Neobavaisoflavone 是一种从Psoralea corylifolia 的种子中分离出来的类黄酮。它具有抗炎,抗癌和抗氧化的作用。它在中至高浓度下可抑制 DNA 聚合酶,也可抑制血小板聚集。
T2S0843 Negletein

黄芩素-7-甲醚,7-O-Methylbaicalein,Baicalein-7-methylether

IL Receptor; TNF; NOS; Interleukin Apoptosis; Immunology/Inflammation
Negletein (7-O-Methylbaicalein) 一种神经保护剂,可增强神经生长因子的作用并诱导 PC12 细胞中的神经突生长。它通过抑制TNF-α和IL-表现出抗炎活性,其 IC50值分别为 16.4 和 10.8 μM。它还具有抗菌、抗缺氧和抗阿尔茨海默病活性。
T6S0077 Byakangelicol

COX Immunology/Inflammation; Neuroscience
Byakangelicol 是一种分离自白芷的白三醇,能够抑制环加氧酶-2的表达及活性,从而减少白细胞介素-诱导的 A549 细胞中前列腺素 E2 的释放。它可用于研究气道炎症。
T6S1538 Neochlorogenic acid

新绿原酸,trans-5-O-Caffeoylquinic acid,Neochlorogenate,金银花,5-O-Caffeoylquinic acid

TNF; NF-κB; COX; Antibacterial; Interleukin Apoptosis; Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB
Neochlorogenic acid (trans-5-O-Caffeoylquinic acid) 是在干果和其他植物中发现的一种多酚类天然产物,可抑制iNOS 和COX-2蛋白表达,抑制TNF-α和IL-产生,还抑制磷酸化的NF-κB p65和p38 MAPK 活化。
T79970 Taxamairin B

Taxamairin B是有效的抗炎化合物,能显著抑制LPS诱导的RAW264.7细胞中促炎因子(TNF-α, IL-IL-6)表达及NO、ROS生成,并对LPS引起的急性肺损伤模型小鼠具有保护效果。

天然产物

Monotropein
Cat.No: T6S1579
Synonym: 水晶兰苷,Monotropeine
Target: Others
Mulberroside A
Cat.No: T6S1597
Synonym: 桑皮苷 A,桑皮苷A
Target: TNF, Tyrosinase, Interleukin
Neobavaisoflavone
Cat.No: T6S0139
Synonym:
Target: Apoptosis, DNA/RNA Synthesis
Negletein
Cat.No: T2S0843
Synonym: 黄芩素-7-甲醚,7-O-Methylbaicalein,Baicalein-7-methylether
Target: IL Receptor, TNF, NOS, Interleukin
Byakangelicol
Cat.No: T6S0077
Synonym:
Target: COX
Neochlorogenic acid
Cat.No: T6S1538
Synonym: 新绿原酸,trans-5-O-Caffeoylquinic acid,Neochlorogenate,金银花,5-O-Caffeoylquinic acid
Target: TNF, NF-κB, COX, Antibacterial, Interleukin
Taxamairin B
Cat.No: T79970
Synonym:
Target:
TargetMol Loading
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