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14

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T9029	STING-IN-3 C-171	STING	Immunology/Inflammation
	STING-IN-3 (C-171) 是干扰素基因刺激物 (STING) 的抑制剂。它与 STING 结合，抑制其棕榈酰化，并阻止 TBK1 的募集和磷酸化。
T72614	STING modulator-3
	STINGmodulator-3 是一种 STING 抑制剂。在闪烁接近实验中，STINGmodulator-3 抑制 R232STING 的 Ki 值为 43.1 nM。STINGmodulator-3 对 THP-1 细胞的 IRF-3 激活和 TNF-β诱导无影响。
T81082	STING-IN-7	STING	Immunology/Inflammation
	STING-IN-7（化合物 21），作为一种STING抑制剂，具有11.5 nM的IC50值，能够抑制STING与干扰素调节因子 3 (IRF3) 的磷酸化。
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.
T83901	BDW568
	BDW568是一种刺激素干扰素基因（STING）的激动剂，同时是BDW-OH的前药形式。在使用THP-1细胞的报告基因测定中，它能诱导STING转录活性（EC50 = 7.6 µM）。BDW568（50 µM）在THP-1细胞中诱导TANK结合激酶1（TBK1）和IFN调节因子3（IRF3）的磷酸化。
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...
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.
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...
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。
T73873	c-di-AMP disodium
	c-di-AMP (Cyclic diadenylate) sodium 作为一种STING 激动剂，通过结合STING 激活TBK3-IRF3 信号途径，引发I 型 IFN 和 TNF 产生，兼具细菌第二信使功能，在革兰氏阳性细菌中调控细胞生长、存活及毒力，并影响宿主免疫反应。此外，作为有效的粘膜佐剂，它能刺激体液和细胞反应。
T83874	S-72
	S-72是一种微管聚合抑制剂，以1, 3, 10 µM的浓度在无细胞测定中抑制微管聚合，并在MCF-7和耐紫杉醇的MCF-7/T乳腺癌细胞中降低细胞活性（IC50分别为15.64和26.32 nM）。50 nM浓度的S-72能抑制MCF-7和MCF-7/T细胞的迁移和侵袭，并减少划痕实验中的伤口闭合百分比。100 nM的S-72在MCF-7/T细胞中诱导G2/M期的细胞周期阻滞以及凋亡，并在同一浓度下抑制这些细胞中干扰素基因激活剂（STING）的激活。以每天15 mg/kg的剂量，S-72抑制了耐紫杉醇的MCF-7/T和MX-1/T小鼠异种移植模型中的肿瘤生长。
T35422	5'-pApA (sodium salt)
	5'-pApA is a linearized form of cyclic di-AMP, a bacterial second messenger that activates the host innate immune system through stimulator of interferon genes (STING).1,2,3,4It is a metabolite of cyclic di-AMP formedviahydrolysis by various phosphodiesterases (PDEs).55'-pApA is intended for use as a negative control for cyclic di-AMP signaling. 1.Burdette, D.L., Monroe, K.M., Sotelo-Troha, K., et al.STING is a direct innate immune sensor of cyclic-di-GMPNature478(7370)515-518(2011) 2.Parvatiyar...
T36133	3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one)
	3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) is a non-nucleotide inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; Ki = 50 μM).1,2 It also inhibits urease (IC50 = 84.53 μM for the Jack bean enzyme).3 \|1. Choudhary, M.I., Fatima, N., Khan, K.M., et al. New biscoumarin derivatives-cytotoxicity and enzyme inhibitory activities. Bioorg. Med. Chem. 14(23), 8066-8072 (2006).\|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, ...
T37832	CAY10761 CAY10761
	CAY10761 is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4 \|1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases/p...

化合物

Cat.No: T9029

Synonym: C-171

Target: STING

STING modulator-3

Cat.No: T72614

Cat.No: T81082

Target: STING

3',3'-cGAMP sodium salt

Cat.No: T41205

Cat.No: T83901

Cat.No: T36461

Synonym: CAY10748

2',3'-cGAMP-C2-PPA

Cat.No: T40224

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

STING Agonist C11

Cat.No: T38161

Synonym: STING Agonist C11

Cat.No: T10065

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

Target: STING, cGAS

c-di-AMP disodium

Cat.No: T73873

Cat.No: T83874

5'-pApA (sodium salt)

Cat.No: T35422

3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one)

Cat.No: T36133

Cat.No: T37832

Synonym: CAY10761

Cat. No.	Product Name	Target	Signaling Pathways
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

cGAMP diammonium

Cat.No: T73717

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