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Cat. No. | Product Name | Target | Signaling Pathways |
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T36097 | TNF-α-IN-2 | ||
TNF-α-IN-2 is a highly potent and orally bioavailable inhibitor of tumor necrosis factor alpha (TNFα), exhibiting an IC50 of 25 nM in the HTRF assay. It exerts its inhibitory effects by inducing conformational changes in the TNFα trimer upon binding, resulting in disrupted signaling when the trimer interacts with TNFR1. TNF-α-IN-2 holds promise as a valuable tool for investigating the pathogenesis of rheumatoid arthritis[1]. | |||
T64349 |
Necroptosis-IN-3
Cyclohexanecarboxamide, N-(2-thienylmethyl)- |
Necroptosis | Apoptosis |
Necroptosis-IN-3 (Cyclohexanecarboxamide, N-(2-thienylmethyl)-)(Compound 69) 是一种坏死性凋亡 (necroptosis) 抑制剂,抑制 TNF-α 诱导的坏死性凋亡。Necroptosis-IN-3(Compound 69) 也抑制 11β-HSD1。 | |||
T10865L |
Cot inhibitor-1 hydrochloride
Cot inhibitor-1 hydrochloride(915365-57-0 Free base) |
TNF; MAPK | Apoptosis; MAPK |
Cot inhibitor-1 hydrochloride 是肿瘤进展位点 2 激酶 (IC50 = 28 nM) 的抑制剂,可抑制人全血中 TNF-α 的产生 (IC50 = 5.7 nM)。 | |||
T10866 |
Cot inhibitor-2
|
TNF; MAPK | Apoptosis; MAPK |
Cot inhibitor-2 是一种 cot (Tpl2/MAP3K8) 抑制剂(IC50 : 1.6 nM),具有有效性,选择性和口服活性。Cot inhibitor-2 对LPS 刺激的人全血中 TNF-α 的产生具有抑制作用,IC50 为 0.3 μM。 | |||
T36524 |
IKK2-IN-4
5-Phenyl-2-ureidothiophene-3-carboxylic Acid Amide,IKK2 Inhibitor IV |
IκB/IKK; TNF | Apoptosis; NF-κB |
IKK2-IN-4 (IKK2 Inhibitor IV)是一种高效的 IKK-2 抑制剂,IC50 值为 25 nM。IKK2-IN-4 对 LPS 诱导的 PBMC 中 TNFα 的产生有抑制作用。 | |||
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。 | |||
T4092 |
AG126
Tyrphostin AG126,AG 126 |
ERK; COX | Immunology/Inflammation; MAPK; Neuroscience |
AG126 (Tyrphostin AG126) 是一种酪氨酸激酶抑制剂,可阻止丝裂原活化蛋白激酶 p42MAPK(ERK2) 的激活。 | |||
T15017 |
CU-T12-9
|
TLR | Immunology/Inflammation |
CU-T12-9 是特异性 TLR1/2激动剂,可激活先天免疫系统和适应性免疫系统。它选择性激活 TLR1/2 异二聚体,可通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号,引起下游 TNF-α、IL-10 和 iNOS 增加。 | |||
T7672 |
MD2-TLR4-IN-1
|
TLR | Immunology/Inflammation |
MD2-TLR4-IN-1 是一种骨髓分化蛋白 2/toll 样受体 4 (MD2-TLR4) 复合物抑制剂,能够抑制巨噬细胞 LPS 诱导的 TNF-α 和 IL-6 的表达,IC50值分别为 0.89 和 0.53 μM。 | |||
T24816 |
SP-100030
SP100030,SP 100030 |
NF-κB | NF-κB |
SP-100030 是一种有效的 NF-κB 和激活蛋白-1 (AP-1) 双抑制剂 (IC50 分别为 50 和 50 nM)。SP-10003 抑制 Jurkat 和其他T 细胞系产生的 IL-2、IL-8 和 TNF-α 的产生。SP-100030 降低小鼠胶原性关节炎 (CIA)。 | |||
T77097 | Nerelimomab | ||
Nerelimomab (BAYX1351) 是一种抗TNF-α抗体。Nerelimomab 可用于脓毒症研究。 | |||
T60357 |
NF-κB-IN-2
JEUD-38 |
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NF-κB-IN-2 抑制 PC-3细胞中 TNF-α诱导的的经典 NF-κB 信号传导。 | |||
T12203L |
Necrostatin 2
|
Others | Others |
Necrostatin 2 is an effective necroptosis inhibitor. Necrostatin 2 is also a RIPK1 inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. | |||
T79190 |
Homouridine
|
Nucleoside Antimetabolite/Analog | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Homouridine 是一种尿苷类似物,可作为中间体合成抑制剂 compound I(MMP-2 抑制剂, IC50=150 μM)。此外,Compound I (EP1338282) 也能抑制 TNF-α 与 TNF-αR1 的结合。 | |||
