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12

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T62060	NF-κB-IN-5
	NF-κB-IN-5 (化合物 4d) 是口服有效的靶向 NF-κB 抑制剂。NF-κB-IN-5 具有明显的抗肿瘤活性，抑制人癌细胞株，包括 HCT116、U87-MG、HepG2、BGC823、PC9，IC50分别为 5.35、2.81、2.83、2.02 和 3.90 μM。
T6611	NSC697923 2-[(4-methylphenyl)sulfonyl]-5-nitrofuran	E1/E2/E3 Enzyme	Ubiquitination
	NSC-697923 (2-[(4-methylphenyl)sulfonyl]-5-nitrofuran), a potent inhibitor of UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13), exhibits its role in inducing cell death in neuroblastoma (NB) cells through two distinct mechanisms. In p53 wild-type NB cells, NSC-697923 promotes the nuclear importation of p53, thereby triggering cell death. Meanwhile, in p53 mutant NB cells, NSC-697923 activates the JNK-mediated apoptotic pathway, leading to cell death. Additionally, NSC-697923 inhibits DNA damage ...
T39412	ACAT-IN-5
	ACAT-IN-5 (example 19) is a compound that functions as an inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT). By inhibiting ACAT, this compound effectively suppresses the transcription mediated by NF-κB.
T37026	Mesalamine impurity P
	Mesalamine impurity P is an impurity of Mesalamine . 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1]. [1]. Kyle Dammann, et al.PAK1 modulates a PPARγ/NF-κB cascade in intestinal inflammation.Biochim Biophys Acta. 2015 Oct;1853(10 Pt A):2349-60.
T83670	F1 TFA Tat-IKIP (46-60),Tat-Inhibitor of NF-κB Kinase-interacting Peptide
	F1是一种抗炎肽，由HIV-1 Tat蛋白质转导域与对应于抑制因子NF-κB激酶-相互作用肽（IKIP）46-60残基的15氨基酸肽链接而成。在5 µM浓度下，F1抑制了小鼠腹腔巨噬细胞中LPS诱导的IκB激酶α（IKKα）和IKKβ的磷酸化以及NF-κB（p65）的核内转移。在体内，F1（5 mg/kg）降低了LPS诱导的脓毒症小鼠模型中IL-6、TNF-α和IL-1β的血清水平，并增加了生存率。
T62111	Antioxidant agent-5
	Antioxidant agent-5 (compound D-6) 是一种有效的抗氧化剂。Antioxidant agent-5 能够抑制 oxLDL 诱导的 ROS 水平升高和 NF-κB 核转位。Antioxidant agent-5 对 oxLDL (氧化型低密度脂蛋白)诱导的 VECs 细胞凋亡 (apoptosis) 及 ICAM-1 和 VCAM-1 的表达表现出抑制作用。Antioxidant agent-5 可以激活 Nrf2/HO-1 抗氧化通路，对 oxLDL 诱导的内皮损伤表现出保护活性。
T35855	AAA
	AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension...
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...
T36713	Streptochlorin
	Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the productio...
T35672	SMU127
	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...
T35438	(5E)-7-Oxozeaenol
	(5E)-7-Oxozeaenol is a resorcylic acid lactone that has been found in the fungus MSX 63935 and has enzyme inhibitory and anticancer activities.1,2 It inhibits TGF-β-activated kinase 1 (TAK-1; IC50 = 1.3 μM).1 (5E)-7-Oxozeaenol inhibits proliferation of MCF-7, H460, SF-268, HT-29, and MDA-MB-435 human cancer cells with IC50 values of 4.9, 1.2, 5.6, 4.4, and 5.5 μM, respectively.2 \|1. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growt...
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...

