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Cat. No. | Product Name | ||
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L3800 | NF-κB 通路分子库 | 729 compounds | |
729 个 NF-κB 信号通路相关的小分子化合物的特有集合,用于高通量、高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T14847 |
B I09
|
Others; IRE1 | Cell Cycle/Checkpoint; Others |
B I09是一种 IRE-1 RNase 抑制剂,IC50为1230 nM,对人 WaC3细胞中 XBP1 mRNA 的剪接和 LPS 刺激的 B 细胞中 xbp -1的表达有抑制作用。B I09可用于 CLL 细胞模拟XBP-1缺陷的研究。 | |||
TD0099 |
Malachite green oxalate
|
Apoptosis; Others; IκB/IKK; NF-κB | Apoptosis; NF-κB; Others |
Malachite green oxalate 是一种三苯基甲烷染料,可用于检测酶促反应中磷酸盐的释放。它也是一种选择性IKBKE 抑制剂,在体内外均表现出抗肿瘤活性。 | |||
T25465 |
GS143
GS-143,GS 143 |
IκB/IKK; E1/E2/E3 Enzyme; NF-κB | NF-κB; Ubiquitination |
GS-143 是选择性的IκBα泛素化抑制剂,抑制 SCFβTrCP1介导的IκBα泛素化作用,IC50=5.2 μM。GS143 抑制NF-κB 的活化和靶基因的转录,并且不抑制蛋白酶体的特性,并具有抗哮喘作用。 | |||
T1934 |
Bay 11-7085
BAY 11-7083 |
Apoptosis; IκB/IKK; Ferroptosis; NF-κB | Apoptosis; NF-κB |
Bay 11-7085 抑制NF-κB 激活和IκBα磷酸化,其稳定 IκBα 的IC50值为 10 μM。 | |||
T1902 |
BAY 11-7082
BAY 11-7821 |
Apoptosis; Others; IκB/IKK; DUB; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; NF-κB; Others; Ubiquitination |
BAY 11-7082 (BAY 11-7821) 是一种 NF-κB 抑制剂,可抑制 TNFα 诱导的 IκBα 磷酸化 (IC50=10 μM)。BAY 11-7082 也是一种泛素特异性蛋白酶 USP7 和 USP21 的抑制剂 (IC50=0.19/0.96 μM)。 | |||
T6141 |
IMD-0354
IKK2 Inhibitor V,IMD 0354 |
IκB/IKK | NF-κB |
IMD-0354 (IKK2 Inhibitor V) 是一种选择性IKKβ抑制剂,能够抑制 NF-κB 活性。它能够抑制 TNF-α 诱导的 NF-κB 转录活性,IC50=1.2 μM。 | |||
T125120 |
Cyclo(L-Pro-L-Val)
|
IκB/IKK; NOS; NF-κB; COX; Antibacterial | Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB |
Cyclo(L-Pro-L-Val) 是从辣椒溶杆菌AZ2和白斑分枝杆菌果实中提取出的 2,5-二酮哌嗪,具有抗炎活性,对植物病原微生物 (如 R. fascians LMG 3605) 具有毒性活性,能抑制革兰氏阳性植物病原菌。Cyclo(L-Pro-L-Val) 以浓度依赖性方式显著抑制了IKKα、IKKβ、IκBα和NF-κB 的磷酸化以及iNOS 和COX-2的活化,是治疗炎症相关疾病的潜在治疗剂。 | |||
T1930 |
JSH-23
|
NF-κB | NF-κB |
JSH-23 是NF-κB 抑制剂,作用于脂多糖刺激的巨噬细胞 RAW 264.7,抑制 NF-κB 转录活性(IC50=7.1 μM),抑制 NF-κB p65 的核易位而不影响 IκBα 降解。 | |||
T28210 |
NSC663627
|
Others | Others |
NSC663627 is an IκBα phosphorylation inhibitor. | |||
TP1961 |
PR-39
PR 39 (porcine) |
||
Antibacterial peptide. Stimulates angiogenesis and inhibits inflammatory responses by selectively blocking proteasome degradation of IκBα. | |||
T34632 |
SH-5
SH5 PIA5. LchiroInositol 1deoxy6Omethyl 5(2R)2methoxy3(octadecyloxy)propyl hydrogen phosphate. Akt inhibitor II |
