MAT2A Inhibitor II, FIDAS-5-Calbiochem

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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 ?M with FIDAS-5 vs. 4.9 ?M with FIDAS-3; [L-Met] = [ATP] = 1 mM, [MAT2A] = 10 ?g/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 ?M FIDAS-5 or 10 ?M FIDAS-3) assays. FIDAS-5 at 3 ?M is shown to completely inhibit the proliferation of LS174T CRC (colorectal cancer) for up to 7 din vitroand, when administered orally, effectively suppress HT29 CRC tumor expansion in micein vivo(by 58% on d 18 post HT29 xenograft; 20 mg/kg/day starting d 4). Computer-aidedin silicomodeling predicts that FIDAS-3 & -5 target SAM-binding pocket at the interface of MAT2A dimer andin vitrobinding 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 ?M) and in LS174T colorectal cancer (CRC) cultures (3 ?M). FIDAS-5 at 3 ?M is shown to completely inhibit the proliferation of LS174T for up to 7 din vitroand effectively suppress HT29 CRC tumor expansion in micein 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

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