Cat. No. | Product Name | Target | Signaling Pathways |
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T73322 |
TBK1-IN-1
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IκB/IKK | NF-κB |
TBK1-IN-1 是一种具有特异性和高效性的 TANK 结合激酶 1 (TBK1) 抑制剂(IC50: 22.4 nM),具有抗癌活性。TBK1-IN-1 对 TBK1 下游靶基因 cxcl10 和 ifnβ 的表达有抑制作用。 | |||
T15559 |
TBK1/IKKε-IN-2
|
IκB/IKK | NF-κB |
TBK1/IKKε-IN-2 是双重TBK1和IKKε抑制剂。 | |||
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。 | |||
T13097 |
TBK1/IKKε-IN-1
|
IκB/IKK | NF-κB |
TBK1/IKKε-IN-1 is a dual inhibitor of TBK1 and IKKε (IC50s of <100 nM). | |||
T39841 |
TBK1/IKKε-IN-6
TBK1/IKKε-IN-6 |
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TBK1/IKKε-IN-6 (example 110) is a potent inhibitor of TBK1 and IKKε, with IC50 values of less than 100 nM for both enzymes. | |||
T38263 |
TBK1/IKKε-IN-4
TBK1/IKKε-IN-4 |
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TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1]. TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1/IK... | |||
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。 | |||
T28107 |
MRT-68601 HCl
|
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MRT-68601 HCl, a potent TBK1 (TANK-binding kinase-1), inhibits the formation of autophagosomes in lung cancer cells. | |||
T36995 |
MRT 68601 hydrochloride
|
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Potent TBK1 (TANK-binding kinase-1) inhibitor (IC50 = 6 nM). Inhibits the formation of autophagosomes in lung cancer cells. Newman et al (2012) TBK1 kinase addiction in lung cancer cells is mediated via autophagy of Tax1bp1/Ndp52 and non-canonical NF-κB signalling. PLoS ONE 7 e50672 PMID:23209807 |McIver et al (2012) Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases. Bioorg.Med.Chem.Lett. 22 7169 PMID:23099093 | |||
T23028 |
MRT67307 HCl (1190378-57-4 free base)
MRT67307 HCl |
Others | Others |
MRT67307 is an inhibitor for TBK1, IKKε , MARK1-4 and NUAK1 with IC50 value of 19, 160, 27-52 and 230nM , respectively [1]. It is an inhibitor for ULK1and ULK2 with IC50 value of 45 and 38nM, respectively [2]. Also, it is a salt inducible kinase (SIK) inhibitor with IC50 value of 250, 67 and 430nM for SIK1, SIK2 and SIK3, respectively.<br />SIKs prevent the formation of regulatory macrophages and their inhibition induces increasing in some markers of regulatory macrophages, such as IL-10 and oth... | |||
T36461 |
CAY10748
CAY10748 |
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CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β an... | |||
T75096 | STING agonist-28 | ||
STINGagonist-28 (CF510) 是一种非核苷酸小分子STING 激动剂。STINGagonist-23 激活STING,增加STING、TBK1和IRF3的磷酸化。STINGagonist-23 可促进肿瘤细胞中IFN-β、IL-6、CXCL-10、TNF-α、ISG-15和CCL-5的水平。STINGagonist-23 表现出抗SARS-CoV 系列的活性。 | |||
T75094 | STING agonist-26 | ||
STINGagonist-26 (CF508) 是一种非核苷酸小分子STING 激动剂。STINGagonist-23 激活STING,增加STING、TBK1和IRF3的磷酸化。STINGagonist-23 可促进肿瘤细胞中IFN-β、IL-6、CXCL-10、TNF-α、ISG-15和CCL-5的水平。STINGagonist-23 表现出抗SARS-CoV 系列的活性。 | |||
T75093 | STING agonist-25 | ||
STINGagonist-25 (CF505) 是一种非核苷酸小分子 STING 激动剂。STINGagonist-23 激活 STING,增加 STING、TBK1和 IRF3的磷酸化。STINGagonist-23 可促进肿瘤细胞中IFN-β、IL-6、CXCL-10、TNF-α、ISG-15和CCL-5的水平。STINGagonist-23 表现出抗SARS-CoV 系列的活性。 | |||
T75092 | STING agonist-24 | ||
STINGagonist-24 (CF504) 是一种非核苷酸小分子STING 激动剂。STINGagonist-23 激活STING,增加STING、TBK1和IRF3的磷酸化。STINGagonist-23 可促进肿瘤细胞中IFN-β、IL-6、CXCL-10、TNF-α、ISG-15和CCL-5的水平。STINGagonist-23 表现出抗SARS-CoV 系列的活性。 | |||
T83901 |
BDW568
|
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BDW568是一种刺激素干扰素基因(STING)的激动剂,同时是BDW-OH的前药形式。在使用THP-1细胞的报告基因测定中,它能诱导STING转录活性(EC50 = 7.6 µM)。BDW568(50 µM)在THP-1细胞中诱导TANK结合激酶1(TBK1)和IFN调节因子3(IRF3)的磷酸化。 | |||
T75091 | STING agonist-23 | ||
STINGagonist-23 (CF502) 是一种非核苷酸小分子 STING 激动剂。STINGagonist-23 激活 STING,增加 STING、TBK1和 IRF3的磷酸化。STINGagonist-23 可促进肿瘤细胞中 IFN-β、IL-6、CXCL-10、TNF-α、ISG-15和 CCL-5的水平。STINGagonist-23 表现出抗 SARS-CoV 系列的活性。 | |||
T83841 |
STING Agonist D61
D61,Stimulator of Interferon Genes Agonist D61 |
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STING激动剂D61(D61)是干扰素基因刺激剂(STING)的激动剂。它在基于细胞的分析中诱导IFN3诱导的分泌性碱性磷酸酶(SEAP)报告基因和IFN-β诱导的报告基因的表达(EC50分别为52.9和116 nM)。D61(4, 6, 和8 µM)增加了编码IFN-β和化学因子(C-X-C基序)配体10(CXCL10)的mRNA的表达以及TANK结合激酶1(TBK1)、IRF3和STING在THP-1单核细胞中的磷酸化。在体内,D61(每隔一天0.25 mg/kg)在CT26小鼠结肠癌模型中减少肿瘤体积,而不影响体重。 | |||
T36996 |
MSA-2 dimer
|
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MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1]. MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1]. MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression[1].MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) le... |