IFN

抑制剂选择性比较

IFN产品

所有产品(18) IFN抑制剂(10) IFN激活剂(8)

目录号	产品描述	文献引用	实验数据
S3023	Bufexamac Bufexamac是一种COX抑制剂，靶点是IFN-α， EC50 为8.9 μM。	Autophagy, 2016, 12(10):1738-1758 Oncotarget, 2016, 7(37):59388-59401 Nat Biotechnol, 2015, 10.1038/nbt.3130	(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 nitrate Butoconazole 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	CCCP CCCP (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。	Cancers (Basel), 2021, 13(5)1097 Oxid Med Cell Longev, 2020, 2020:6579696
S3827	Royal jelly acid Royal 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.
S8879^New	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。
S0437^New	SAR-20347 SAR-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。
S7259	FLLL32 FLLL32 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。	Onco Targets Ther, 2021, 14:379-392 Onco Targets Ther, 2020, 12;13:2215-2224 Transl Oncol, 2020, 13(10):100825	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.
S5588	Creatine Creatine (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。
S6727	AX-024 HCl AX-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 Rb1 Ginsenoside 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.	J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S1537	DMXAA (Vadimezan) DMXAA (Vadimezan)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。	Immunity, 2020, 7 pii: S1074-7613(20)30129-1 Sci Rep, 2020, 10(1):21360 J Ethnopharmacol, 2020, 113246	(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^New	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-emodin Aloe-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。	PLoS One, 2019, 14(4):e0215664 J Tradit Complement Med, 2015, 5(2):96-9	Flow cytometry result. Promastigotes were stained with Annexin V and propidium iodide 48 hours after treatment with aloe-emodin
S8133	Resiquimod 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。	Vaccines (Basel), 2020, 15;8(2):E186 Nat Commun, 2020, 11(1):3521 Cancer Lett, 2020, 469:173-185
S5020	Tilorone dihydrochloride Tilorone 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 Salt 2',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'-cGAMP 3',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-276001 SM-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
S3023	Bufexamac Bufexamac是一种COX抑制剂，靶点是IFN-α， EC50 为8.9 μM。	Autophagy,2016, 12(10):1738-1758 Oncotarget,2016, 7(37):59388-59401 Nat Biotechnol,2015, 10.1038/nbt.3130	(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 nitrate Butoconazole 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	CCCP CCCP (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。	Cancers (Basel),2021, 13(5)1097 Oxid Med Cell Longev,2020, 2020:6579696
S3827	Royal jelly acid Royal 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.
S8879^New	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。
S0437^New	SAR-20347 SAR-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。
S7259	FLLL32 FLLL32 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。	Onco Targets Ther,2021, 14:379-392 Onco Targets Ther,2020, 12;13:2215-2224 Transl Oncol,2020, 13(10):100825	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.
S5588	Creatine Creatine (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。
S6727	AX-024 HCl AX-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 Rb1 Ginsenoside 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.	J Ethnopharmacol,2021, S0378-8741(21)00169-0

目录号	产品描述	文献引用	实验数据
S1537	DMXAA (Vadimezan) DMXAA (Vadimezan)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。	Immunity, 2020, 7 pii: S1074-7613(20)30129-1 Sci Rep, 2020, 10(1):21360 J Ethnopharmacol, 2020, 113246	(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^New	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-emodin Aloe-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。	PLoS One, 2019, 14(4):e0215664 J Tradit Complement Med, 2015, 5(2):96-9	Flow cytometry result. Promastigotes were stained with Annexin V and propidium iodide 48 hours after treatment with aloe-emodin
S8133	Resiquimod 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。	Vaccines (Basel), 2020, 15;8(2):E186 Nat Commun, 2020, 11(1):3521 Cancer Lett, 2020, 469:173-185
S5020	Tilorone dihydrochloride Tilorone 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 Salt 2',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'-cGAMP 3',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-276001 SM-276001 is a potent and selective agonist of TLR7 that induces antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer.