SML2200
辛-(R)-2HG
≥98% (HPLC), film, α-KG-dependent dioxygenases prolyl hydroxylases inhibitor
别名:
(2R)-2-羟基戊二酸辛酯, (2R)-辛基-α-羟基戊二酸, 1-辛基-D-2-羟基戊二酸盐, 1-辛基酯, R-2HG 辛基酯, 羟基戊二酸, 辛-D-2HG, 辛基-2HG
产品名称
辛-(R)-2HG, ≥98% (HPLC)
方案
≥98% (HPLC)
表单
film
储存条件
desiccated
颜色
colorless
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
O[C@H](CCC(=O)O)C(=O)OCCCCCCCC
InChI key
UJZOKTKSGUOCCM-LLVKDONJSA-N
相关类别
应用
辛基-（R）-2羟基戊二酸酯（HG）已被用作胶质母细胞瘤细胞中的膜渗透性致癌代谢物（oncometabolite），用于测试其对NANOG转录因子表达的影响。它还被用作酮戊二酸酯（α-KG）依赖性脱氧酶α的竞争性抑制剂。
生化/生理作用
抑制 α-酮戊二酸/α-KG 依赖性双加氧酶类的肿瘤代谢产物 D-2-羟基戊二酸的膜渗透前体形式。
辛基-(R)-2HG (Octyl-D-2HG) 是肿瘤细胞因 NADP + 依赖性异柠檬酸脱氢酶基因 IDH1 和 IDH2 突变而产生的肿瘤代谢产物 D-2-羟基戊二酸盐 (D-2HG) 的膜渗透前体形式。D-2HG 通过与 α-KG 结合竞争抑制多种 α-酮戊二酸/α-KG-依赖性双加氧酶。通过 Octyl-(R)-2HG 处理 (1-50 mM) 的细胞 D-2HG 传递显示出抑制脱甲基酶活性（~148%H3K9me2 和 ~310%H3K79me2 上调；U-87 mg 中 50 mm）以及因为分别抑制 α-KG-依赖性双加氧酶脯氨酰羟化酶 (PHD) 和胶原脯氨酰-4-羟化酶 (C-P4H)而增加 HIF-1α通过, 降低内皮抑素水平。
制备说明
该化合物未报告密度。分子量为260.33。DMSO中的溶解性经测试为2 mg/mL，然而其他数据来源表明其在DMSO中的溶解度可高达10 mg/mL。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Zachary J Reitman et al.
The Journal of biological chemistry, 289(34), 23318-23328 (2014-07-06)
Mutations in the cytosolic NADP(+)-dependent isocitrate dehydrogenase (IDH1) occur in several types of cancer, and altered cellular metabolism associated with IDH1 mutations presents unique therapeutic opportunities. By altering IDH1, these mutations target a critical step in reductive glutamine metabolism, the
alpha-Ketoglutarate-Activated NF-$\kappa$B Signaling Promotes Compensatory Glucose Uptake and Brain Tumor Development
Wang X, et al.
Molecular Cell, 76(1), 148-162 (2019)
IDH1R132H Causes Resistance to HDAC Inhibitors by Increasing NANOG in Glioblastoma Cells
Kim G H, et al.
International Journal of Molecular Sciences, 20(11), 2679-2679 (2019)
Steven M Chan et al.
Nature medicine, 21(2), 178-184 (2015-01-20)
Mutant isocitrate dehydrogenase (IDH) 1 and 2 proteins alter the epigenetic landscape in acute myeloid leukemia (AML) cells through production of the oncometabolite (R)-2-hydroxyglutarate (2-HG). Here we performed a large-scale RNA interference (RNAi) screen to identify genes that are synthetic
Makoto Hirata et al.
Proceedings of the National Academy of Sciences of the United States of America, 112(9), 2829-2834 (2015-03-03)
Enchondromas are benign cartilage tumors and precursors to malignant chondrosarcomas. Somatic mutations in the isocitrate dehydrogenase genes (IDH1 and IDH2) are present in the majority of these tumor types. How these mutations cause enchondromas is unclear. Here, we identified the
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