T37726 |
MMP-9 Inhibitor I
|
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MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively). It also decreases the activity of TNF-α converting enzyme (TACE) in a dose-dependent manner (IC50 = 0.54 μM). MMP-9 inhibitor I decreases TNF-α secretion stimulated by LPS in BV-2 microglial cells when used at concentrations of 50 and 100 μM. | |||
T76988 | Tanfanercept | ||
Tanfanercept (HL036337),一种抗TNF-α单克隆抗体,在干眼症(DE)小鼠模型中能有效改善角膜糜烂。 | |||
TP1962 |
Pam2CSK4
|
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Toll-like receptor 2/6 (TLR2/6) agonist. Induces TNF-α production in human mononuclear cells. Also induces proliferation and activation of mouse splenic B cells. | |||
T79256 |
DPP-4-IN-8
|
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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-1β 的表达水平[1]。 | |||
T72017 |
6(5H)-Phenanthridinone
|
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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-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimenta... | |||
T36401 | DCVC | ||
DCVC inhibits pathogen-stimulated TNF-α in human extra placental membranes in vitro.Target: TNF-αin vitro: DCVC inhibits pathogen stimulated cytokine release from tissue punch cultures. DCVC (5-50 μM) significantly inhibits LTA-, LPS-, and GBS-stimulated cytokine release from tissue cultures as early as 4 h (P ≤ 0.05). In contrast, TCA (up to 500 μM) does not inhibit LTA-stimulated cytokine release from tissue punches. DCVC effects on LTA-stimulated and LPS-stimulated TNF-α release from tissue p... | |||
T36486 |
Benpyrine
|
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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... | |||
T76963 |
Certolizumab pegol
|
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Certolizumab pegol (Certolizumab) 是经过重组和聚乙二醇化处理的人源化单克隆抗体抗原结合片段,它选择性地靶向并中和肿瘤坏死因子-α (TNF-α)。适用于类风湿关节炎和克罗恩病的研究领域。 | |||
T63943 |
COX-2-IN-10
|
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COX-2-IN-10 是 COX-2 的有效抑制剂。COX-2-IN-10 对 IL-6、TNF-α 和 IL-1β 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。 | |||
T37590 |
ML 3403
|
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p38 MAPK inhibitor (IC50 = 0.38 μM). Inhibits the release of IL-1β 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)-... | |||
T78508 |
Delmitide acetate
RDP-58 acetate |
IFNAR | Immunology/Inflammation |
Delmitide acetate (RDP58) 是一种 d-异构体十肽,具有抗炎活性和口服活性。该化合物能够抑制 TNF-α、IFN-γ 以及白细胞介素 (IL)-12 的生成,同时提高血红素加氧酶 1 的活性,可用于针对溃疡性结肠炎的研究。 | |||
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-1β和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。 | |||
T83734 |
PapRIV TFA
|
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PapRIV是最初从B. cereus分离出的一种群体感应七肽。它被转译为一个48-氨基酸多肽,由NprB蛋白酶在细胞外分泌和加工形成活性七肽。PapRIV(1-25 µM)在BV-2微胶质细胞中诱导IL-6和TNF-α的产生,并促使NF-κB转移。 | |||
