半岛bd体育手机客户端 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 (Pro564and Pro530in HIF-1α and HIF-2α, respectively) and aspartyl/asparanginyl β-hydroxylase-catalyzed CAD Asp hydroxylation (Asn803and Asn851in 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 modelin 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 (Pro564and Pro530in HIF-1α and HIF-2α, respectively) and aspartyl/asparanginyl β-hydroxylase-catalyzed CAD Asp hydroxylation (Asn803and Asn851in 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 modelin 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
经验(实验)分子式 | C6H9NO5 |
分子量 | 175.14 |
MDL编号 | MFCD05865098 |
NACRES | NA.77 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze desiccated (hygroscopic) |
颜色 | pink-white to peach-white |
溶解性 | DMSO: 50 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
InChI | 1S/C6H9NO5/c1-11-4(8)3-7-5(9)6(10)12-2/h3H2,1-2H3,(H,7,9) |
InChI key | BNJOZDZCRHCODO-UHFFFAOYSA-N |
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 |
Sigma-Aldrich