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TX-1918 - CAS 503473-32-3 - Calbiochem

Sigma-Aldrich

Catalog No.
C15-1244-415
Manufacturer No.
655203-10MG
Manufacturer Name
Sigma-Aldrich
Quantity
10
Unit of Measure
MG
Price: $343.47
List Price: $381.63

A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC 50 = 440 nM), while it inhibits other kinases at much higher concentrations (IC 50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and

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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.

A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM). Inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Reported to exhibit potent anti-tumor 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). May be useful as a therapeutic agent for cancer treatment in animal models.

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

Warning

Toxicity: Harmful (C)

Reconstitution

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

UPC:
42204012
Condition:
New
Weight:
1.00 Ounces
HazmatClass:
No
WeightUOM:
LB
MPN:
655203-10MG


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