T35406 |
α-MSH TFA
|
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α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube fo... | |||
T38002 | LEO 39652 | ||
LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) [1]. LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin... | |||
T83698 |
Cathelicidin-2 (128-153) (chicken) TFA
Fowlicidin-2 (128-153),CATH-2 (128-153),Myeloid Antimicrobial Peptide 27 (128-153) |
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Cathelicidin-2 (CATH-2) (128-153) 是一种合成抗菌肽,对应于鸡CATH-2的128至153个氨基酸。该化合物对E. coli、S. aureus、S. enteritidis和B. globigii展示出浓度依赖性的活性。CATH-2 (128-153) (40 µM) 可诱导孤立的鸡红细胞溶解,但对孤立的人外周血单个核细胞(PBMCs)无细胞毒性。它能促进化学因子(C-C-基序)配体2 (CCL2)的产生,并抑制LPS诱导的TNF-α、IL-6、IL-8和IL-10在孤立的人PBMCs中的产生。 | |||
T76945 | Cetrelimab | ||
Cetrelimab (JNJ 63723283; JNJ 3283) 为人源化IgG4κ单克隆抗体,专门针对PD-1。其与PD-1的结合Kd值为1.72 nM(在HEK293细胞中测得)。Cetrelimab有效阻断PD-1与其配体PD-L1和PD-L2的结合,其IC50值分别为111.7 ng/mL与138.6 ng/mL。此外,Cetrelimab能激活外周T细胞,提升细胞因子(IFN-γ, IL-2, TNF-α)的表达水平,进而抑制肿瘤在体内的生长。 | |||
T37289 |
Resolvin D2 n-3 DPA
Resolvin D2 n-3 DPA |
||
Resolvin D2 n-3 DPA (RvD2 n-3 DPA) is a specialized pro-resolving mediator (SPM).1It is formed from docosapentaenoic acid , an intermediate in the conversion of eicosapentaenoic acid to docosahexaenoic acid , in human leukocytes. RvD2 n-3 DPA (1 nM) reduces TNF-α-induced chemotaxis and adhesion of isolated human neutrophils.In vivo, RvD2 n-3 DPA (100 ng/animal; i.v.) reduces peritoneal neutrophil infiltration and exudate levels of IL-6 and chemokine (C-C motif) ligand 2 (CCL2) in a mouse model o... | |||
T83798 |
8-bromo NAD+ sodium
8-bromo Nicotinamide adenine dinucleotide,N(8-bromo-A)D+ |
||
8-bromo NAD+ 作为循环ADP-核糖(cADPR)抑制剂8-bromo cADPR的前药形式,通过CD38转化为8-bromo-cADPR。在1 mM浓度下,8-bromo NAD+ 阻止由N-formyl-Met-Leu-Phe (fMLP) 在分离的小鼠骨髓衍生的中性粒细胞内引起的细胞内钙水平增加和趋化作用。同时,在100 µM浓度下使用,减少了小鼠原代小胶质细胞中LPS诱导的亚硝酸盐产生以及TNF-α和IL-2的分泌。 | |||
T35812 |
CAY10591
CAY10591 |
||
Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This com... | |||
T37722 |
Diprovocim-1
|
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Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma mo... | |||
T71285 |
Metaxalone-d6
|
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Metaxalone-d6 is intended for use as an internal standard for the quantification of metaxalone by GC-or LC-MS. Metaxalone is a skeletal muscle relaxant. It inhibits the proliferation of, and induces apoptosis in, RAW 264.7 cells in vitro when used at concentrations ranging from 1 to 100 µM. Metaxalone also reduces LPS-induced increases in COX-1, COX-2, and NF-kB levels and inhibits LPS-induced production of TNF-α, IL-6, and prostaglandin E2 in RAW 264.7 cells. Formulations containing metaxalone ... | |||
T82189 |
HMGB1-IN-2
|
