DMOG
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
DMOG(Dimethyloxalylglycine)对从鸡胚肺中提取的羟脯氨酸合成有抑制作用,对应于从组织和培养基来源的其IC50值分别为9.3 μM和3.7 μM[1]。
DMOG是脯氨酰-4-羟基化酶域(PHD)酶的一个抑制剂,可调节低氧诱导因子(HIF)的稳定性。感染和炎症的一个特征是局部组织缺氧,通过氧传感羟化酶的抑制可导致转录因子HIF-1α和NF-β的上调。
在体外正常氧环境下,0.1到1 mmol/L的DMOG可使HIF-1α的表达稳定[2]。
在体内,DMOG预处理削弱了LPS-诱导的NF-κB通路的激活。LPS诱导刺激下,处理了DMOG的老鼠存活率明显增加。此外,DMOG处理上调了IL-10的表达量,特别是在腹膜B-1细胞群中[3]。
临床试验:目前没有相关的临床数据。
参考文献:
[1] Baader E, Tschank G, Baringhaus KH, Burghard H, Günzler V. Inhibition of prolyl 4-hydroxylase by oxalyl amino acid derivatives in vitro, in isolated microsomes and in embryonic chicken tissues. Biochem J. 1994 Jun 1;300 ( Pt 2):525-30.
[2] Jaakkola P, Mole DR, Tian YM, Wilson MI, Gielbert J, Gaskell SJ, von Kriegsheim A, Hebestreit HF, Mukherji M, Schofield CJ, Maxwell PH, Pugh CW, Ratcliffe PJ. Targeting of HIF-alpha to the von Hippel-Lindau ubiquitylation complex by O2-regulated prolyl hydroxylation. Science. 2001 Apr 20;292(5516):468-72.
[3] Hams E, Saunders SP, Cummins EP, O'Connor A, Tambuwala MT, Gallagher WM, Byrne A, Campos-Torres A, Moynagh PM, Jobin C, Taylor CT, Fallon PG. The hydroxylase inhibitor dimethyloxallyl glycine attenuates endotoxic shock via alternative activation of macrophages and IL-10 production by B1 cells. Shock. 2011 Sep;36(3):295-302.
- 1. Vijesh J. Bhute, James Harte, et al. "AMannose binding lectin is hydroxylated by collagen prolyl-4-hydroxylase and inhibited by some PHD inhibitors." Kidney360. April 3, 2020.
- 2. Zhang Y, Zheng D, et al. "Aberrant hydroxymethylation of ANGPTL4 is associated with selective intrauterine growth restriction in monochorionic twin pregnancies." Epigenetics. 2020;1-13. PMID:32114885
- 3. Luo A, Chen Y. "Label-free Interactome Analysis Revealed an Essential Role of CUL3-KEAP1 Complex in Mediating the Ubiquitination and Degradation of PHD2." J Proteome Res. 2019 Nov 25. PMID:31763849
Storage | Store at -20°C |
M.Wt | 175.14 |
Cas No. | 89464-63-1 |
Formula | C6H9NO5 |
Solubility | ≥17.8 mg/mL in EtOH with ultrasonic; ≥34.47 mg/mL in H2O with ultrasonic; ≥8.75 mg/mL in DMSO |
Chemical Name | methyl 2-[(2-methoxy-2-oxoethyl)amino]-2-oxoacetate |
SDF | Download SDF |
Canonical SMILES | COC(=O)CNC(=O)C(=O)OC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
B1细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于8.8 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
1 mM,2 hours |
应用 |
在腹膜M中DMOG上调磷酸化p50(S337)。 |
动物实验 [1]: | |
动物模型 |
BALB/c和C57BL/6小鼠 |
给药剂量 |
8 mg/mouse,腹腔注射 |
应用 |
LPS诱导休克后,DMOG明显增加生存率。在腹膜B-1细胞中,DMOG上调了IL-10的表达。手术前接受DMOG治疗的小鼠产生疾病症状的严重恶化,死亡率明显升高。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Hams E, Saunders S P, Cummins E P, et al. The hydroxylase inhibitor DMOG attenuates endotoxic shock via alternative activation of macrophages and IL-10 production by B-1 cells[J]. Shock (Augusta, Ga.), 2011, 36(3): 295. |
描述 | DMOG是细胞通透的竞争性HIF-PH抑制剂。 | |||||
靶点 | HIF-PH | |||||
IC50 |
质量控制和MSDS
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