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18

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13606	cGAMP 3',3'-cGAMP,Cyclic GMP-AMP	Others	Others
	cGAMP is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. It also is a STING ligand.
T39582	2',3'-cGAMP-C2-SH 2',3'-cGAMP-C2-SH
	2', 3'-cGAMP-C2-SH is a ADC cytotoxin.
T40224	2',3'-cGAMP-C2-PPA 2',3'-cGAMP-C2-PPA
	2',3'-cGAMP-C2-PPA (45) is a cyclic di-nucleotide that acts as a STING agonist (US20210015941A1). It is a drug-linker conjugate for antibody-drug conjugates (ADC) used in the targeted treatment of cancer.
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).
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...
T41205	3',3'-cGAMP sodium salt
	3',3'-cGAMP sodium salt is a STING agonist. Reduces B cell proliferation and induces apoptosis of malignant B cellsin vitro. Suppresses 5TGM1 multiple myeloma xenograft growth in immunodeficient mice, and induces leukemic regression in Eμ-TCL1 mice.
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。
T77870	Mal-Val-Ala-PABA-cGAMP
	Mal-Val-Ala-PABA-cGAMP 是一款 ADC 连接剂，适用于与 STING 激动剂的结合。该化合物主要用于合成抗体-活性分子偶联物（ADCs）。
T8655	SR-717	STING	Immunology/Inflammation
	SR-717 是一种 cGAMP 的类似物，一种非核苷类 STING 激动剂，可以诱导 STING 形成“封闭”的激活构象。SR-717 具有抗肿瘤活性，可以促进免疫细胞的激活以及抗原的交叉提呈。
T9028	STING-IN-2 C-170	STING	Immunology/Inflammation
	STING-IN-2 (C-170) 是一种 STING 共价抑制剂，可抑制小鼠 STING (mmSTING) 和人类 STING (hsSTING)，可用于自身炎症性疾病的研究。
T79032	Enpp-1-IN-17
	Enpp-1-IN-17 (example 274) 是一种ENPP1抑制剂，其对cGAMP水解的Ki值在100 nM-1 μM范围内，而对ATP水解的Ki值则大于1 μM。该化合物在抑制cGAMP水解方面相对于ATP水解的选择性比率超过6.4。
T39829	BPK-25
	BPK-25 is an active acrylamide compound that enhances the degradation of proteins in the nucleosome remodeling and deacetylation (NuRD) complex through a post-translational mechanism involving covalent protein interaction. Additionally, BPK-25 acts as an inhibitor of TMEM173 activation by the cyclic dinucleotide ligand cGAMP.
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...
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).
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...
T38319	93-O17O 93-O17O
	93-O17O is a chalcogen-containing cationic lipidoid.1,2It has been used in the generation of lipid nanoparticles (LPNs). LPNs containing 93-O17O localize to the spleen after intravenous injection into mice.1LPNs containing 93-O17O have been used for the delivery of Cre recombinase and ribonucleoproteins for genome editing in mice and for the intratumoral delivery of cGAMP to enhance cross-presentation of tumor antigens.3,2 1.Zhao, X., Chen, J., Qiu, M., et al.Imidazole-based synthetic lipidoids ...
T38320	93-O17S 93-O17S
	93-O17S is a chalcogen-containing cationic lipidoid.1It has been used in the synthesis of lipid nanoparticles (LPNs) for the delivery of Cre recombinase and ribonucleoproteins for genome editing in mice. LPNs containing 93-O17S have been used for the intratumoral delivery of cGAMP to enhance cross-presentation of tumor antigens and stimulation of interferon genes (STING) activation in a B16/F10 murine melanoma model.2 1.Li, Y., Yang, T., Yu, Y., et al.Combinatorial library of chalcogen-containin...

化合物

Cat.No: T13606

Synonym: 3',3'-cGAMP,Cyclic GMP-AMP

Target: Others

2',3'-cGAMP-C2-SH

Cat.No: T39582

Synonym: 2',3'-cGAMP-C2-SH

2',3'-cGAMP-C2-PPA

Cat.No: T40224

Synonym: 2',3'-cGAMP-C2-PPA

3'3'-cGAMP (sodium salt)

Cat.No: T38091

2'2'-cGAMP (sodium salt)

Cat.No: T35654

3',3'-cGAMP sodium salt

Cat.No: T41205

Cat.No: T10065

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

Target: STING, cGAS

Mal-Val-Ala-PABA-cGAMP

Cat.No: T77870

Cat.No: T8655

Target: STING

Cat.No: T9028

Synonym: C-170

Target: STING

Cat.No: T79032

Cat.No: T39829

Cyclic di-UMP (sodium salt)

Cat.No: T36985

Cat.No: T38162

SR-717 free acid

Cat.No: T39926

Cat.No: T38328

Cat.No: T38319

Synonym: 93-O17O

Cat.No: T38320

Synonym: 93-O17S

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。
T13606L	cGAMP disodium
	cGAMP disodium 是在细菌中发现的一种环二核苷酸 (CDN) ，可作为内源性第二信使，影响干扰素的产生以响应胞浆 DNA。cGAMP disodium 通过激活干扰素基因刺激因子 (STING)使 I 型干扰素和其他免疫介质的信号产生级联现象。cGAMP disodium 是一种有效的舌下免疫佐剂，能使免疫功能（血清抗 PA 中和和气道分泌物抗 PA SIgA 反应）更好的发挥作用。
T73717	cGAMP diammonium
	cGAMP (Cyclic GMP-AMPP) diammonium 是一种内源性第二信使，通过触发干扰素的产生来响应胞浆 DNA。它通过激活干扰素基因刺激因子（STING），启动信号级联，进而导致I型干扰素及其他免疫介质的生成。

天然产物

2',3'-cGAMP sodium

Cat.No: T10065L

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

Target: STING, cGAS

cGAMP disodium

Cat.No: T13606L

cGAMP diammonium

Cat.No: T73717

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