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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-1β、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。 | |||
T35864 |
T-5342126
|
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T-5342126 is a toll-like receptor 4 (TLR4) antagonist.1It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50= 27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s = 110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-depen... | |||
T35536 |
Tpl2 Kinase Inhibitor (hydrochloride)
|
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Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5... | |||
T36782 |
TAK1-IN-2
TAK1-IN-2 |
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TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM[1]. TAK1-IN-2 (compound 54) (10 μM) has no effect on cell viability in TNF-α stimulated HCT-15 cells[1]. [1]. Veerman JJN, et, al. Discovery of 2,4-1 H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562. | |||
T35929 |
O-Demethyl Apremilast
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O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral admi... | |||
T36408 |
Rhein-13C4
Rhein-13C4 |
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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... | |||
T36779 |
NG 25 (hydrochloride hydrate)
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NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectiv... | |||
T83895 |
NCI 126224
NSC 126224 |
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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-1β 和 TNF-α 水平(IC50s = 5.92, 0.42, 和 1.54 µM,分别)。 | |||
T36517 |
Resveratrol-3-O-sulfate sodium
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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-1β, 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... | |||
T35854 |
9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)
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9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-co... | |||
T35672 |
SMU127
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SMU127 is an agonist of the toll-like receptor 1/2 (TLR1/2) heterodimer.1It induces NF-κB signaling in cells expressing human TLR2 (EC50= 0.55 μM) but not cells expressing human TLR3, -4, -5, -7, or -8 when used at concentrations ranging from 0.1 to 100 μM. SMU127 induces the production of TNF-α in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 0.01 to 1 μM.In vivo, SMU127 (0.1 mg/animal) reduces tumor volume in a 4T1 murine mammary carcinoma m... | |||
T71303 |
Flufenamic Acid-d4
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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... | |||
T83866 |
LCC-12 formate
|
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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-1β、IL-2、IL-6、IL-8和TNF-α的细胞因子水平,以及JAK2、STAT2和IL-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。 | |||
