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23

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13736	Interferon receptor inducer-1	IFNAR	Immunology/Inflammation
	Interferon receptor inducer-1 是一种干扰素(IFN)受体诱导剂，可用于干扰素诱导参与的紊乱性疾病的研究。
T12933	SM-276001	TLR; COX	Immunology/Inflammation; Neuroscience
	SM-276001 是可口服的干扰素诱导剂，是选择性TLR7激动剂，可以诱导抗肿瘤免疫反应。
T8798	MSA-2	STING	Immunology/Inflammation
	MSA-2 是可口服的非核苷酸 STING 激动剂，以具有纳摩尔亲和力的非共价二聚体形式与 STING 结合。它在同基因小鼠肿瘤模型中显示抗肿瘤活性，与抗 PD-1 协同作用，可刺激肿瘤分泌干扰素-β，诱导肿瘤消退，具有持久的抗肿瘤免疫。
T14687	Deucravacitinib BMS-986165	Tyrosine Kinases; JAK; IFNAR; Interleukin	Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	Deucravacitinib (BMS-986165) 是一种高选择性、口服生物可利用的变构 TYK2 抑制剂，用于治疗自身免疫性疾病。它通过稳定调节 JH2 结构域来阻断受体介导的 Tyk2 激活，可抑制IL-12/23和 I 型IFN 途径。它选择性结合 TYK2 假激酶 (JH2) 结构域，IC50为1.0 nM。
T11630	IFN alpha-IFNAR-IN-1 hydrochloride	Others; IFNAR	Immunology/Inflammation; Others
	IFN alpha-IFNAR-IN-1 hydrochloride 是 IFN-α 和 IFNAR 相互作用的抑制剂。 IFN alpha-IFNAR-IN-1 hydrochloride 抑制 BM-pDCs 的 MVA 诱导的 IFN-α 反应，IC50 为 2-8 μM。
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。
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。
T4403	AX-024 hydrochloride AX-024 HCl	IL Receptor; TNF; COX; IFNAR; Interleukin	Apoptosis; Immunology/Inflammation; Neuroscience
	AX-024 hydrochloride (AX-024 HCl) 是一种细胞因子释放抑制剂，可强烈抑制 IL-6、TNFα、IFN-γ、IL-10 和 IL-17A 的产生。它是口服可利用的 TCR-Nck 相互作用抑制剂，可选择性地抑制 TCR 触发的 T 细胞活化。它通过靶向 SH3结构域调节细胞信号传导，具有低毒、高效和高选择性的特点。
T22142	RO8191 RO4948191,CDM-3008	HCV Protease; HBV; JAK; IFNAR; STAT	Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Microbiology/Virology; Proteases/Proteasome; Stem Cells
	RO8191 (CDM-3008) 是干扰素 (IFN) 受体激动剂。它直接与 IFNα/β 受体 2 结合，激活 IFN 刺激的基因表达和 JAK/STAT 磷酸化。它通过具有干扰素样活性发挥 cccDNA 调节剂作用，并具有抗 HBV 活性。
T6273	Vadimezan DMXAA,伐地美生,5,6-Dimethylxanthenone-4-acetic Acid,NSC 640488,ASA-404	Influenza Virus; VDA; STING; IFNAR	Angiogenesis; Immunology/Inflammation; Microbiology/Virology
	Vadimezan (DMXAA) 是一种血管破坏剂，一种鼠 STING 激动剂，也是一种细胞因子如 I 型 IFN 的诱导剂。Vadimezan 具有抗肿瘤活性，可以诱导肿瘤中的血流快速停止，但不影响正常组织中的血流。
T26895	BRD0476 BRD-0476,ML 187,ML187,ML-187,BRD 0476
	BRD0476 is a suppressor of pancreatic β-cell apoptosis. BRD0476 inhibits interferon-gamma (IFN-γ)-induced Janus kinase 2 (JAK2) and signal transducer and activation of transcription 1 (STAT1) signaling to promote β-cell survival. BRD0476 inhibits JAK-STAT
T38162	STING18
	STING18 is a competitive ligand of stimulator of interferon genes (STING; IC50 = 0.068 μM in a radioligand binding assay).1 It inhibits cGAMP-induced IFN-β production (IC50 = 11 μM) but does not stimulate IFN-β production (EC50 = >30 μM) in THP-1 cells. \|1. Siu, T., Altman, M.D., Baltus, G.A., et al. Discovery of a novel cGAMP competitive ligand of the inactive form of STING. Med. Chem. Lett. 10(1), 92-97 (2019).
T76930	Bifarcept
	Bifarcept为一种针对干扰素受体I型(IFN-RI)的重组抗体，能与IFN-β结合，从而延长其在血清中的半衰期。
T35654	2'2'-cGAMP (sodium salt)