Others | Others |
SH-5 是一种AKT抑制剂,通过抑制IκBα激酶激活调节的抗凋亡、增殖和转移基因产物,增强细胞凋亡并抑制侵袭。 | |||
T23693 |
AKCI
|
Others | Others |
AKCI is a PPI inhibitor that acts by targeting the AURKC-IκBα interaction. | |||
T71747 |
IKKß-IN-124
|
Others | Others |
IKKß-IN-124 is an allosteric inhibitor of IκBα phosphorylation and NF-κB transcriptional activity through selective capture of the inactive conformation and hence blockade of IKKβ S177/S181 phosphorylation. | |||
T63107 |
Anti-inflammatory agent 6
|
Others | Others |
Anti-inflammatory agent 6 能够阻断作为炎症关键控制器的 Iκb 激酶 α/β(IKKα/β)、IκBα 和核因子 kB p65(NF-κb p65)的磷酸化,表现出抗炎潜力。 | |||
T78816 |
Anti-osteoporosis agent-4
|
NF-κB | NF-κB |
Anti-osteoporosis agent-4 (Compound 11h) 在生物医学领域中表现为有效抑制原代破骨细胞的分化,减弱RANKL诱导的破骨细胞生成,并展示出强抑制作用,具有 IC50 值为358.29 nM。此外,该化合物还能抑制关键的 PI3K/AKT 和 IκBα/NF-κB 信号通路激活,表明其在防治骨质疏松症中的潜在应用价值。 | |||
TP1961L |
PR 39 (porcine) acetate
|
Proteasome; Antibacterial | Microbiology/Virology; Proteases/Proteasome; Ubiquitination |
PR 39 (porcine) acetate 是一种非竞争性、可逆的变构蛋白酶体抑制剂。 它可逆地与蛋白酶体的 α7 亚基结合,并通过泛素-蛋白酶体途径阻断 NF-κB 抑制剂 IκBα 的降解。 | |||
T60868 |
NF-κB-IN-4
|
Others | Others |
NF-κB-IN-4 (化合物 17) 是有效的NF-κB 通路抑制剂,可透过血脑屏障(BBB)。NF-κB-IN-4 具有潜在的抗神经炎症活性,毒性低,可用于研究神经炎症相关疾病。NF-κB-IN-4 可阻断 IκBα 的活化及磷酸化,降低 NLRP3 的表达,从而抑制NF-κB 的激活。 | |||
T75870 |
PR-39 TFA
|
||
PR-39 TFA 是富含脯氨酸和精氨酸的天然抗菌肽,是一种非竞争性,可逆和变构的蛋白酶体 (proteasome) 抑制剂。PR-39 TFA 可逆地结合到蛋白酶体的 α7 亚基上,并通过泛素-蛋白酶体途径阻断 NF-κB 抑制剂 IκBα 的降解。PR-39 TFA 刺激小鼠的血管生成,抑制炎症反应并显着减小心肌梗死面积。 | |||
T36191 |
CAY10681
|
Others | Others |
Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling. It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53. CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65. It blocks the proliferation of cancer cell lines (IC50s range from 33 to 37 μM). CAY10681 exhibits excellent oral bioavailability and... | |||
T79671 |
NF-κB-IN-11
|
NF-κB | NF-κB |
NF-κB-IN-11(Compound 3i)是一种抑制剂,有效抑止TNF-α诱发的NF-κB信号通路激活及其核内转移。此化合物通过下调IKK、IκBα和NF-κBp65的磷酸化水平,展现出显著的抗炎作用,并能缓解小鼠的DSS引起的结肠炎症状。口服给药的NF-κB-IN-11在小鼠急性毒性测试中显示出其最大耐受剂量(MTD)超过1852 mg/kg。 | |||
T37644 |
Bengamide B
|
Others | Others |
