IFN
抑制剂选择性比较
IFN产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| A2041New |
Emapalumab (anti-IFNγ)Emapalumab (anti-IFNγ)是一种针对IFNγ的单克隆抗体，是第一个全球批准用于治疗难治性原发性噬血性血细胞淋巴组织细胞增多症(HLH)的儿童和成人患者的治疗方法。 |
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| S3023 |
BufexamacBufexamac是一种COX抑制剂，靶点是IFN-α， EC50 为8.9 μM。 |
(a) Treatment of HeLa cells with 1 mM bufexamac results in the induction of HIF1-α, as determined by immunoblotting. The known hypoxia mimetics CPX and DFX were used as positive controls; vinculin served as loading control. (b) Verification of bufexamac-specific upregulation of HIF1-α. HIF1-α protein expression was analyzed 4 h after treatment of cells with the indicated compounds. Ac, acetylated. (c) Time-course analysis of HIF1-α induction by bufexamac. The induction of HIF1-α protein was analyzed by immunoblotting. The graph shows rapid stabilization of HIF1-α upon bufexamac treatment with half-maximal intensity I1/2 of about 75 min. Error bars represent s.d. of three independent experiments. (d) HIF1-α is stabilized only at higher concentrations of bufexamac and accumulates in the nucleus. Induction of endogenous HIF1-α and its nuclear accumulation was analyzed using immunofluorescence microscopy; scale bar, 10 μm. |
|
| S1833 |
Butoconazole nitrateButoconazole nitrate (RS-35887)是一种抗真菌剂，抑制PHA刺激下人外周血淋巴细胞中细胞因子（如IL-2, TNFα, IFN 和 GM-CSF）的分泌，IC50分别为7.2 μg/mL, 14.4 μg/mL, 7.36 μg/mL 和 7.6 μg/mL。 |
||
| 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。 |
||
| S3827 |
Royal jelly acidRoyal jelly acid (10-Hydroxy-trans-2-decenoic acid, 10H2DA) is the principal lipid component in royal jelly which is the food for queen and larvae honeybees. It is involved in several treatment processes of autoimmune and inflammatory diseases, including inhibition of lipopolysaccharide (LPS)- and interferon (IFN)-γ-stimulated macrophage responses, inhibition of T-cell proliferation and anti-rheumatoid activity. |
||
| S7259 |
FLLL32FLLL32 是一种有效的 JAK2/STAT3 抑制剂，IC50 <5 μM。FLLL32 在乳腺癌细胞中通过 IFNα 和 IL-6 来抑制STAT3磷酸化的诱导。 |
Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.
|
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| S3544 |
VBIT-4VBIT-4 是一种 voltage-dependent anion channel (VDAC) oligomerization 的抑制剂，可降低在系统性红斑狼疮小鼠模型中 mitochondrial DNA (mtDNA) 的释放、type I interferon (IFN) 的信号传导、中性粒细胞胞外陷阱和疾病的严重性。 |
||
| S5588 |
CreatineCreatine (Methylguanidoacetic acid) 是一种天然存在于脊椎动物中的含氮有机酸。Creatine 可以通过抑制 IFN-γ receptors 与 JAK2 的相互作用来抑制 JAK-STAT1 信号传递，以ATP非依赖性的方式促进三磷酸腺苷（ATP）的循环，从而抑制下游促炎基因表达。 |
||
| S0437 |
SAR-20347SAR-20347 是一种有效的 TYK2、JAK1、JAK2 和 JAK3 的抑制剂，对应的IC50值为0.6 nM、23 nM、26 nM和41 nM。SAR-20347可抑制TYK2和JAK1介导的 IL-12 和 IFN-α 信号传导。 |
||
| S8879 |
Deucravacitinib (BMS-986165)Deucravacitinib (BMS-986165)是一种强效的、选择性的 Tyk2 的变构抑制剂，其与 Tyk2 假激酶结构域结合的Ki值为0.02 nM。它对一组265种激酶和假激酶的实验中具有高度的选择性。 |
||
| S6727 |
AX-024 HClAX-024 HCl 可抑制CD3ε PRS与SH3.1(Nck)的相互作用。AX-024 HCl 可抑制 IL-6、TNF-α、IFN-γ、IL-10 和 IL-17A。 |
||
| S3924 |
Ginsenoside Rb1Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS. |
||
| 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。 |
||
| S2259 |
Aloe-emodinAloe-emodin (NSC 38628, Rhabarberone) 是一种干扰素诱导剂，作用于JEV，IC50为1 μg/mL，作用于EV71，IC50为0.33 μg/mL。 |
Flow cytometry result. Promastigotes were stained with Annexin V and propidium iodide 48 hours after treatment with aloe-emodin |
|
| S8133 |
Resiquimod (R-848)Resiquimod (R-848, S28463)是一种免疫反应调节剂，用作有效的TLR 7/TLR 8激动剂并可诱导如 TNF-α、IL-6 和 IFN-α 等细胞因子的上调。Resiquimod 可减少 hepatitis C virus (HCV)感染。Phase 2。 |
||
| S5020 |
Tilorone dihydrochlorideTilorone dihydrochloride是一种广谱的、具有口服活性的抗病毒试剂，可激活干扰素的生成。它具有抗肿瘤和抗炎活性。 |
||
| 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。 |
||
| S2952 |
SM-276001SM-276001 is a potent and selective agonist of TLR7 that induces antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer. |
||
| S0289 |
