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28

抑制剂 & 化合物

9

天然产物

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Cat. No. Product Name Target Signaling Pathways
T36983 Cyclic-di-GMP disodium

Cyclic diguanylate,5GP-5GP disodium,3',5'-Cyclic diguanylic acid,Cyclic di-GMP (sodium salt),cyclic diguanylate disodium,c-di-GMP,c-di-GMP disodium

STING; Endogenous Metabolite Immunology/Inflammation; Metabolism
Cyclic-di-GMP disodium (5GP-5GP disodium) 是细菌的第二信使,也是一种 STING 激动剂,参与原核生物的多种过程,包括生物膜的形成、运动、和细胞周期的进展。Cyclic-di-GMP disodium 对癌细胞显示出抗增殖活性,可诱导 CD4 受体表达升高和细胞周期停滞。Cyclic-di-GMP disodium 可用于癌研究癌症。
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。
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。
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。
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。
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.
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。
T31597 Ecabapide

DQ2511,DQ 2511,DQ-2511

Others Others
Ecabapide (DQ-2511) 是一种新型促胃肠蠕动剂,能显著增强SHRSP的胃排空能力。Ecabapide 可激活的兔胃壁细胞中的环状 GMP 依赖性管家 Cl- 通道。
T31020 CP 461

OSI 461,UNII-68OJX9I7DT,CP-461,CP461

Apoptosis; PDE Apoptosis; Metabolism
CP 461 (UNII-68OJX9I7DT) 是一种特异性 PDE2A 抑制剂,是一种新型促凋亡化合物,能抑制环 GMP 磷酸二酯酶,但不能抑制环氧化酶-1 或-2。CP 461 在体外可抑制多种人类肿瘤细胞系的生长,并选择性地诱导癌细胞系而不是正常细胞凋亡。
T16344 NS-2028

Others; Guanylate cyclase GPCR/G Protein; Others
NS-2028 是一种高度选择性的可溶性鸟苷酸环化酶抑制剂。它抑制 3-吗啉代-sydnonimine 在人培养的脐静脉内皮细胞中形成环状 GMP,IC50为30mM。它抑制小鼠小脑匀浆和神经元 NO 合酶中的可溶性鸟苷酸环化酶活性,IC50分别为 17 和 20 mM。它可降低血管内皮生长因子诱导的血管生成和通透性。
T23009 MMPX

Others Others
calmodulin-sensitive cyclic GMP phosphodiesterase inhibitor
T38122 5'-pGpG (sodium salt)

5'-pGpG is a linearized form of cyclic di-GMP, a bacterial second messenger that activates the host innate immune system through stimulator of interferon genes (STING).1,2,3It is a metabolite of cyclic di-GMP formedviahydrolysis by various phosphodiesterases (PDEs) that binds to the cyclic di-GMP-I riboswitch with reduced affinity compared to cyclic di-GMP.4,55'-pGpG is intended for use as a negative control for cyclic di-GMP signaling.
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...
T81407 Prepro-Atrial Natriuretic Factor (26-55) (human)

Prepro-Atrial Natriuretic Factor (26-55) (human) 为促进肾皮质与髓质循环GMP水平上升的多肽,同时也增强肾腺苷酸环化酶的活性。
T37960 Guanylin(human) TFA

Guanylin (human) TFA is a 15-amino acid peptide that serves as an endogenous activator of intestinal guanylate cyclase. This compound is primarily located in the gastrointestinal tract, where it regulates electrolyte and water transport in the intestinal and renal epithelia through a mechanism dependent on cyclic GMP. [1][2]
T28391 PF-9404C

PF9404C

PF-9404C is the S-S diesteroisomer of a beta adrenergic receptors blocker with vasodilatory properties. PF9404C increased the formation of cyclic GMP from 3 pmol mg−1 protein in basal conditions, to 53 pmol mg−1 protein in 10 μM in rat aorta smooth muscle
T40895 Calmodulin antagonist-1

Calmodulin antagonist-1 (W-7) is a calmodulin (CaM) antagonist that effectively inhibits calmodulin-activated Ca 2+ -phosphodiesterase (PDE) with an IC 50 of 28 μM. This compound also competitively inhibits trypsin-treated Ca 2+ -PDE with respect to cyclic GMP, exhibiting an IC 50 of 375 μM and a K i value of 300 μM.
T21705 8-CPT-Cyclic AMP (sodium salt)

8-CPT-Cyclic AMP (8-CPT-cAMP) sodium 是环 AMP 依赖性蛋白激酶的选择性激活剂。 8-CPT-Cyclic AMP sodium 也是有效的环 GMP 特异性磷酸二酯酶(PDE VA)抑制剂,IC50为 0.9 μM。 8-CPT-Cyclic AMP sodium 还抑制 PDE III 和 PDE IV,IC50分别为 24 和 25 μM。8-CPT-Cyclic AMP sodium 对 Epac 具有非常高的亲和力,是一种有效的Epac 活化剂。
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。
T73609 Ribonuclease T1

Ribonuclease T1 (Rnase T1),常用于生化研究。Ribonuclease T1 是一种内切酶,可特异性降解单链 RNA。Ribonuclease T1 能够形成核苷 2′,3′-环磷酸中间体,以切割 3′-鸟苷残基与邻近核苷 5′-OH 基团之间的磷酸二酯键,产生 3′-GMP 末端寡核苷酸。
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...
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...
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...
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).
T36984 Cyclic di-IMP (sodium salt)

Cyclic di-IMP (sodium salt) (c-di-IMP) is a synthetic second messenger structurally related to the bacterial second messengers cyclic di-GMP and cyclic di-AMP . C-di-IMP has adjuvant properties when co-administered with antigens in vitro and by mucosal routes in vivo. C-di-IMP enriches the population of MHC class I and II, CD80, CD86, CD40, and CD54 positive dendritic cells derived from murine bone marrow. It also stimulates macrophages at 500 ng/ml. Mice immunized with β-galactosidase (β-gal) p...
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...
T37800 PF-04449613

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-0444...

化合物

Cyclic-di-GMP disodium
Cat.No: T36983
Synonym: Cyclic diguanylate,5GP-5GP disodium,3',5'-Cyclic diguanylic acid,Cyclic di-GMP (sodium salt),cyclic diguanylate disodium,c-di-GMP,c-di-GMP disodium
Target: STING, Endogenous Metabolite
G140
Cat.No: T9213
Synonym:
Target: cGAS
PF-06928215
Cat.No: T12432
Synonym:
Target: cGAS
IRAK4-IN-4
Cat.No: T11673
Synonym:
Target: IRAK, cGAS
RU.521
Cat.No: T5486
Synonym: RU320521
Target: DNA, cGAS
G150
Cat.No: T11344
Synonym:
Target: DNA, cGAS
cGAMP
Cat.No: T13606
Synonym: 3',3'-cGAMP,Cyclic GMP-AMP
Target: Others
2',3'-cGAMP
Cat.No: T10065
Synonym: 2'-3'-cyclic GMP-AMP
Target: STING, cGAS
Ecabapide
Cat.No: T31597
Synonym: DQ2511,DQ 2511,DQ-2511
Target: Others
CP 461
Cat.No: T31020
Synonym: OSI 461,UNII-68OJX9I7DT,CP-461,CP461
Target: Apoptosis, PDE
NS-2028
Cat.No: T16344
Synonym:
Target: Others, Guanylate cyclase
MMPX
Cat.No: T23009
Synonym:
Target: Others
5'-pGpG (sodium salt)
Cat.No: T38122
Synonym:
Target:
Cyclic di-UMP (sodium salt)
Cat.No: T36985
Synonym:
Target:
Prepro-Atrial Natriuretic Factor (26-55) (human)
Cat.No: T81407
Synonym:
Target:
Guanylin(human) TFA
Cat.No: T37960
Synonym:
Target:
PF-9404C
Cat.No: T28391
Synonym: PF9404C
Target:
Calmodulin antagonist-1
Cat.No: T40895
Synonym:
Target:
8-CPT-Cyclic AMP (sodium salt)
Cat.No: T21705
Synonym:
Target:
cGAS-IN-1
Cat.No: T78858
Synonym:
Target:
Ribonuclease T1
Cat.No: T73609
Synonym:
Target:
2'2'-cGAMP (sodium salt)
Cat.No: T35654
Synonym:
Target:
CU-76
Cat.No: T38329
Synonym:
Target:
CU-32
Cat.No: T38328
Synonym:
Target:
3'3'-cGAMP (sodium salt)
Cat.No: T38091
Synonym:
Target:
Cyclic di-IMP (sodium salt)
Cat.No: T36984
Synonym:
Target:
5'-pApA (sodium salt)
Cat.No: T35422
Synonym:
Target:
PF-04449613
Cat.No: T37800
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5065 GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD

