产品说明
一般描述
A cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) analogue of FIDAS-3 (Cat. No. 681677) that is >2-fold more potent than FIDAS-3 in inhibiting MAT2A-catalyzed SAM (S-adenosylmethionine) synthesis both in cell-free (IC50 = 2.1 µM with FIDAS-5 vs. 4.9 µM with FIDAS-3; [L-Met] = [ATP] = 1 mM, [MAT2A] = 10 µg/mL; 20 min FIDAS preincubation prior to 30 min reaction) and cell-based (64% and 56% decrease of SAM and SAH level, respectively, in LS174T cells after 36 h treatment with either 3 µM FIDAS-5 or 10 µM FIDAS-3) assays. FIDAS-5 at 3 µM is shown to completely inhibit the proliferation of LS174T CRC (colorectal cancer) for up to 7 d in vitro and, when administered orally, effectively suppress HT29 CRC tumor expansion in mice in vivo (by 58% on d 18 post HT29 xenograft; 20 mg/kg/day starting d 4). Computer-aided in silico modeling predicts that FIDAS-3 & -5 target SAM-binding pocket at the interface of MAT2A dimer and in vitro binding studies reveals FIDAS-3 effectively competes against SAM for MAT2A binding.
A cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) analogue of FIDAS-3 (Cat. No. 681677) that competes against SAM for MAT2A binding and is >2-fold more potent than FIDAS-3 in inhibiting MAT2A-catalyzed SAM synthesis both in cell-free assays (IC50 = 2.1 µM) and in LS174T colorectal cancer (CRC) cultures (3 µM). FIDAS-5 at 3 µM is shown to completely inhibit the proliferation of LS174T for up to 7 d in vitro and effectively suppress HT29 CRC tumor expansion in mice in vivo (20 mg/kg/day p.o.).
生化/生理作用
Cell permeable: yes
Reversible: yes
Primary Target
MAT2A
包装
Packaged under inert gas
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
Zhang, W., et al. 2013. ACS Chem. Biol.8, 796.
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 | C15H13ClFN |
分子量 | 261.72 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | semisolid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | yellow |
溶解性 | DMSO: 100 mg/mL |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 2 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich