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19

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T78858	cGAS-IN-1
	cGAS-IN-1（化合物C20）是一种黄酮类化合物，作为Cyclic GMP-AMP Synthase（cGAS）的抑制剂，其IC50分别为2.28 μM（针对人类cGAS）和1.44 μM（针对小鼠cGAS）。由于cGAS异常激活与众多免疫介导的炎症性疾病相关，cGAS-IN-1显示出了其抗炎潜力。
T12432	PF-06928215	cGAS	Immunology/Inflammation
	PF-06928215 是高亲和力 cGAS 抑制剂，IC50为 4.9 μΜ，亲和力 Kd 值为 0.2 μΜ。
T11673	IRAK4-IN-4	IRAK; cGAS	Immunology/Inflammation; NF-κB
	IRAK4-IN-4 （化合物 15）是白介素-1 受体相关激酶抑制剂，IC50为 2.8 nM。它还抑制环 GMP-AM 合酶，IC50为 2.1 nM。
T9213	G140	cGAS	Immunology/Inflammation
	G140 是选择性环状GMP-AMP 合酶抑制剂，具有抗炎活性，对 h-cGAS 和 m-cGAS 的IC50值分别为 14.0 和 442 nM。
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。
T11344	G150	DNA; cGAS	DNA Damage/DNA Repair; Immunology/Inflammation
	G150 是高选择性h-cGAS 抑制剂，IC50值为 10.2 nM，用于抑制 dsDNA 引发的干扰素表达。
T5486	RU.521 RU320521	DNA; cGAS	DNA Damage/DNA Repair; Immunology/Inflammation
	RU.521 (RU3205217) 是选择性的环状 GMP-AMP 合成酶 (cGAS) 抑制剂，抑制 cGAS 介导的干扰素上调。它也抑制dsDNA 激活受体的活性，IC50为 700 nM。它可降低来自 Aicardi-Goutières 综合征小鼠模型的巨噬细胞中干扰素的组成型表达。
T61575	USP15-IN-1	DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	USP15-IN-1 是一种有效的 USP15 抑制剂（IC50 为 3.76 μM）。USP15-IN-1对非小细胞肺癌和白血病细胞具有高度的抗增殖活性。USP15是 cGAS 的互作蛋白，并且 USP15可以促进 cGAS 识别DNA 激活下游信号通路。
T69663	G108
	G108 is a Novel h-cGAS specific inhibitor for repression of dsDNA-triggered interferon expression (IC50 of 27.5 nM and 5150 nM for h-cGAS and m-cGAS, respectively).
T39926	SR-717 free acid
	SR-717 free acid is a stable cGAMP mimetic and a non-nucleotide STING agonist. It exhibits antitumor activity with EC50 values of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively.
T38328	CU-32
	CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas...
T36985	Cyclic di-UMP (sodium salt)
	Cyclic di-UMP is a pyrimidine-containing cyclic dinucleotide (CDN).1It is produced by bacterial cGAS/DncV-like nucleotidyltransferases (CD-NTases), such as LpCdnE02 fromL. pneumophila, and binds to cGAS, in the apo or dsDNA-bound forms, with reduced affinity compared to 2'3'-cGAMP or 3'3'-cGAMP .1,2Cyclic di-UMP is intended for use as a negative control for cyclic di-GMP signaling. 1.Whiteley, A.T., Eaglesham, J.B., de Oliveira Mann, C.C., et al.Bacterial cGAS-like enzymes synthesize diverse nuc...
T64281	ODN TTAGGG
	ODN TTAGGG (A151) 是一种抑制性寡核苷酸 (ODN)，是一种TLR9、AIM2和cGAS 拮抗剂。ODN TTAGGG 能够 DNA 竞争性地抑制 AIM2 炎性体激活，并抑制 cGAS 的活化，表现出免疫抑制活性。 ODN TTAGGG 能够用于研究红斑狼疮等相关自身免疫性疾病。ODN TTAGGG 序列：5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'。
T79001	Biotin-labeled ODN TTAGGG sodium
	Biotin-labeled ODN TTAGGG (sodium) 作为TLR9、AIM2及cGAS拮抗剂的抑制性寡核苷酸，通过生物素检测系统及光学显微技术可评估CpG ODN在细胞内的摄取与定位。
T79002	FITC-labeled ODN TTAGGG sodium
	FITC-labeled ODN TTAGGG (sodium) 作为一种寡核苷酸抑制剂，对TLR9、AIM2及cGAS具有拮抗作用。通过共聚焦激光扫描显微镜（激发/发射光波长：495/520 nm）或流式细胞术，可以评估CpG ODN在细胞内的摄取及定位情况。
T38329	CU-76
	CU-76 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50= 0.24 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. CU-76 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP sy...
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。
T80761	XQ2B
	XQ2B为cGAS抑制剂，针对蛋白质-DNA相互作用及其相分离。该化合物可阻止单纯疱疹病毒1（HSV-1）触发的抗病毒免疫响应，在体外与体内都能增强HSV-1的感染效果。
T69888	SB02024
	SB02024 is a VPS34 inhibitor. SB02024 activates cGAS-STING signaling and sensitizes tumors to STING agonist. SB02024 blocked autophagy in vitro and reduced xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7, in vivo. Vps34 inhibitor significantly potentiated cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro in monolayer cultures and when grown as multicellular spheroids. Our data suggests that inhibition of autophagy significantly improves sensitivity...

化合物

Cat.No: T78858

Cat.No: T12432

Target: cGAS

Cat.No: T11673

Target: IRAK, cGAS

Cat.No: T9213

Target: cGAS

Cat.No: T9119

Target: Others

Cat.No: T11344

Target: DNA, cGAS

Cat.No: T5486

Synonym: RU320521

Target: DNA, cGAS

Cat.No: T61575

Target: DUB

Cat.No: T69663

SR-717 free acid

Cat.No: T39926

Cat.No: T38328

Cyclic di-UMP (sodium salt)

Cat.No: T36985

Cat.No: T64281

Biotin-labeled ODN TTAGGG sodium

Cat.No: T79001

FITC-labeled ODN TTAGGG sodium

Cat.No: T79002

Cat.No: T38329

Cat.No: T10065

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

Target: STING, cGAS

Cat.No: T80761

Cat.No: T69888

Cat. No.	Product Name	Target	Signaling Pathways
T10065L	2',3'-cGAMP sodium 2'-3'-cyclic GMP-AMP sodium	STING; cGAS	Immunology/Inflammation
	2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) 是一种cGAMP 合成酶(cGAS)影响细胞质DNA 产生的第二信使，是一种跨膜衔接蛋白，是细胞对致病性细胞质DNA 的先天免疫反应的关键组成部分。

天然产物

2',3'-cGAMP sodium

Cat.No: T10065L

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

Target: STING, cGAS

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