AG-490

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WARNING: This product is for research use only, not for human or veterinary use.

Description:Tyrphostin AG490 is a JAK-2 specific inhibitor, which inhibits phosphorylation of EGFR and signal transducer and activator of transcription 3 [STAT-3], and subsequently reduce invasion and adhesion potential of malignant cells. The hematopoietic cancer c-Kit+, Jak-2+ and non hematopoietic tumors c-Kit+, HER-2+, JAK-2+ can be inhibited by the chemosensitizing agent AG490 causing programmed cell death.

Price and Availability

AG-490 (99%), purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 200121Name: AG-490CAS#: 133550-30-8Chemical Formula: C17H14N2O3Exact Mass: 294.10044Molecular Weight: 294.3Elemental Analysis:C, 69.38; H, 4.79; N, 9.52; O, 16.31

Synonym:AG 490; AG490; AG-490; Tyrphostin AG 490

IUPAC/Chemical Name:(E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide

InChi Key:TUCIOBMMDDOEMM-RIYZIHGNSA-N

InChi Code:InChI=1S/C17H14N2O3/c18-10-14(8-13-6-7-15(20)16(21)9-13)17(22)19-11-12-4-2-1-3-5-12/h1-9,20-21H,11H2,(H,19,22)/b14-8+

SMILES Code:O=C(NCC1=CC=CC=C1)/C(C#N)=C/C2=CC=C(O)C(O)=C2

Technical Data

Additional Information

AG490 greatly inhibited osteoclast apoptosis. AG490 stimulated the phosphorylation of Akt and ERK. Adenovirus-mediated expression of dominant negative (DN)-Akt and DN-Ras in osteoclasts inhibited the survival of osteoclasts despite the presence of AG490. Cytochrome c release during osteoclast apoptosis was inhibited by AG490 treatment, but this effect was inhibited in the presence of LY294002 or U0126. AG490 suppressed the proapoptotic proteins Bad and Bim, which was inhibited in osteoclasts infected with DN-Akt and DN-Ras adenovirus. In addition, constitutively active MEK and myristoylated-Akt adenovirus suppressed the cleavage of pro-caspase-9 and -3 and inhibited osteoclast apoptosis induced by etoposide. Taken together, our results suggest that AG490 inhibited cytochrome c release into the cytosol at least partly by inhibiting the pro-apoptotic proteins Bad and Bim, which in turn suppressed caspase-9 and -3 activation, thereby inhibiting osteoclast apoptosis.   

References

1: DU AL, Ji TL, Yang B, Cao JF, Zhang XG, LiY, Pan S, Zhang B, Hu ZB, Zeng XW.  Neuroprotective effect of AG490 inexperimental traumatic brain injury of rats. Chin Med J (Engl). 2013Aug;126(15):2934-7. PubMed PMID: 23924471.