Potent inhibitor of NF-κB activation (IC50 = 85 nM); decreases IκBα phosphorylation. Attenuates LPS-induced nitric oxide production and expression of TNF-α, IL-6 and MCP. Suppresses proliferation of HeLa and HCT116 cells. Anti-inflammatory and antitumor. Hu et al (2007) Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases. Chem.Biol. 14 764 PMID:17656313 |Johnson et al (2012) Myxobacteria versus sponge-derived alkaloids: the be... | |||
T78730 |
TNF-α-IN-11
|
Others | Others |
TNF-α-IN-11 (Compound 10)是一种TNF-α抑制剂, KD值为12.06 μM。该化合物通过结合TNF-α并阻断其诱发的caspase和NF-κB信号通路激活,来实现其抑制作用。其具体机制包括抑制IκBα磷酸化和NF κB p65的核转位,适用于研究TNF-α介导的自身免疫性疾病。 | |||
T35773 |
Gliotoxin-13C13
Gliotoxin-13C13 |
Others | Others |
Gliotoxin-13C13is intended for use as an internal standard for the quantification of gliotoxin by GC- or LC-MS. Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains ofAspergillusand other fungi with diverse biological activities.1,2,3,4,5,6,7,8It inhibits 20S proteasomal chymotrypsin activity (IC50= 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.2,3Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutr... | |||
T36192 |
CAY10682
|
Others | Others |
(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway. It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKK (IC50s = 80.5, 78.2, and 57.1... | |||
T36486 |
Benpyrine
|
Others | Others |
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... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1637 |
Eurycomalactone
|
Anti-infection; NF-κB | Microbiology/Virology; NF-κB |
Eurycomalactone 是一种NF-κB 抑制剂,IC50=0.5 μM,是一种天然产物。它可抑制蛋白合成,降低 cyclin D1 蛋白水平,但对 TNFα 诱导的 IκBα 降解或 IKKα/β 和 IκBα 的磷酸化水平没有作用。 | |||
T3384 |
Wedelolactone
蟛蜞菊内酯,IKK Inhibitor II |
Apoptosis; NF-κB; Lipoxygenase; Caspase | Apoptosis; Metabolism; NF-κB; Proteases/Proteasome |
Wedelolactone (IKK Inhibitor II) 是来自旱莲草的一种天然产物,通过阻断 IκBα 的磷酸化和降解来抑制细胞中 NF-κB 介导的基因转录,具有抗癌,抗炎和抗氧化活性。 | |||
T2947 |
Indole-3-carbinol
吲哚-3-甲醇,I3C,3-Indolemethanol,3-吲哚甲醇,Indole-3-Methanol |
E1/E2/E3 Enzyme; NF-κB; Aryl Hydrocarbon Receptor; Endogenous Metabolite; p53 | Apoptosis; Immunology/Inflammation; Metabolism; NF-κB; Ubiquitination |
Indole-3-carbinol (I3C) 是樟子松中的一种天然产物,是可口服的硫代葡萄糖苷葡糖苷酶裂解产物。它是芳烃受体 (AhR) 的激动剂,可抑制 NF-κB 和 IκBα 激酶活化。 | |||
T4237 |
Rubiadin-1-methyl ether
Rubiadin 1-methyl ether,3-羟基-1-甲氧基-2-甲基蒽醌 |
Anti-infection; NF-κB | Microbiology/Virology; NF-κB |
Rubiadin-1-methyl ether (Rubiadin 1-methyl ether) 是一种巴戟天中的蒽醌类化合物,能够抑制 NF-κB p65 的磷酸化和 IκBα 的降解以及减少 p65 的核转位,阻碍破骨细胞的骨吸收。 | |||