化合物

Cat.No: T62060

Cat.No: T6611

Synonym: 2-[(4-methylphenyl)sulfonyl]-5-nitrofuran

Target: E1/E2/E3 Enzyme

Cat.No: T39412

Mesalamine impurity P

Cat.No: T37026

Cat.No: T83670

Synonym: Tat-IKIP (46-60),Tat-Inhibitor of NF-κB Kinase-interacting Peptide

Antioxidant agent-5

Cat.No: T62111

Cat.No: T35855

Cat.No: T36408

Synonym: Rhein-13C4

Cat.No: T36713

Cat.No: T35672

(5E)-7-Oxozeaenol

Cat.No: T35438

Cat.No: T36486

Cat. No.	Product Name	Target	Signaling Pathways
TN2143	3,7,4'-Trihydroxyflavone Resokaempferol,5-Deoxykampferol	DNA	DNA Damage/DNA Repair
	3,7,4'-Trihydroxyflavone(5-Deoxykampferol) 是从黄檀心材中分离得到的一种具有 DNA 断链活性的黄酮类化合物，可抑制 NF-κB 配体（RANKL）受体激活剂诱导的 RAW 264.7 细胞和骨髓巨噬细胞中的破骨细胞分化、肌动蛋白环形成和骨吸收。
TN1237	3-O-Methylgallic acid 3,4-Dihydroxy-5-methoxybenzoic acid,3-O-甲基没食子酸	Apoptosis; NF-κB; OCT; DNA/RNA Synthesis; STAT	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; JAK/STAT signaling; Membrane transporter/Ion channel; NF-κB; Stem Cells
	3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) 是一种花青素代谢产物，具有强大的抗氧化能力。它还诱导细胞凋亡并具有抗癌作用，可抑制 Caco-2 细胞增殖，IC50值为 24.1 μM。
T0646	5-Aminosalicylic Acid Mesalazine,5-ASA,5-氨基水杨酸,Mesalamine	NF-κB; Lipoxygenase; COX; Glutathione Peroxidase; Endogenous Metabolite; PAK; PPAR	Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB
	5-Aminosalicylic Acid (5-ASA) 是一种特异性的PPARγ激动剂，还抑制 p21-激活激酶1(PAK1) 和NF-κB，具有抗炎活性。
T3676	Sesamol 1,3-Benzodioxol-5-ol,3,4-Methylenedioxyphenol,芝麻酚	Apoptosis; AMPK	Apoptosis; Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	Sesamol (1,3-Benzodioxol-5-ol) 是芝麻油的主要成分，具有抗氧化和抗肿瘤活性。它是一种自由基清除剂，在 DPPH 实验中，IC50为 5.95±0.56 μg/mL。
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。
T4S2326	Cornuside 7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside	ERK; p38 MAPK; NF-κB; JNK	MAPK; NF-κB
	Cornuside (Comuside) 是从山茱萸的果实中分离出的环烯醚萜苷，可用于炎症疾病的研究和促进血液循环。它通过下调 MAPK 和 NF-κB 信号通路抑制肥大细胞介导的过敏反应，用于炎性过敏性疾病中的潜能。
TN1182	11-Keto-beta-boswellic acid 11-Keto-beta-boswellic acid,11-酮基-BETA-乳香酸	Leukotriene Receptor; NF-κB; Lipoxygenase	GPCR/G Protein; Metabolism; NF-κB
	11-Keto-beta-boswellic acid 是来自乳香的一种五环三萜酸，具有抗炎活性和剂量依赖性心脏保护作用，主要是由于抑制5-脂氧合酶、白三烯、NF-κB 的激活和肿瘤坏死因子 α 的产生。
T6S1315	Oroxylin A 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether	Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy	Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。
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。
T72429	α-Lipoic Acid sodium Thioctic acid sodium,DL-α-Lipoic acid sodium,Thioctic acid sodium ; (±)-α-Lipoic acid sodium ; DL-α-Lipoic acid sodium,(±)-α-Lipoic acid sodium
	α-Lipoic Acid (Thioctic acid) sodium 是一种抗氧化剂，是线粒体酶复合物的重要辅助因子。α-Lipoic Acid sodium 可抑制NF-κB 依赖性的HIV-1LTR 活化。α-Lipoic Acid sodium 诱导内质网应激 (ERS) 介导的肝癌细胞凋亡 (apoptosis)。α-Lipoic Acid sodium 可与CPUL1 合成自组装的纳米聚合体 CPUL1-LA NA，其抗肿瘤效果优于 CPUL1。
T4700	1,3,5-Trihydroxy-4-prenylxanthone
	1,3,5-Trihydroxy-4-prenylxanthone is a relatively potent inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 3.0 μM; it shows in vitro inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 valu
T37911	cis-Resveratrol 顺式白藜芦醇,(Z)-Resveratrol
	Resveratrol is a potent phenolic antioxidant found in grapes, red wine, and various berries that also has antiproliferative and anti-inflammatory activity. cis-Resveratrol is the double bond isomer of trans-resveratrol, the more often studied and naturally abundant of the two resveratrol isomers. cis-Resveratrol exhibits antioxidant activity in the &#181M range similar to that observed with trans-resveratrol. It blocks production of reactive oxygen species (ROS) by inhibition of NAD(P)H oxidase ...

天然产物

3,7,4'-Trihydroxyflavone

Cat.No: TN2143

Synonym: Resokaempferol,5-Deoxykampferol

Target: DNA

3-O-Methylgallic acid

Cat.No: TN1237

Synonym: 3,4-Dihydroxy-5-methoxybenzoic acid,3-O-甲基没食子酸

Target: Apoptosis, NF-κB, OCT, DNA/RNA Synthesis, STAT

5-Aminosalicylic Acid

Cat.No: T0646

Synonym: Mesalazine,5-ASA,5-氨基水杨酸,Mesalamine

Target: NF-κB, Lipoxygenase, COX, Glutathione Peroxidase, Endogenous Metabolite, PAK, PPAR

Cat.No: T3676

Synonym: 1,3-Benzodioxol-5-ol,3,4-Methylenedioxyphenol,芝麻酚

Target: Apoptosis, AMPK

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

Cat.No: T4S2326

Synonym: 7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside

Target: ERK, p38 MAPK, NF-κB, JNK

11-Keto-beta-boswellic acid

Cat.No: TN1182

Synonym: 11-Keto-beta-boswellic acid,11-酮基-BETA-乳香酸

Target: Leukotriene Receptor, NF-κB, Lipoxygenase

Cat.No: T6S1315

Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether

Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy

Ginsenoside Rg5

Cat.No: T6S1487

Synonym: 人参皂苷Rg5,人参皂甙 Rg5

Target: NF-κB, COX, IGF-1R

α-Lipoic Acid sodium

Cat.No: T72429

Synonym: Thioctic acid sodium,DL-α-Lipoic acid sodium,Thioctic acid sodium ; (±)-α-Lipoic acid sodium ; DL-α-Lipoic acid sodium,(±)-α-Lipoic acid sodium

1,3,5-Trihydroxy-4-prenylxanthone

Cat.No: T4700

cis-Resveratrol

Cat.No: T37911

Synonym: 顺式白藜芦醇,(Z)-Resveratrol

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