AG 494 - CAS 139087-53-9
Catalog number: 139087-53-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C16H12N2O3
Molecular Weight:
280.28
COA:
Inquire
Targets:
EGFR
Description:
AG-494 is a EGFR (epidermal growth factor receptor) kinase inhibitor with IC50 value of 0.7 μM. It is selective over ErbB2, PDGFR and insulin receptor kinase (IC50 values are 42, 6 and > 100 μM respectively). AG-494 tyrphostin also can block Cdk2 activation.
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Purity:
98%
Appearance:
Yellow solid
Synonyms:
alpha-Cyano-(3,4-dihydroxy)-N-phenylcinnamide; Tyrphostin AG-494; Tyrphostin B48
Solubility:
Soluble to 5 mM in ethanol and to 50 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
HKHOVJYOELRGMV-XYOKQWHBSA-N
InChI:
1S/C16H12N2O3/c17-10-12(8-11-6-7-14(19)15(20)9-11)16(21)18-13-4-2-1-3-5-13/h1-9,19-20H,(H,18,21)/b12-8+
Canonical SMILES:
C(\C(=C\c1cc(c(cc1)O)O)C#N)(=O)Nc1ccccc1
1.The inhibitory mechanisms of the tyrosine kinase inhibitors herbimycin a, genistein, and tyrphostin B48 with regard to the function of the aryl hydrocarbon receptor in Caco-2 cells.
Kasai S1, Kikuchi H. Biosci Biotechnol Biochem. 2010;74(1):36-43. Epub 2010 Jan 7.
The aryl hydrocarbon receptor (AhR) is a transcription factor that is activated by dioxin and related xenobiotics. Although the activation of AhR is inhibited by tyrosine kinase inhibitors, the molecular mechanism has not been clarified. In the current study, the inhibitory mechanisms of several inhibitors of tyrosine kinase, herbimycin A, genistein, and tyrphostin B48, on AhR activation was analyzed in human Caco-2 cells. All the inhibitors suppressed the transcriptional activation of AhR induced by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). Herbimycin A induced down-regulation of the AhR protein by inhibiting its molecular chaperone heat shock protein 90 (HSP90). In contrast, genistein and tyrphostin B48 inhibited the nuclear localization of AhR induced by TCDD, although the amount of AhR protein was not altered. The inhibitory effects of genistein and tyrphostin B48 on endogenous tyrosine kinase activity were evaluated by detection of alterations in the tyrosine phosphorylation states of cellular proteins.
2.Tyrphostin AG 494 blocks Cdk2 activation.
Osherov N1, Levitzki A. FEBS Lett. 1997 Jun 30;410(2-3):187-90.
We have previously shown that the EGFR kinase selective tyrphostin AG 494 fails to inhibit EGFR kinase in intact cells. Yet, AG 494 proved to inhibit EGF- or serum-induced cell proliferation (Osherov et al., J. Biol. Chem. 268 (1993) 11134-11142). In this preliminary communication we show that AG 494 as well as its close analogs AG 490 and AG 555 block Cdk2 activation. In contrast, AG 1478, a more selective EGFR kinase blocker which is also active as EGFR kinase blocker in intact cells, fails to do so. AG 494 exerts its full inhibitory activity on Cdk2 activation even when added 20 h subsequent to EGF addition when Cdk2 activation is maximal. The inhibitory activity on Cdk2 activation parallels its DNA synthesis inhibitory activity, strongly suggesting that its target is one of the molecular mechanisms involved in Cdk2 activation. AG 494 and its analogs may become useful lead compounds for the development of drugs aimed at the cell cycle machinery.
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CAS 139087-53-9 AG 494

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