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Merck

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:
503473-32-3
Molecular Weight:
228.24
MDL number:
MFCD06411462
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

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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

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

Quality Level

100

Related Categories

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
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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