5.04173
MAT2A Inhibitor II, FIDAS-5
Synonym(s):
MAT2A Inhibitor II, FIDAS-5, FIDAS5, Methionine S-Adenosyltransferase 2A Inhibitor II, (E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline, Methionine S-Adenosyltransferase 2A Inhibitor II, FIDAS5, (E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline
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About This Item
Empirical Formula (Hill Notation):
C15H13ClFN
CAS Number:
Molecular Weight:
261.72
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
semisolid
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
form
semisolid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
SMILES string
Fc1c(c(ccc1)Cl)\C=C\c2ccc(cc2)NC
InChI key
KXVXICBOMOGFMH-JXMROGBWSA-N
General description
A cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) analogue of FIDAS-3 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MAT2A
MAT2A
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Zhang, W., et al. 2013. ACS Chem. Biol.8, 796.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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