655203
TX-1918
A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K, while it inhibits other kinases at much higher concentrations.
Synonym(s):
TX-1918, 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
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About This Item
Empirical Formula (Hill Notation):
C14H12O3
CAS Number:
Molecular Weight:
228.24
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light orange
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
Oc1c(cc(cc1C)C=C2C(=O)C=CC2=O)C
InChI
1S/C14H12O3/c1-8-5-10(6-9(2)14(8)17)7-11-12(15)3-4-13(11)16/h3-7,17H,1-2H3
InChI key
YHWRISYBKMXSGJ-UHFFFAOYSA-N
General description
A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM), while it inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Displays potent antitumor activity (EC50 = 2.07 and 230 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
eEF2-K
eEF2-K
Product does not compete with ATP.
Reversible: no
Target IC50: 440 nM against eEF2-K
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Other Notes
Hori, H., et al. 2002. Bioorg. Med. Chem.10, 3257.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
Storage Class
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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