39
4
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0306 |
MLN120B
|
IκB/IKK | NF-κB |
MLN120B 是一种ATP 竞争性的、有效的、具有口服活性的IKKβ抑制剂,IC50=60 nM。它在体内外抑制多发性骨髓瘤细胞生长,也可用于研究类风湿关节炎。 | |||
T5540 |
GSK8612
|
IκB/IKK | NF-κB |
GSK8612 是一种具有高度选择性的TBK1强效抑制剂,其 pIC50=6.8。 | |||
T15564 |
IMD-0560
|
IκB/IKK | NF-κB |
IMD-0560 是新型 IκB kinase β抑制剂。 | |||
T5209 |
INH14
|
IκB/IKK | NF-κB |
INH14 是 IKKα (IC50:8.97 μM) / IKKβ (IC50:3.59 μM) 的抑制剂。它能够抑制 IKKα/β 依赖性 TLR 炎症反应,抑制 TAK1/TAB1 的下游和 NF-kB 信号通路。它具有抗炎和抗癌作用。 | |||
T6771 |
AZD3264
|
IκB/IKK | NF-κB |
AZD3264 是 IkB 激酶 IKK2抑制剂。 | |||
T1830 |
BX795
|
IκB/IKK; Chk; CDK; c-Kit; PDK; Autophagy | Autophagy; Cell Cycle/Checkpoint; NF-κB; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
BX795 是一种选择性PDK1抑制剂,也是相对特异性的TBK1和IKKɛ 抑制剂。它抑制 S6K1,Akt,PKCδ 和 GSK3β 的磷酸化,可调节自噬。 | |||
T10477 |
BAY-985
|
IκB/IKK | NF-κB |
BAY-985 是高效的、ATP 竞争性的、有口服活性的、选择性的TBK1和IKKε双重抑制剂,对 TBK1 (在低/高 ATP 实验中) 和 IKKε 的IC50分别为 2/30 和 2 nM。它具有抗肿瘤作用。 | |||
T7951 |
TBK1/IKKε-IN-5
|
IκB/IKK | NF-κB |
TBK1/IKKε-IN-5 是一种 TBK1 (IC50:1 nM) 和 IKKε (IC50:5.6 nM) 的双抑制剂。 | |||
T15559 |
TBK1/IKKε-IN-2
|
IκB/IKK | NF-κB |
TBK1/IKKε-IN-2 是双重TBK1和IKKε抑制剂。 | |||
T10237 |
ACHP Hydrochloride
IKK-2 Inhibitor VIII |
IκB/IKK | NF-κB |
ACHP Hydrochloride (IKK-2 Inhibitor VIII) 是选择性的IKK-β抑制剂 (IC50=5.8 nM)。 | |||
T8705 |
BOT-64
|
IκB/IKK | NF-κB |
BOT-64 是一种 IKK-2 抑制剂,靶向激酶激活环结构域中的 Ser177 和/或 Ser181 残基。BOT-64 是一种可渗透细胞的苯并恶硫醇化合物。 | |||
T3094 |
PS-1145
IKK Inhibitor X |
Apoptosis; IκB/IKK | Apoptosis; NF-κB |
PS-1145 (IKK Inhibitor X) 是一种 IκB 激酶抑制剂,IC50为 88 nM。 | |||
T2081 |
LY2409881 trihydrochloride
LY2409881 |
Apoptosis; IκB/IKK | Apoptosis; NF-κB |
LY2409881 trihydrochloride 是一种新型 IKK2 特异性抑制剂,IC50为 30 nM。 | |||
T2118 |
SC-514
GK 01140 |
IκB/IKK; p38 MAPK; Serine Protease; CDK; Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; NF-κB; Proteases/Proteasome |
SC-514 (GK 01140) 是 IKK-2 的选择性抑制剂 (IC50=11.2 μM),不抑制其他 IKK 亚型或其他丝氨酸-苏氨酸和酪氨酸激酶。 | |||
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。 | |||
T6176 |
IKK 16
IKK Inhibitor VII,IKK-16,IKK16 |
IκB/IKK; LRRK2 | Autophagy; NF-κB |
IKK 16 (IKK Inhibitor VII) 是一种选择性的 IκB 激酶 (IKK) 抑制剂,作用于 IKK2、IKK complex 和 IKK1,IC50分别为 40 nM、70 nM 和 200 nM。它还抑制富亮氨酸重复激酶 2,IC50为 50 nM。 | |||
T0097 |
MRT67307
MRT67307 HCl |
IκB/IKK; Autophagy | Autophagy; NF-κB |
MRT67307 是一种IKKε和TBK-1的双抑制剂,IC50分别为 160 和 19 nM。它抑制细胞自噬,也可抑制ULK1和ULK2,IC50分别为 45 和 38 nM。 | |||
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。 | |||
T0708 |
Oxaprozin
奥沙普秦,Oxaprozinum,Wy21743 |
NF-κB; COX | Immunology/Inflammation; Neuroscience; NF-κB |
Oxaprozin (Oxaprozinum) 是 COX-1和 COX-2的抑制剂,还能抑制 NF-κB 的活化,对人类血小板 COX-1 和 IL-1 刺激的人类滑膜细胞 COX-2 的 IC50值分别为 2.2 和 36 μM。 | |||
