Cyclic di-GMP
(Synonyms: 环二鸟苷酸,c-di-GMP; cyclic diguanylate; 5GP-5GP) 目录号 : GC15048
Cyclic di-GMP是一种干扰素基因刺激因子（STING）激动剂。Cyclic di-GMP是一种环状二核苷酸，是细菌第二信使，能够调节不同细菌的生物膜形成、运动性和毒力。
Cas No.:61093-23-0
Sample solution is provided at 25 µL, 10mM.
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Cyclic di-GMP is a stimulator of interferon genes (STING) agonist[1]. Cyclic di-GMP is a cyclic dinucleotide and a bacterial second messenger that regulates biofilm formation, motility and virulence of different bacteria[2]. Cyclic di-GMP has anti-cancer cell proliferation activity and can also induce increased CD4 receptor expression and cell cycle arrest[3].
In vitro, treatment of human cecal adenocarcinoma H508 cells with Cyclic di-GMP (0.5-50μM) for 5 days inhibited basal cell proliferation as well as cell proliferation stimulated by acetylcholine and epidermal growth factor (EGF)[4]. Treatment of lymphoblastoid CD4+ Jurkat cell line with Cyclic di-GMP (50μM) significantly increased intracellular CD4 expression and led to S phase arrest of the cell cycle[5].
In vivo, Cyclic di-GMP (100µg) was administered intravenously to mice bearing B16F10 cell xenografts, which effectively enhanced the immune response produced by the TriVax vaccine and induced the production of more antigen-specific CD8 T cells in mice[6].
References:
[1] Burdette D L, Monroe K M, Sotelo-Troha K, et al. STING is a direct innate immune sensor of cyclic di-GMP[J]. Nature, 2011, 478(7370): 515-518.
[2] Jenal U, Reinders A, Lori C. Cyclic di-GMP: second messenger extraordinaire[J]. Nature Reviews Microbiology, 2017, 15(5): 271-284.
[3] Li A, Yi M, Qin S, et al. Activating cGAS-STING pathway for the optimal effect of cancer immunotherapy[J]. Journal of hematology & oncology, 2019, 12: 1-12.
[4] Karaolis D K R, Cheng K, Lipsky M, et al. 3′, 5′-Cyclic diguanylic acid (c-di-GMP) inhibits basal and growth factor-stimulated human colon cancer cell proliferation[J]. Biochemical and biophysical research communications, 2005, 329(1): 40-45.
[5] Steinberger O, Lapidot Z, Ben-Ishai Z, et al. Elevated expression of the CD4 receptor and cell cycle arrest are induced in Jurkat cells by treatment with the novel cyclic dinucleotide 3′, 5′-cyclic diguanylic acid[J]. FEBS letters, 1999, 444(1): 125-129.
[6] Wang Z, Celis E. STING activator c-di-GMP enhances the anti-tumor effects of peptide vaccines in melanoma-bearing mice[J]. Cancer Immunology, Immunotherapy, 2015, 64: 1057-1066.
Cyclic di-GMP是一种干扰素基因刺激因子（STING）激动剂[1]。Cyclic di-GMP是一种环状二核苷酸，是细菌第二信使，能够调节不同细菌的生物膜形成、运动性和毒力[2]。Cyclic di-GMP具有抗癌细胞增殖活性，还能够诱导CD4受体表达升高和细胞周期停滞[3]。
在体外，Cyclic di-GMP（0.5-50μM）处理人类盲肠腺癌H508细胞5天，抑制了细胞基础增殖以及乙酰胆碱和表皮生长因子（EGF）刺激的细胞增殖[4]。Cyclic di-GMP（50μM）处理淋巴母细胞CD4+ Jurkat细胞系，显著提高了细胞内CD4的表达，导致了细胞周期S期阻滞[5]。
在体内，Cyclic di-GMP（100µg）通过静脉注射治疗B16F10细胞异种移植小鼠，有效增强了TriVax疫苗产生的免疫反应强度，诱导了小鼠体内产生更多抗原特异性CD8 T细胞[6]。
| Cell experiment [1]: | |
Cell lines | Human cecal adenocarcinoma (H508 cells) |
Preparation Method | H508 cells were incubated in the absence or presence of a growth stimulant [acetylcholine (300μM) and epidermal growth factor (EGF) (1ng/mL)] for 5 days alone or with increasing concentrations of Cyclic di-GMP (0.5–50μM). Cell proliferation was determined by the sulforhodamine blue (SRB) colorimetric assay. |
Reaction Conditions | 0.5–50μM; 5 days |
Applications | Increasing concentrations of Cyclic di-GMP inhibit basal, and acetylcholine- and EGF-stimulated colon cancer cell proliferation. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Mice (five per group) were subcutaneously injected with 4×105 B16F10 cells in the shaved rear flank. Eight days later, they received the first vaccine (prime) intravenously (200µL/injection via tail vein), TriVax consisted of a mixture of 120μg Pam-hgp100, 100µg hgp100 or 100µg Ova, 50µg anti CD40 antibody, and 25μg Poly-IC. Nine days after priming, a booster was administered with the same components except for a reduced anti-CD40 dose (25µg). In some experiments, 100µg Cyclic di-GMP was added to both prime and boost. Tumor growth was monitored every 2-3 days by measuring two perpendicular diameters, and mice were euthanized when the tumor area exceeded 400mm2 or if ulceration or >20% weight loss occurred. |
Dosage form | 100µg; given two sequential vaccinations 9 days apart (prime and boost); i.v. |
Applications | The administration of Cyclic di-GMP is effective in potentiating the magnitude of the immune responses generated by TriVax. TriVax in combination with Cyclic di-GMP induced significantly higher numbers of antigen-specific CD8 T cells as compared to TriVax w/o Cyclic di-GMP. |
References: | |
| Cas No. | 61093-23-0 | SDF | |
| 别名 | 环二鸟苷酸,c-di-GMP; cyclic diguanylate; 5GP-5GP | ||
| 化学名 | 9,9'-((2R,3R,3aS,7aR,9R,10R,10aS,14aR)-3,5,10,12-tetrahydroxy-5,12-dioxidodecahydrodifuro[3,2-d:3',2'-j][1,3,7,9,2,8]tetraoxadiphosphacyclododecine-2,9-diyl)bis(2-amino-1H-purin-6(9H)-one) | ||
| Canonical SMILES | O=C1NC(N)=NC2=C1N=CN2[C@H](O[C@@]([C@@]3([H])OP(O)(OC[C@]([C@@]4([H])OP5(O)=O)(O[C@@H](N6C(N=C(N)NC7=O)=C7N=C6)[C@@H]4O)[H])=O)(CO5)[H])[C@@H]3O | ||
| 分子式 | C20H24N10O14P2 | 分子量 | 690.41 |
| 溶解度 | Soluble in Water | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4484 mL | 7.2421 mL | 14.4841 mL |
| 5 mM | 0.2897 mL | 1.4484 mL | 2.8968 mL |
| 10 mM | 0.1448 mL | 0.7242 mL | 1.4484 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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