DMOG 是一种有效的 HI F脯氨酰羟化酶抑制剂，以及 α-ketoglutarate 辅因子的拮抗剂

基本信息

技术规格

物性(参考值)

产品说明

应用

二甲基草酰甘氨酸(DMOG)用作TET3蛋白抑制剂。
DMOG用于：

• 缺氧诱导因子(HIF)活性测定
• 研究其对HIF-1α降解和肾脏再生的影响
• 脂肪组织DMOG预处理
• CD34⁺细胞原代液体培养的媒介对照
• 刺激内皮细胞

包装

10, 50 mg in glass bottle

生化/生理作用

DMGO是一种细胞渗透脯氨酸-4-羟化酶抑制剂，上调HIF(缺氧诱导因子)。HIF蛋白质水平-1α 后转录亚基被脯氨酰和天冬酰胺羟化酶调节(PAH)。PAH活性抑制增强了内源性HIF-1α水平。DMGO是一种细胞透过性、含蛋白脯氨酰羟化酶结构域的竞争性抑制剂(PHDs和HIF-PHs)。已经发现DMOG通过葡萄糖代谢保存对于NFG缺乏细胞培养有神经元保护效果。DMOG在兔子缺血再灌注模型中也可以减轻心肌损伤。DMOG比以前的抑制剂4-苯基-吡啶-2,5-二羧酸更有效(R395889；sigma-aldrich稀有化学文库)。IC₅₀ is 5.18 μM.

特点和优势

该化合物是基因调控研究的特色产品。点击此处以了解更多的基因调控特色产品。可访问sigma.com/discover-bsm了解更多关于用于其他研究领域生物活性小分子。

基本信息

产品性质

安全信息

象形图
警示用语：	Warning
危险声明	H302
预防措施声明	P301 + P312 + P330
危险分类	Acute Tox. 4 Oral
储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

产品说明

一般描述

A cell-permeable 2-OG (2-oxoglutarate) analog that is expected to act as a competitive inhibitor against all 2-OG-dependent dioxygenases. Effectively upregulates normoxia HIF-α transcription activity (effective conc. = 1 mM in cultures) by inhibiting HIF-PH- (HIF-α-prolyl hydroxylase) catalyzed ODD (oxygen-dependent degradation domain) Prolyl hydroxylation (Pro⁵⁶⁴ and Pro⁵³⁰ in HIF-1α and HIF-2α, respectively) and aspartyl/asparanginyl β-hydroxylase-catalyzed CAD Asp hydroxylation (Asn⁸⁰³ and Asn⁸⁵¹ in HIF-1α and HIF-2α, respectively), resulting in a blockage of pVHL (von Hippel-Lindau) ubiquitin ligase complex-mediated HIF-α degradation and a simultaneous promotion of HIF CAD (COOH-terminal activation domain) p300/CBP association. DMOG is also demonstrated to augment artery ligation-induced up-regulation of HIF-1α and FLK (by 100% and 40%, respectively, in 11 days; 8 mg/0.5 ml/animal/i.p.; q.o.d.) in muscle tissues in a murine ischaemic model in vivo.
A cell-permeable 2-OG (2-oxoglutarate) analog that is expected to act as a competitive inhibitor against all 2-OG-dependent dioxygenases. Effectively upregulates normoxia HIF-α transcription activity (effective conc. = 1 mM in cultures) by inhibiting HIF-PH- (HIF-α-prolyl hydroxylase) catalyzed ODD (oxygen-dependent degradation domain) Prolyl hydroxylation (Pro⁵⁶⁴ and Pro⁵³⁰ in HIF-1α and HIF-2α, respectively) and aspartyl/asparanginyl β-hydroxylase-catalyzed CAD Asp hydroxylation (Asn⁸⁰³ and Asn⁸⁵¹ in HIF-1α and HIF-2α, respectively), resulting in a blockage of pVHL (von Hippel-Lindau) ubiquitin ligase complex-mediated HIF-α degradation and a simultaneous promotion of HIF CAD (COOH-terminal activation domain) p300/CBP association. DMOG is also demonstrated to augment artery ligation-induced up-regulation of HIF-1α and FLK (by 100% and 40%, respectively, in 11 days; 8 mg/0.5 ml/animal/i.p.; q.o.d.) in muscle tissues in a murine ischaemic model in vivo.

包装

50 mg in Glass bottle

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Pollard, P.J., et al. 2008. Biochem. J.416, 387.
Chen, H., et al. 2006. Cancer Res.66, 9009.
Milkiewicz, M., et al. 2004. J. Physiol.560, 21.
Lando, D., et al. 2002. Science295, 858.
Jaakkola, P., et al. 2001. Science292, 468.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息

象形图
警示用语：	Warning
危险声明	H302
预防措施声明	P264 - P270 - P301 + P312 - P501
危险分类	Acute Tox. 4 Oral
储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

基本信息

安全信息

图形或危害标志
危险性说明	H302: Harmful if swallowed. H315: Causes skin irritation. H319: Causes serious eye irritation. H332: Harmful if inhaled. H335: May cause respiratory irritation.
防范说明	P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing . P264: Wash hands thoroughly after handling. P270: Do not eat, drink or smoke when using this product. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P301 + P312: IF SWALLOWED: Call a POISON CENTER or doctor/physician if you feel unwell. P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing.. P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see relevant procedures. on this label). P330: Rinse mouth. P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to in accordance with local regulation .