Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9119 |
SU0268
|
Others | Others |
SU0268 是有效的 8-8-氧鸟嘌呤 DNA 糖基化酶1的选择性抑制剂,具有调控铜绿假单胞杆菌感染免疫反应的能力。 | |||
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。 | |||
T5317 |
Cridanimod
CMA,吖啶酮乙酸,XBIO-101,10-carboxymethyl-9-acridanone |
Progesterone Receptor; STING; IFNAR | Immunology/Inflammation; Others |
Cridanimod (10-carboxymethyl-9-acridanone, CMA) 是一种是小分子免疫调节剂和干扰素诱导剂,是一种孕酮受体激活剂,能够诱导 IFNα和IFNβ的表达,显著增加 PR 的表达。 | |||
T7081 |
CCCP
Carbonyl Cyanide m-Chlorophenylhydrazone,Carbonyl cyanide 3-chlorophenylhydrazone,羰基氰化氯苯腙 |
Apoptosis; IκB/IKK; COX; Mitochondrial Metabolism; STING; IFNAR; Antibacterial | Apoptosis; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB |
CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) 是一种氧化磷酸化 (OXPHOS) 抑制剂,线粒体质子载体解偶联剂。CCCP 抑制 STING 及其下游信号分子 TBK1 和 IRF3 的激活。 | |||
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。 | |||
T6285 |
GSK-690693
GSK690693 |
Serine Protease; Akt; PKC; AMPK; Autophagy | Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
GSK-690693 是一种泛 Akt 抑制剂,对 Akt1、Akt2和 Akt3的 IC50分别为 2 nM、13 nM 和9 nM。它也是一种 AMPK 的抑制剂,影响 ULK1 的活性,并能显著抑制 STING 依赖的 IRF3 的激活。 | |||
T4027 |
KIN1148
|
Influenza Virus | Microbiology/Virology |
KIN1148 是一种新型小分子佐剂,是IRF3激动剂,用于增强流感疫苗效率。 | |||
T27732 |
KIN1400
|
||
KIN1400, a novel IRF3 activator, triggers IRF3-dependent innate immune antiviral genes and IFNbeta307 expression, suppresses WNV, DV infection, and HCV replication. | |||
T83047 | Anti-inflammatory agent 65 | STING | Immunology/Inflammation |
Anti-inflammatory agent 65(compound 29)是一种从常春藤酸衍生且具有有效抗炎活性的化合物。它能够抑制一氧化氮(NO)的释放,阻止IRF3和p65的核转位,破坏STING/IRF3/NF-κB信号通路,有效减弱炎症反应。 | |||
T10642 |
c-di-AMP
环二腺苷酸,Cyclic diadenylate,Cyclic-di-AMP |
Others | Others |
c-di-AMP (Cyclic diadenylate) is a STING agonist. It binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway. | |||
T72615 | STING modulator-4 | ||
STINGmodulator-4 是一种竞争性的 STING 调节剂,对 R232HSTING 的 Ki 为 0.0933 μM。STINGmodulator-4 在 THP-1 细胞中对 p-IRF3 的 EC50为 >10 μM。 | |||
T81082 |
STING-IN-7
|
STING | Immunology/Inflammation |
STING-IN-7(化合物 21),作为一种STING抑制剂,具有11.5 nM的IC50值,能够抑制STING与干扰素调节因子 3 (IRF3) 的磷酸化。 | |||
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。 | |||
T83901 |
BDW568
|
||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T36461 |
CAY10748
CAY10748 |
||
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... | |||
T73873 |
c-di-AMP disodium
|
||
c-di-AMP (Cyclic diadenylate) sodium 作为一种STING 激动剂,通过结合STING 激活TBK3-IRF3 信号途径,引发I 型 IFN 和 TNF 产生,兼具细菌第二信使功能,在革兰氏阳性细菌中调控细胞生长、存活及毒力,并影响宿主免疫反应。此外,作为有效的粘膜佐剂,它能刺激体液和细胞反应。 | |||
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... | |||
T38161 |
STING Agonist C11
STING Agonist C11 |
||
STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses gro... | |||
T83841 |
STING Agonist D61
D61,Stimulator of Interferon Genes Agonist D61 |
||
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。 | |||
T38263 |
TBK1/IKKε-IN-4
TBK1/IKKε-IN-4 |
||
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... |