	2'2'-cGAMP is a synthetic dinucleotide (CDN) that contains non-canonical 2'5'-phosphodiester bonds. It binds to the adapter protein stimulator of interferon genes , which is a component of the innate immune response that activates the type I interferon pathway when bound to cyclic dinucleotides. 2'2-cGAMP shows weaker binding to STING than 2'3'-cGAMP but binds more strongly than 3'3'-cGAMP , cyclic di-GMP , or 3'2'-cGAMP, which bind in the micromolar range (Kds = 1.04, 1.21, or 1.61 μM, respecti...
T10065	2',3'-cGAMP 2'-3'-cyclic GMP-AMP	STING; cGAS	Immunology/Inflammation
	2',3'-cGAMP (2'-3'-cyclic GMP-AMP) 是细胞天然免疫中第二信使，在DNA结合条件下由 cGAMP 合成酶 (cGAS) 催化形成。2',3'-cGAMP 可与 STING 结合形成二聚体，诱导干扰素-β（IFN-β）及其他细胞因子的产生和表达。
T73693	Peginterferon beta-1a
	Peginterferon beta-1a (Peginterferon β-1a) 是一个聚乙二醇化干扰素 beta-1a 分子。Peginterferon beta-1a 诱导癌细胞凋亡并且在裸鼠模型中显示出抗肿瘤活性。Peginterferon beta-1a 可用于癌症和多发性硬化 (RMS) 的研究。
T38091	3'3'-cGAMP (sodium salt)
	3'3'-cGAMP is a second messenger produced in bacteria by specific dinucleotide cyclases. It contains canonical 3'5'-phosphodiester bonds and regulates chemotaxis, colonization, and other cellular functions. 3'3'-cGAMP shows weaker binding to the adapter protein stimulator of interferon genes (STING; Kd = 1.04 μM) than 2'2'-cGAMP and 2'3'-cGAMP but has similar binding affinity to 3'2'-cGAMP (Kd = 1.61 μM) and cyclic di-GMP . 3'3'-cGAMP induces IFN-β mRNA expression in L929 cells (EC50 = 40.5 nM).
T38160	STING Agonist 1a
	STING agonist 1a is an agonist of stimulator of interferon genes (STING).1It induces expression of an IRF-inducible SEAP reporter gene in a cell-based assay (EC50= 16.77 μM). STING agonist 1a (12.5-100 μM) induces expression of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells, an effect that can be reversed by STING knockout or the STING inhibitor H-151 . 1.Hou, H., Yang, R., Liu, X., et al.Discovery of triazoloquinoxaline as novel STING agonists via structure-based vir...
T38158	StA-IFN-1
	StA-IFN-1 is an inhibitor of the interferon (IFN) induction pathway with an IC50 value of 4.1 μM in a GFP reporter assay for IFN induction similar to TPCA-1 , which specifically inhibits the IKKβ component of the IFN induction pathway. It does not show inhibitory activity in a GFP reporter assay for IFN signaling in which ruxolitinib , which is specific for the IFN signaling component JAK1, is active. StA-IFN-1 reduces the levels of IFN-β, but not ISG MxA, mRNA, suggesting that it is selective f...
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...
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。
T83775	STING Agonist 12L Stimulator of Interferon Genes Agonist 12L
	STING激动剂12L是一种刺激干扰素基因(STING)的激动剂。它与野生型STING结合(IC50 = 1.15 µM)，以及STING的R232、AQ和Q变体(IC50分别为1.06、0.61和1.12 µM)，并在THP-1和RAW 264.7细胞中诱导报告基因表达(EC50分别为0.38和12.94 µM)。STING激动剂12L (5 µM)在THP-1细胞中诱导IFNB1、CXCL10和IL6 mRNA的表达。在体内，STING激动剂12L (10 mg/kg)提高了血浆IFN-β水平，并且在B16/F10小鼠黑色素瘤模型中减少了肿瘤体积和肺转移灶的数量。

