48208-26-0
中文名稱
RG108
英文名稱
RG108
CAS
48208-26-0
分子式
C19H14N2O4
MDL 編號
MFCD08705332
分子量
334.33
MOL 文件
48208-26-0.mol
更新日期
2024/12/23 17:39:04
48208-26-0 結(jié)構(gòu)式
基本信息
中文別名
N-鄰苯二甲?；?L-色氨酸 英文別名
RG108 >98%RG108/RG-108
N-Phthalyl-L-tryptophan
N-Phthaloyl-L-tryptophan
DNA Methyltransferase Inhibitor
RG108/DNA Methyltransferase Inhibitor/N-Phthalyl-L-tryptophan
(S)-2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl)propanoic acid
(S)-3-(Indol-3-yl)-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)propanoic acid
1H-Indole-3-propanoic acid, α-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-, (αS)-
N-Phthaloyl-L-tryptophan (S)-3-(Indol-3-yl)-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)propanoic acid
所屬類別
生物化工：DNA Methyltransferase 抑制劑物理化學性質(zhì)
熔點192-194℃
沸點606.0±50.0 °C(Predicted)
密度1.502±0.06 g/cm3(Predicted)
儲存條件-20°C
儲存條件Store at RT
溶解度二甲基亞砜：>10mg/mL
酸度系數(shù)(pKa)3.62±0.10(Predicted)
形態(tài)粉末
顏色黃色
敏感性感光
穩(wěn)定性可在-20°下的DMSO或乙醇溶液保存長達1個月。
CAS 數(shù)據(jù)庫48208-26-0
常見問題列表
生物活性
RG108是一種DNA甲基轉(zhuǎn)移酶抑制劑，IC50為115 nM，不會引起共價酶的誘捕。體外研究
RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences. In another study, the synthesis and in vitro analysis of a biotinylated RG108 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes. In a recent study, it is shown RG108 can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs.生物活性
RG108 (N-Phthalyl-L-tryptophan)是一種DNA methyltransferase抑制劑，無細胞試驗中IC50為115 nM，不會引起共價酶的誘捕。靶點
| Target | Value |
|
DNA methyltransferase
(Cell-free assay) | 115 nM |
體外研究
RG108有效阻斷體外人細胞系中DNA甲基轉(zhuǎn)移酶，并且不會引起共價酶俘獲。細胞用低微摩爾濃度的RG108培育，導致基因組DNA顯著脫甲基化，而沒有可檢測的毒性。有趣的是，RG108引起腫瘤抑制基因脫甲基和再活化，但是它不影響著絲?；蛐蛄械募谆Ｔ诹硪粋€研究中，進行生物素化RG108綴合物的合成和體外分析以評估與DNA甲基轉(zhuǎn)移酶的相互作用。最近的研究表明，與天然SMs相比，RG108能夠顯著降低SM衍生的iPS細胞中DNA活性。