STING
抑制剂选择性比较
STING产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1113 |
GSK690693GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。 |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
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| S6494 |
CCCPCCCP (Carbonyl cyanide m-chlorophenyl hydrazone, Carbonyl cyanide 3-chlorophenylhydrazone)是一种氧化磷酸化抑制剂，是线粒体质子载体解偶联剂，可增加线粒体膜对质子的通透性，从而破坏线粒体膜电位。 |
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| S6667 |
STING inhibitor C-178C-178是STING的共价抑制剂，与Cys91共价结合。 |
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| S6575 |
C-176 (STING inhibitor)STING inhibitor C-176是一种有效的STING抑制剂。STING是细胞内DNA感应通路的主要信号分子。 |
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| S7904 |
2',3'-cGAMP Sodium Salt2',3'-cGAMP Sodium Salt (2'-3'-cyclic GMP-AMP Sodium)是响应哺乳动物细胞质中的DNA产生的，并能以高亲和力结合 STING，且有效地诱导 interferon-β (IFNβ)。2',3'-cGAMP 结合 STING 的Kd值为3.79 nM。 |
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| S7905 |
3',3'-cGAMP3',3'-cGAMP (3',3'-cyclic GMP-AMP, Cyclic GMP-AMP, cGAMP)可激活内质网(ER)内源性受体 stimulator of interferon genes (STING) ，从而诱导抗病毒状态和I型IFN的分泌。 |
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| S6652 |
H-151H-151是STING的共价拮抗剂，在人细胞和体内均具有显著的抑制活性。 |
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| S1537 |
Vadimezan (ASA404)Vadimezan (ASA404, NSC 640488, DMXAA)是一种vascular disrupting agents (VDA)，也是一种DT-diaphorase的竞争性抑制剂，无细胞试验中Ki为20 μM ，IC50为62.5 μM。DMXAA (Vadimezan) 也是一种STING 激动剂，具有潜在的抗肿瘤活性。DMXAA (Vadimezan) 在体外可有效诱导 IFN-β 和 TNF-α 的表达，但对 TNF-α 影响相对较低。DMXAA (Vadimezan)具有抗病毒活性。Phase 3。 |
(B and C) sh-scrambled or sh-ck2a–transducted L929 cells (B) and Raw cells (C) were stimulated by DMXAA (100 μg/ml) for various times. Cytosolic and nuclear extracts were prepared as described in Materials and Methods. Five percent of the cytosolic proteins and 20% of the nuclear proteins were resolved by 10% SDS-PAGE. Subsequently, immunoblotting was conducted by indicated Abs. The amounts of Tubulin and Lamin B1 in cytosol versus nuclei detected by respective Abs were used as internal control for fractionation.
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| S8954 |
STING agonist-1 (G10)STING agonist-1 (G10) 是一种新型人类特异性 STING 激动剂，可在人成纤维细胞中触发 IFN regulatory factor 3 (IRF3)/ type I interferon (IFN) 相关转录。STING agonist-1 (G10) 可有效抑制 Chikungunya virus (CHIKV) 的生长，IC90值为8.01 μM 和 Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV)的复制，IC90为24.57 μM。 |
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| S3804 |
Alpha-MangostinAlpha-mangostin is the main xanthone purified from mangosteen and has health promoting benefits including anti-bacterial, anti-inflammatory, anti-oxidant, anti-cancer and cardioprotective activities. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Alpha-mangostin is also an agonist of human STING. |
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| S0853 |
SR-717 lithiumSR-717 lithium 是一种非核苷酸 STING 的激动剂并具有广泛的种间和等位基因特异性，在ISG-THP1 (WT)和ISG-THP1 (cGAS KO)细胞系中的EC50值分别为2.1 μM和2.2 μM。SR-717 lithium 还以STING依赖性方式诱导临床相关靶标的表达，包括程序性细胞死亡1配体1(PD-L1)。SR-717 lithium 具有抗肿瘤活性。 |
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| S9681 |