T38309 |
LL-37 amide (trifluoroacetate salt)
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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. ... |
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。 | |||
TN6694 |
5,6-Benzoflavone
β-Naphthoflavone,beta-NF |
Antioxidant | oxidation-reduction |
5,6-Benzoflavone (β-Naphthoflavone) 是芳烃受体的外源配体,可破坏人肝癌 HepG2 细胞中的锌稳态。5,6-Benzoflavone (β-Naphthoflavone) 具有抗炎和抗氧化活性,抑制通过 AKT/Nrf-2/HO-1-NF-kappaB 信号转导轴,抑制 LPS 诱导的炎症,抑制TNF-α诱导的ICAM-1和VCAM-1表达,可用于研究神经退行性疾病。 | |||
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-1β和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。 | |||
T3763 |
Fumaric acid
Lichenic acid,Fumarate,2-Butenedioic acid,Trans-Butenedioic acid,反丁烯二酸,Donitic acid,Allomaleic acid,富马酸 |
Endogenous Metabolite | Metabolism |
Fumaric acid (2-Butenedioic acid) 与烟酸酶缺乏症相关,是癌症相关的内源性代谢物。 | |||
T5S0045 |
Isofraxidin
6,8-Dimethoxyumbelliferone,异秦皮啶,Phytodolor,异嗪皮啶 |
MMP; ERK; p38 MAPK; TLR; COX | Immunology/Inflammation; MAPK; Neuroscience; Proteases/Proteasome |
Isofraxidin (Phytodolor) 是来自刺五加的香豆素成分,抑制MMP-7表达和人肝癌细胞侵袭。它作用于肝癌细胞,抑制ERK1/2磷酸化。它减弱iNOS 和COX-2表达,还抑制TLR4/髓样分化蛋白 2 复合物的形成。 | |||
T6S0653 |
Linarin
Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷 |
TNF; AChE | Apoptosis; Neuroscience |
Linarin (Acacetin-7-O-rutinoside) 是一种选择性的乙酰胆碱酯酶 (AChE) 抑制剂,从薄荷花提取物中分离得到。 | |||
T6S1495 |
Ginsenoside Rk3
人参皂苷Rk3,人参皂甙 Rk3 |
Others; NF-κB | NF-κB; Others |
Ginsenoside Rk3 是存在于 Panax notoginseng 的根中。它能够抑制 HepG2 细胞中 TNF-α 诱导的 NF-κB 转录活性,IC50=14.24±1.30 μM。 | |||
T3826 |
Polygalasaponin F
异牡荆苷,瓜子金皂苷己 |
NF-κB; TLR; Akt; PI3K | Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; PI3K/Akt/mTOR signaling |
Polygalasaponin F 是从瓜子金中提取的齐墩果烷型三萜皂苷,可通过调节TLR4-PI3K/AKT-NF-kB 信号通路减少神经炎症细胞因子的分泌,能降低炎性细胞因子肿瘤坏死因子 α 的释放。 | |||
T4S2063 |
Tetrahydrocoptisine
人血草碱,STYLOPINE |
ERK; p38 MAPK; NF-κB | MAPK; NF-κB |
Tetrahydrocoptisine (STYLOPINE) 具有抑制炎症的有效作用。它通过抑制 NF-κB 信号通路对 LPS 诱导的 ALI 具有保护作用,这可能涉及抑制肺部炎症过程。它具有胃保护活性,归因于减少 NO 产生和调节促炎细胞因子,抑制中性粒细胞积累和 NF-κB 表达。它是一种活性抗炎成分,通过下调 NF-κB 活化、磷酸化 ERK1/2 和磷酸化-p38MAPK 信号通路抑制 TNF-α、IL-6 和 NO 的产生。 | |||
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-1β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。 | |||
T2S2264 |
Linalool
Linalol,(±)-Linalool,Phantol,沉香醇 |
Apoptosis; IL Receptor; TNF; Endogenous Metabolite; iGluR | Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Linalool (Linalol) 是存在芫荽等植物中的单萜类天然产物,是竞争性NMDA 受体拮抗剂,具有抗肿瘤和抗心脏毒性的作用。它通过激活 Nrf2 诱导抗氧化防御和通过抑制 NF-κB 减少炎症反应来保护其免受 LPS/GalN 诱导的肝损伤,具有镇痛、抗菌和抗炎的特性。 | |||
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。 | |||
T6S1917 |
Schisandrol B
Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B |
P450; Reactive Oxygen Species; Autophagy | Autophagy; Immunology/Inflammation; Metabolism; NF-κB |
Schisandrol B (Besigomsin) 是华中五味子的主要活性成分,具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生,也抑制 P-糖蛋白和CYP3A 的活性。 | |||
T4S1521 |