化合物

Interferon receptor inducer-1

Cat.No: T13736

Target: IFNAR

Cat.No: T12933

Target: TLR, COX

Cat.No: T8798

Target: STING

Deucravacitinib

Cat.No: T14687

Synonym: BMS-986165

Target: Tyrosine Kinases, JAK, IFNAR, Interleukin

IFN alpha-IFNAR-IN-1 hydrochloride

Cat.No: T11630

Target: Others, IFNAR

Cat.No: T7081

Synonym: Carbonyl Cyanide m-Chlorophenylhydrazone,Carbonyl cyanide 3-chlorophenylhydrazone,羰基氰化氯苯腙

Target: Apoptosis, IκB/IKK, COX, Mitochondrial Metabolism, STING, IFNAR, Antibacterial

Cat.No: T5317

Synonym: CMA,吖啶酮乙酸,XBIO-101,10-carboxymethyl-9-acridanone

Target: Progesterone Receptor, STING, IFNAR

AX-024 hydrochloride

Cat.No: T4403

Synonym: AX-024 HCl

Target: IL Receptor, TNF, COX, IFNAR, Interleukin

Cat.No: T22142

Synonym: RO4948191,CDM-3008

Target: HCV Protease, HBV, JAK, IFNAR, STAT

Cat.No: T6273

Synonym: DMXAA,伐地美生,5,6-Dimethylxanthenone-4-acetic Acid,NSC 640488,ASA-404

Target: Influenza Virus, VDA, STING, IFNAR

Cat.No: T26895

Synonym: BRD-0476,ML 187,ML187,ML-187,BRD 0476

Cat.No: T38162

Cat.No: T76930

2'2'-cGAMP (sodium salt)

Cat.No: T35654

Cat.No: T10065

Synonym: 2'-3'-cyclic GMP-AMP

Target: STING, cGAS

Peginterferon beta-1a

Cat.No: T73693

3'3'-cGAMP (sodium salt)

Cat.No: T38091

STING Agonist 1a

Cat.No: T38160

Cat.No: T38158

Cat.No: T36461

Synonym: CAY10748

STING Agonist C11

Cat.No: T38161

Synonym: STING Agonist C11

STING Agonist D61

Cat.No: T83841

Synonym: D61,Stimulator of Interferon Genes Agonist D61

STING Agonist 12L

Cat.No: T83775

Synonym: Stimulator of Interferon Genes Agonist 12L

Cat. No.	Product Name	Target	Signaling Pathways
T3829	Ginsenoside F3 人参皂苷F3	Others; IFNAR; Interleukin	Immunology/Inflammation; Others
	Ginsenoside F3 是一种皂苷，提取自Panax ginseng 叶片。它能够调节1 型 (IL-2, IFN-γ) 及 2 型细胞因子(IL-4 and IL-10) 的产生和表达，有免疫增强的作用。
T14854	Caerulomycin A 浅蓝霉素,Cerulomycin,Caerulomycin	Antifungal	Microbiology/Virology
	Caerulomycin A (Caerulomycin) 是抗真菌和抗细菌化合物，能够诱导 T 细胞的产生。它能够抑制 IFN-γ 诱导的 STAT1 通路，从而增强 TGF-β-Smad3 信号通路。它可用于自身免疫病的研究。

天然产物

Cat.No: T3829

Synonym: 人参皂苷F3

Target: Others, IFNAR, Interleukin

Cat.No: T14854

Synonym: 浅蓝霉素,Cerulomycin,Caerulomycin

Target: Antifungal

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