T6326 |
BMS-345541
BMS-345541 free base,IKK Inhibitor III,BMS345541 |
IκB/IKK | NF-κB |
BMS-345541 (IKK Inhibitor III) 是选择性的 IKK 催化亚基 IKK-1 和 IKK-2 抑制剂,抑制 IKK-2 (IC50=0.3 nM) 和 IKK-1 (IC50=4 nM)。它与 IKK 的变构位点结合。 | |||
T3049 |
TPCA-1
GW683965,IKK2 Inhibitor IV,TPCA1 |
Apoptosis; IκB/IKK; STAT | Apoptosis; JAK/STAT signaling; NF-κB; Stem Cells |
TPCA-1 (TPCA1) 是一种选择性IKK-2抑制剂,IC50值为 17.9 nM。它也是反式激活、DNA 结合以及STAT3磷酸化的一种抑制剂。 | |||
T1639 |
Amlexanox
氨来呫诺,CHX3673,Amoxanox,氨来诺,AA673 |
IL Receptor; FGFR; Others; IκB/IKK | Angiogenesis; Immunology/Inflammation; NF-κB; Others; Tyrosine Kinase/Adaptors |
Amlexanox (AA673) 是一种特异性的 IKKε和 TBK1抑制剂,其 IC50=1-2 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)。 | |||
T2279 |
Tizoxanide
替唑尼特,Desacetyl-nitazoxanide,TIZ |
Antiviral; HIV Protease; Antibacterial; Autophagy | Autophagy; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
Tizoxanide (Desacetyl-nitazoxanide) 是 Nitazoxanide 活性代谢物,有抗HIV-1的活性。Nitazoxanide 可抗细菌和多种病毒复制。 | |||
T8542 |
BMS-345541 hydrochloride
N-(1,8-二甲基咪唑并[1,2-A]喹喔啉-4-基)-1,2-乙二胺盐酸盐 |
IκB/IKK | NF-κB |
BMS-345541 hydrochloride 是选择性的 IKK 催化亚基 IKK-1 和 IKK-2 抑制剂,抑制 IKK-2 (IC50=0.3 nM) 和 IKK-1 (IC50=4 nM)。它与 IKK 的变构位点结合。 | |||
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。 | |||
T9105 |
NF-κB-IN-1
1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)- |
IκB/IKK; NF-κB | NF-κB |
NF-κB-IN-1 (1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-)是一种 4-亚芳基姜黄素类似物,是抑制有效的NF-κB 信号通路抑制剂。它可有效抑制肺癌细胞的活力并减弱 A549 细胞的克隆活性。它可直接抑制IKK 来阻断 NF-κB 的激活。 | |||
T2055 |
WS3
|
EGFR; IκB/IKK | Angiogenesis; JAK/STAT signaling; NF-κB; Tyrosine Kinase/Adaptors |
WS3 是一种可促进鼠和人原代胰岛的胰腺 β 细胞增殖的增殖分子。它可用于研究 I 型糖尿病。 | |||
T2106 |
WS6
|
EGFR; IκB/IKK | Angiogenesis; JAK/STAT signaling; NF-κB; Tyrosine Kinase/Adaptors |
WS6 是一种具有促beta 细胞增生作用的新型小分子,在啮齿类动物和人源原发性胰岛中EC50值为0.28uM。 | |||
T23191 |
PS 1145 dihydrochloride
|
Others | Others |
IκB kinase (IKK) inhibitor | |||
T24470 |
Mitochonic Acid 35
MA35,MA-35,MA 35,Mitochonic Acid-35 |
||
Mitochonic Acid 35 is a dual TNF-α and TGF-β1 inhibitor that acts by inhibiting IκB kinase phosphorylation and Smad3 phosphorylation. | |||
T41101 |
LY2409881
LY2409881 |
||
LY2409881 is a selective IκB kinase β ( IKK2 ) inhibitor with an IC 50 of 30 nM. | |||
T15557 | IKK 16 hydrochloride | Others | Others |
IKK 16 hydrochloride is a selective IKK2, IKK complex, and IKK1 IκB kinase (IKK) inhibitor (IC50s: 40 nM, 70 nM and 200 nM, respectively). IKK16 inhibits leucine-rich repeat kinase-2 (LRRK2; IC50: 50 nM). | |||
T16464 | Pelubiprofen | COX | Immunology/Inflammation; Neuroscience |
Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway. It also has significant anti-inflammatory and analgesic effects. Pelubiprofen is an orally active and non-steroidal anti-inflammatory drug and is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity . | |||
T63107 | Anti-inflammatory agent 6 | ||
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。 | |||
T37449 |
SR 12460
|
||
SR 12460 is a mimetic of the IκB kinase β (IKKβ) NEMO/IKKγ-binding domain (NBD) that inhibits the protein-protein interaction between the IKK complex subunits NF-κB essential modulator (NEMO/IKKγ) and IKKβ.1It inhibits TNF-α-induced NF-κB activation in a reporter assay when used at concentrations ranging from 25 to 150 μM. It reduces LPS-induced production of IL-6 in RAW 264.7 cells. SR 12460 (30 mg/kg) improves grip strength in themdxmouse model of Duchenne muscular dystrophy. 1.Zhao, J., Zhang... | |||
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。 | |||
T69898 | NG25 trihydrochloride | ||
NG25 trihydrochloride is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 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, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration... | |||
T36779 |
NG 25 (hydrochloride hydrate)
|
||
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... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5796 |
Plantainoside D
Isoplantamajoside,车前草苷D |
RAAS; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Endocrinology/Hormones |
Plantainoside D (Isoplantamajoside) 可以抑制 ACE ,IC50=2.17 mM。Plantainoside D 也是IKK-β抑制剂。 | |||
T1558 |
Resveratrol
白藜芦醇,trans-Resveratrol,SRT 501 |
Apoptosis; Mitophagy; IκB/IKK; Lipoxygenase; Sirtuin; COX; NADPH; DNA/RNA Synthesis; Nrf2; Antibacterial; Antibiotic; Autophagy; Antifungal | Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB |
Resveratrol (SRT 501) 属于多酚类天然产物,是一种植物抗毒素,具有抗氧化和化学预防活性。Resveratrol 的靶点广泛,包括 COX、SIRT、LOC 等。Resveratrol 可以诱导细胞自噬和凋亡。 | |||
T0167 |
Vinpocetine
长春西丁,RGH-4405,长春西汀,Ethyl apovincaminate |
IκB/IKK; NF-κB; Sodium Channel; PDE | Membrane transporter/Ion channel; Metabolism; NF-κB |
Vinpocetine (RGH-4405) 是一种长春花生物碱衍生物,是阻断 Na+通道的阻断剂。Vinpocetine 抑制IKK 的IC50为 17.17 μM。Vinpocetine 也是PDE 抑制剂,并通过直接靶向IKK 抑制NF-κB 依赖性炎症反应,已被广泛用于研究脑血管疾病。 | |||
TN1504 |
Citreorosein
羟基大黄素 |
cAMP; NF-κB; PI3K | GPCR/G Protein; NF-κB; PI3K/Akt/mTOR signaling |
Citreorosein is a cAMP phosphodiesterase inhibitor, it has anti-inflammatory effect, inhibits proinflammatory cytokines production through the inhibition of both MAPKs and AKT-mediated IκB kinase (IKK) phosphorylation and subsequent inhibition of transcription factor NF-κB activation. |