1,4-Dicaffeoylquinic acid
1,4-二咖啡酰奎宁酸,洋蓟素 |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
1,4-Dicaffeoylquinic acid 是一种苯丙素类物质,从苍耳子中获得,可以减少 LPS 诱导的 TNF-α 的生成,具有抗炎活性。 | |||
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-1β产生,还抑制磷酸化的NF-κB p65和p38 MAPK 活化。 | |||
T6S1487 |
Ginsenoside Rg5
人参皂苷Rg5,人参皂甙 Rg5 |
NF-κB; COX; IGF-1R | Immunology/Inflammation; Neuroscience; NF-κB; Tyrosine Kinase/Adaptors |
Ginsenoside Rg5 是红参的主要成分,可阻断IGF-1与其受体的结合,IC50约为90 nM。它还通过抑制NF-κB p65的 DNA 结合活性来抑制COX-2的 mRNA 表达。它可促进血管生成和改善高血压,具有抗炎和治疗阿尔茨海默病的潜力。 | |||
T4S1469 |
Cucurbitacin IIb
葫芦素IIB,雪胆素乙 |
Apoptosis; Others | Apoptosis; Others |
Cucurbitacin IIb 是一种雪胆中的活性成分。它阻碍 STAT3,JNK 和 Erk1/2 的磷酸化,提高 IκB 和 NF-κB (p65) 的磷酸化水平,抑制 NF-κB (p65) 的核转位,降低 IκBα 和 TNF-α 的 mRNA 水平。它能够诱导细胞凋亡,具有抗炎作用。 | |||
T6S2140 |
β-Anhydroicaritin
Anhydroicaritin,Beta-Anhydroicaritin,脱水淫羊藿素 |
MMP; Others; TNF; Interleukin | Apoptosis; Immunology/Inflammation; Others; Proteases/Proteasome |
β-Anhydroicaritin 是从乳香提取的一种天然产物,具有重要的生物学和药理学作用,如抗骨质疏松症,雌激素调节和抗肿瘤特性。它改善牙周组织的降解,抑制糖尿病大鼠 TNF-α 和 MMP-3 的合成和分泌。它抑制细胞内 Ca2+的升高,并显著降低 iNOS 蛋白的表达。 | |||
T6S1572 |
Sauchinone
|
ERK; p38 MAPK; NF-κB | MAPK; NF-κB |
Sauchinone 是一种从Saururus chinensis 中获得的非对映异构的木脂素。它通过抑制I-κBα磷酸化和p65核易位来抑制 LPS 诱导的 iNOS,TNF-α 和 COX-2 表达。它具有抗炎和抗氧化活性。 | |||
T3673 |
Mollugin
大叶茜草素,Rubimaillin |
HER; JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Mollugin (Rubimaillin) 是Rubia cordifolia L.中主要的生物活性成分。它能通过 p38-Smad 信号通路增强 BMP-2 的成骨作用。它通过抑制 TNF-α 诱导的 NF-κB 激活起抗癌疗效。 | |||
T35614 |
D-Trimannuronic acid
|
||
D-Trimannuronic acid is an alginate oligomer that originates from seaweed. It can induce TNF-α secretion by mouse macrophage cell lines, making it valuable in pain and vascular dementia research [1][2][3]. | |||
T75694 | Lacto-N-neotetraose | ||
Lacto-N-neotetraose (LNnT) 是一种内源性代谢物 (endogenous metabolite)。Lacto-N-neotetraose 可以抑制 TNF-α 诱导的未成熟上皮细胞中的IL-8分泌。Lacto-N-neotetraose 具有抗炎活性,可提高伤口愈合能力。 | |||
TN6539 | Pd-C-II | ||
Pd-C-II has anti-inflammation activity, it can inhibit TNF-α production and iNOS protein expression and inhibit COX-2 protein expression in LPS-stimulated RAW 264.7 cells. Pd-C-II inhibits anaphylactic mediator release from purified mast cells induced by | |||
TN3655 |
Cimiside E
|
ERK; TNF; ROS; Akt; PI3K; PKC; PPAR | Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Metabolism; PI3K/Akt/mTOR signaling |
Cimiside E has anti-inflammatory activity, it selectively inhibits TNF-α-induced expression of VCAM-1 at least by upregulation of PPAR-γ, and signals for ERK1/2, PI3K, and PKC are involved in this effect.Cimiside E may be an effective chemopreventive agen | |||
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-1β和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。 | |||
TN1094 |
Ginsenoside Rg6
人参皂苷Rg6,人参皂苷 Rg6 |
Apoptosis; NF-κB | Apoptosis; NF-κB |
Ginsenoside Rg6 抑制人淋巴瘤 JK 细胞增殖并诱导其凋亡,在 HepG2 细胞中抑制 TNF-α 诱导的 NF-κB 转录活性,IC50为 29.34 μM。 |