KIN1148KIN1148 是一种 interferon regulatory factor 3 (IRF3) 的激动剂，可诱导剂量依赖性IRF3核易位和IRF3反应性启动子的特异性激活。KIN1148 是一种流感疫苗佐剂，可增强流感疫苗的功效。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| A2041New |
Emapalumab (anti-IFNγ)Emapalumab (anti-IFNγ)是一种针对IFNγ的单克隆抗体，是第一个全球批准用于治疗难治性原发性噬血性血细胞淋巴组织细胞增多症(HLH)的儿童和成人患者的治疗方法。 |
||
| S3023 |
BufexamacBufexamac是一种COX抑制剂，靶点是IFN-α， EC50 为8.9 μM。 |
(a) Treatment of HeLa cells with 1 mM bufexamac results in the induction of HIF1-α, as determined by immunoblotting. The known hypoxia mimetics CPX and DFX were used as positive controls; vinculin served as loading control. (b) Verification of bufexamac-specific upregulation of HIF1-α. HIF1-α protein expression was analyzed 4 h after treatment of cells with the indicated compounds. Ac, acetylated. (c) Time-course analysis of HIF1-α induction by bufexamac. The induction of HIF1-α protein was analyzed by immunoblotting. The graph shows rapid stabilization of HIF1-α upon bufexamac treatment with half-maximal intensity I1/2 of about 75 min. Error bars represent s.d. of three independent experiments. (d) HIF1-α is stabilized only at higher concentrations of bufexamac and accumulates in the nucleus. Induction of endogenous HIF1-α and its nuclear accumulation was analyzed using immunofluorescence microscopy; scale bar, 10 μm. |
|
| S1833 |
Butoconazole nitrateButoconazole nitrate (RS-35887)是一种抗真菌剂，抑制PHA刺激下人外周血淋巴细胞中细胞因子（如IL-2, TNFα, IFN 和 GM-CSF）的分泌，IC50分别为7.2 μg/mL, 14.4 μg/mL, 7.36 μg/mL 和 7.6 μg/mL。 |
||
| 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。 |
||
| S3827 |
Royal jelly acidRoyal jelly acid (10-Hydroxy-trans-2-decenoic acid, 10H2DA) is the principal lipid component in royal jelly which is the food for queen and larvae honeybees. It is involved in several treatment processes of autoimmune and inflammatory diseases, including inhibition of lipopolysaccharide (LPS)- and interferon (IFN)-γ-stimulated macrophage responses, inhibition of T-cell proliferation and anti-rheumatoid activity. |
||
| S7259 |
FLLL32FLLL32 是一种有效的 JAK2/STAT3 抑制剂，IC50 <5 μM。FLLL32 在乳腺癌细胞中通过 IFNα 和 IL-6 来抑制STAT3磷酸化的诱导。 |
Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.
|
|
| S3544 |
VBIT-4VBIT-4 是一种 voltage-dependent anion channel (VDAC) oligomerization 的抑制剂，可降低在系统性红斑狼疮小鼠模型中 mitochondrial DNA (mtDNA) 的释放、type I interferon (IFN) 的信号传导、中性粒细胞胞外陷阱和疾病的严重性。 |
||
| S5588 |
CreatineCreatine (Methylguanidoacetic acid) 是一种天然存在于脊椎动物中的含氮有机酸。Creatine 可以通过抑制 IFN-γ receptors 与 JAK2 的相互作用来抑制 JAK-STAT1 信号传递，以ATP非依赖性的方式促进三磷酸腺苷（ATP）的循环，从而抑制下游促炎基因表达。 |
||
| S0437 |
SAR-20347SAR-20347 是一种有效的 TYK2、JAK1、JAK2 和 JAK3 的抑制剂，对应的IC50值为0.6 nM、23 nM、26 nM和41 nM。SAR-20347可抑制TYK2和JAK1介导的 IL-12 和 IFN-α 信号传导。 |
||
| S8879 |
Deucravacitinib (BMS-986165)Deucravacitinib (BMS-986165)是一种强效的、选择性的 Tyk2 的变构抑制剂，其与 Tyk2 假激酶结构域结合的Ki值为0.02 nM。它对一组265种激酶和假激酶的实验中具有高度的选择性。 |
||
| S6727 |
AX-024 HClAX-024 HCl 可抑制CD3ε PRS与SH3.1(Nck)的相互作用。AX-024 HCl 可抑制 IL-6、TNF-α、IFN-γ、IL-10 和 IL-17A。 |
||
| S3924 |
Ginsenoside Rb1Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS. |
| 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。 |
||
| S2259 |
Aloe-emodinAloe-emodin (NSC 38628, Rhabarberone) 是一种干扰素诱导剂，作用于JEV，IC50为1 μg/mL，作用于EV71，IC50为0.33 μg/mL。 |
Flow cytometry result. Promastigotes were stained with Annexin V and propidium iodide 48 hours after treatment with aloe-emodin |
|
| S8133 |
Resiquimod (R-848)Resiquimod (R-848, S28463)是一种免疫反应调节剂，用作有效的TLR 7/TLR 8激动剂并可诱导如 TNF-α、IL-6 和 IFN-α 等细胞因子的上调。Resiquimod 可减少 hepatitis C virus (HCV)感染。Phase 2。 |
||
| S5020 |
Tilorone dihydrochlorideTilorone dihydrochloride是一种广谱的、具有口服活性的抗病毒试剂，可激活干扰素的生成。它具有抗肿瘤和抗炎活性。 |
||
| 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。 |
||
| S2952 |
SM-276001SM-276001 is a potent and selective agonist of TLR7 that induces antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S0289 |
KIN1148KIN1148 是一种 interferon regulatory factor 3 (IRF3) 的激动剂，可诱导剂量依赖性IRF3核易位和IRF3反应性启动子的特异性激活。KIN1148 是一种流感疫苗佐剂，可增强流感疫苗的功效。 |
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