Monosodium-GMP,cGMP sodium salt,鸟苷-3',5'-环磷酸一钠盐,Cyclic GMP

PKA Tyrosine Kinase/Adaptors
GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD (cGMP sodium salt) 也称为 cGMP,是一种细胞调节剂,被描述为第二信使。它的水平随着各种激素的增加而增加,包括乙酰胆碱、胰岛素和催产素。 cGMP 激活蛋白激酶 G(PKG) 并调节离子通道电导,信号传导影响多种过程,包括平滑肌松弛和增殖、光转导和能量稳态。
T72243 Cyclic-di-GMP diammonium

5GP-5GP diammonium,c-di-GMP diammonium ; cyclic diguanylate diammonium ; 5GP-5GP diammonium,c-di-GMP diammonium,cyclic diguanylate diammonium

Cyclic di-GMP (c-di-GMP) diammonium 是一种STING 激活剂和无处不在的第二信使,调节生物膜的形成、运动和各种细菌的毒力。
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。
T10909 Cyclic-di-GMP

c-di-GMP,cyclic diguanylate,5GP-5GP

Others Others
Cyclic-di-GMP is a STING agonist and ubiquitous second messenger, which regulates the formation, motility and virulence of biofilms in various bacterial species.
T64248 Cyclic-di-GMP sodium

Cyclic di-GMP sodium (c-di-GMP sodium) 是一种 STING 激活剂,也是一种无处不在的第二信使,具有调节生物膜的形成、运动和各种细菌的毒力的作用。
PDK0014 3-Methylxanthine

Endogenous Metabolite Metabolism
3-Methylxanthine 是一种黄嘌呤衍生物和环磷酸鸟苷(GMP)抑制剂,在豚鼠分离的气管肌肉中测得其IC50值为 920 μM。
T0167 Vinpocetine

长春西丁,RGH-4405,长春西汀,Ethyl apovincaminate

IκB/IKK; NF-κB; Sodium Channel; PDE Membrane transporter/Ion channel; Metabolism; NF-κB
Vinpocetine (RGH-4405) 是一种长春花生物碱衍生物,是阻断 Na+通道的阻断剂。Vinpocetine 抑制IKK 的IC50为 17.17 μM。Vinpocetine 也是PDE 抑制剂,并通过直接靶向IKK 抑制NF-κB 依赖性炎症反应,已被广泛用于研究脑血管疾病。
T3929 Kaurenoic acid

Kauren-19-Oic Acid,异贝壳杉烯酸,kaurenoate,kaur-16-en-18-oic acid

Others Others
Kaurenoic acid (kaurenoate) 是一种二萜,来源于 Sphagneticola trilobata 中,可以抑制细胞因子的产生和激活 NO–cyclic GMP–PKG–ATP- 敏感型钾通道信号通路,并抑制炎症疼痛。
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

GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD
Cat.No: T5065
Synonym: Monosodium-GMP,cGMP sodium salt,鸟苷-3',5'-环磷酸一钠盐,Cyclic GMP
Target: PKA
Cyclic-di-GMP diammonium
Cat.No: T72243
Synonym: 5GP-5GP diammonium,c-di-GMP diammonium ; cyclic diguanylate diammonium ; 5GP-5GP diammonium,c-di-GMP diammonium,cyclic diguanylate diammonium
Target:
2',3'-cGAMP sodium
Cat.No: T10065L
Synonym: 2'-3'-cyclic GMP-AMP sodium
Target: STING, cGAS
Cyclic-di-GMP
Cat.No: T10909
Synonym: c-di-GMP,cyclic diguanylate,5GP-5GP
Target: Others
Cyclic-di-GMP sodium
Cat.No: T64248
Synonym:
Target:
3-Methylxanthine
Cat.No: PDK0014
Synonym:
Target: Endogenous Metabolite
Vinpocetine
Cat.No: T0167
Synonym: 长春西丁,RGH-4405,长春西汀,Ethyl apovincaminate
Target: IκB/IKK, NF-κB, Sodium Channel, PDE
Kaurenoic acid
Cat.No: T3929
Synonym: Kauren-19-Oic Acid,异贝壳杉烯酸,kaurenoate,kaur-16-en-18-oic acid
Target: Others
cGAMP diammonium
Cat.No: T73717
Synonym:
Target:
TargetMol Loading
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