MSA-2MSA-2 是一种具有抗肿瘤活性的口服非核苷酸人类 STING 激动剂。 |
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| S8796 |
diABZI STING agonist (Compound 3)diABZI STING agonist (diABZI STING agonist-1, Compound 3) 是有效的非核苷类STING激动剂，对于治疗人类癌症具有巨大潜力。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1113 |
GSK690693GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。 |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
|
|
| S6494 |
CCCPCCCP (Carbonyl cyanide m-chlorophenyl hydrazone, Carbonyl cyanide 3-chlorophenylhydrazone)是一种氧化磷酸化抑制剂，是线粒体质子载体解偶联剂，可增加线粒体膜对质子的通透性，从而破坏线粒体膜电位。 |
||
| S6667 |
STING inhibitor C-178C-178是STING的共价抑制剂，与Cys91共价结合。 |
||
| S6575 |
C-176 (STING inhibitor)STING inhibitor C-176是一种有效的STING抑制剂。STING是细胞内DNA感应通路的主要信号分子。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7904 |
2',3'-cGAMP Sodium Salt2',3'-cGAMP Sodium Salt (2'-3'-cyclic GMP-AMP Sodium)是响应哺乳动物细胞质中的DNA产生的，并能以高亲和力结合 STING，且有效地诱导 interferon-β (IFNβ)。2',3'-cGAMP 结合 STING 的Kd值为3.79 nM。 |
||
| S7905 |
3',3'-cGAMP3',3'-cGAMP (3',3'-cyclic GMP-AMP, Cyclic GMP-AMP, cGAMP)可激活内质网(ER)内源性受体 stimulator of interferon genes (STING) ，从而诱导抗病毒状态和I型IFN的分泌。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6652 |
H-151H-151是STING的共价拮抗剂，在人细胞和体内均具有显著的抑制活性。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1537 |
Vadimezan (ASA404)Vadimezan (ASA404, NSC 640488, DMXAA)是一种vascular disrupting agents (VDA)，也是一种DT-diaphorase的竞争性抑制剂，无细胞试验中Ki为20 μM ，IC50为62.5 μM。DMXAA (Vadimezan) 也是一种STING 激动剂，具有潜在的抗肿瘤活性。DMXAA (Vadimezan) 在体外可有效诱导 IFN-β 和 TNF-α 的表达，但对 TNF-α 影响相对较低。DMXAA (Vadimezan)具有抗病毒活性。Phase 3。 |
(B and C) sh-scrambled or sh-ck2a–transducted L929 cells (B) and Raw cells (C) were stimulated by DMXAA (100 μg/ml) for various times. Cytosolic and nuclear extracts were prepared as described in Materials and Methods. Five percent of the cytosolic proteins and 20% of the nuclear proteins were resolved by 10% SDS-PAGE. Subsequently, immunoblotting was conducted by indicated Abs. The amounts of Tubulin and Lamin B1 in cytosol versus nuclei detected by respective Abs were used as internal control for fractionation.
|
|
| S8954 |
STING agonist-1 (G10)STING agonist-1 (G10) 是一种新型人类特异性 STING 激动剂，可在人成纤维细胞中触发 IFN regulatory factor 3 (IRF3)/ type I interferon (IFN) 相关转录。STING agonist-1 (G10) 可有效抑制 Chikungunya virus (CHIKV) 的生长，IC90值为8.01 μM 和 Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV)的复制，IC90为24.57 μM。 |
||
| S3804 |
Alpha-MangostinAlpha-mangostin is the main xanthone purified from mangosteen and has health promoting benefits including anti-bacterial, anti-inflammatory, anti-oxidant, anti-cancer and cardioprotective activities. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Alpha-mangostin is also an agonist of human STING. |
||
| S0853 |
SR-717 lithiumSR-717 lithium 是一种非核苷酸 STING 的激动剂并具有广泛的种间和等位基因特异性，在ISG-THP1 (WT)和ISG-THP1 (cGAS KO)细胞系中的EC50值分别为2.1 μM和2.2 μM。SR-717 lithium 还以STING依赖性方式诱导临床相关靶标的表达，包括程序性细胞死亡1配体1(PD-L1)。SR-717 lithium 具有抗肿瘤活性。 |
||
| S9681 |
MSA-2MSA-2 是一种具有抗肿瘤活性的口服非核苷酸人类 STING 激动剂。 |
||
| S8796 |
diABZI STING agonist (Compound 3)diABZI STING agonist (diABZI STING agonist-1, Compound 3) 是有效的非核苷类STING激动剂，对于治疗人类癌症具有巨大潜力。 |
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