T13265 |
Urolithin B
尿石素B,3-羟基-6H-苯并[C]苯并吡喃-6-酮 |
ERK; NF-κB; Akt; Endogenous Metabolite; JNK; AMPK | Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Metabolism; NF-κB; PI3K/Akt/mTOR signaling |
Urolithin B 是一种 ellagitannins 的肠道微生物代谢产物,具有抗炎和抗氧化作用。它也是骨骼肌质量的调节因子,通过减少 IκBα 的磷酸化和降解来抑制 NF-κB 活性,并抑制 JNK、ERK 和 Akt 的磷酸化,并增强 AMPK 的磷酸化。 | |||
T5688 |
Micheliolide
|
NOS; NF-κB; COX | Immunology/Inflammation; Neuroscience; NF-κB |
Micheliolide 是一种倍半萜内酯,能够抑制各种炎症反应。它能减弱高糖刺激的NF-κB 活化,IκBα的降解,和MCP-1,TGF-β1,FN 在鼠系膜细胞的表达。 | |||
T2913 |
Schisantherin A
五味子酯甲,Schisanwilsonin H,Gomisin-C,Wuweizi ester-A,Schizantherin-A,Arisanschinin K |
NF-κB | NF-κB |
Schisantherin A (Wuweizi ester-A) 是一种利用 IκBα 降解,抑制p65-NF-κB 易位进入细胞核的木脂素。 | |||
T4S1615 |
Sanggenon C
桑根酮C,桑根酮 C,Sanggenone C |
NF-κB | NF-κB |
Sanggenon C (Sanggenone C) 是一种从桑属的根皮中分离得到的黄烷酮 Diels-Alder 加合物化合物。它可抑制NF-κB 活性,抑制 RAW264.7 细胞中诱导型一氧化氮合酶的表达,以及肿瘤坏死因子-α 刺激的细胞粘附和血管细胞粘附分子-1 的表达。 它具有抗氧化和抗炎作用,也有抑制胰脂肪酶作用。 | |||
T5S2059 |
Glaucine
|
Calcium Channel; Dopamine Receptor; Influenza Virus; Adrenergic Receptor; PDE | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience |
Glaucine 是从海罂粟中分离的一种生物碱,具有镇咳、抗炎和支气管扩张作用。它是具有口服活性的磷酸二酯酶 4 选择性抑制剂。它还是非选择性的 α-肾上腺素受体拮抗剂,具有抗氧化和抗病毒活性。 | |||
T7030 |
anemarsaponin B
知母皂苷B,知母皂苷 B |
p38 MAPK; NF-κB; MEK; COX; NO Synthase | Immunology/Inflammation; MAPK; Neuroscience; NF-κB |
Anemarsaponin B 是一种甾体皂苷,可降低iNOS 和COX-2的蛋白和 mRNA 水平,减少促炎细胞因子的表达和产生。它通过阻断 IκBα 的磷酸化来抑制NF-κB 的 p65 亚基的核转位,还抑制 MAP 激酶激酶 3/6 (MKK3/6) 和混合谱系激酶 3 的磷酸化。 | |||
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。 | |||
TN1485 |
Chicanine
|
Others; NF-κB; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; NF-κB; Others |
Chicanine has anti-inflammatory activity in macrophages by down-regulating LPS-induced inflammatory cytokines in IκBα±/MAPK/ERK signaling pathways. | |||
T21577 |
Narasin (sodium salt)
Naracin sodium salt,naransin sodium,海南霉素,HainanMycin |
NF-κB | NF-κB |
Narasin (sodium salt) (HainanMycin) 通过神经胶质瘤细胞中的 ER 应激诱导肿瘤坏死因子相关凋亡诱导配体 (TRAIL) 介导的细胞凋亡,并通过抑制 IκBα 的磷酸化来抑制 NF-κB 信号传导。 | |||
T72208 |
1-Dehydro-[10]-gingerdione
|
Others | Others |
1-Dehydro-[10]-gingerdione 通过靶向IKKβ的激活环直接抑制 IKKβ 活性,从而破坏用激动剂刺激的巨噬细胞中 IKKβ 催化的 IκBα 磷酸化。1-Dehydro-[10]-gingerdione 抑制 LPS 诱导的NF-κB 转录活性。1-Dehydro-[10]-gingerdione 具有用于NF-κB 相关炎症和自身免疫性疾病研究的潜力。 |