GW 441756 Inhibitor CAS No. 504433-23-2

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KI3455	GW 441756	Quote	Quote

Chemical Characteristic

Product Name	GW 441756
CAS No.	504433-23-2
Molecular Weight	275.30462
Formula	C₁₇H₁₃N₃O
Chemical Name	2H-Pyrrolo[3,2-b]pyridin-2-one, 1,3-dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-
Smiles	c12c(cccn1)NC(=O)/C/2=C\c1cn(c2c1cccc2)C
Chemical Structure

Biological activities

GW441756 is a potent and selective inhibitor of the NGF receptor tyrosine kinase A (TrkA). GW441756 inhibits all three Trk kinases (TrkA, TrkB and TrkC) induced NFAT-bla reporter activity.^[1] The IC50s of GW441756 are 0.23, 0.14 and 0.46 µM against TrkA, TrkB and TrkC, respectively.^[2] GW441756 also inhibits the phosphorylation of LRRK2 and the IC50 of GW441756 against LRRK2 is 320 nM.^[3] GW441756 binds to the ATP binding site of the TRK receptors and inhibits the theyrosine phosphorylation and kinase activity of TRK receptors.^[4] Furthermore, GW441756 upregulates p75NTR receptor expression and leads to apoptosis via caspase-3 activation.^[4] In vitro, GW441756 specifically blocks TrkA-induced cell death in a dose-dependent manner, and blocks TrkA-mediated γH2AX production in TrkA-overexpressing cells.^[5] In vivo, GW441756 inhibits the EPSC by decreasing the function of deltorphin.^[6]

Protocols

In vitro, GW441756 is dissolved in DMSO.^[5]

References

[1] Wood ER, et al. Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg Med Chem Lett. 2004, 14(4):953-957. [2] Wang J, et al. Cellular assays for high-throughput screening for modulators of Trk receptor tyrosine kinases. Curr Chem Genomics. 2008, 1:27-33. [3] Hermanson SB, et al. Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation. PLoS One. 2012, 7(8):e43580. [4] M Stabile, et al. Antiproliferative and Proapoptotic Effects of the TrK-inhibitor GW441756 in Human Myosarcomas and Prostatic Carcinoma. Current Signal Transduction Therapy. 2013, 8 (1): 74-83. [5] Jung EJ, et al. Cytosolic accumulation of gammaH2AX is associated with tropomyosin-related kinase A-induced cell death in U2OS cells. Exp Mol Med. 2008, 40(3):276-285. [6] Bie B, et al. Nerve growth factor-regulated emergence of functional delta-opioid receptors. J Neurosci. 2010, 30(16):5617-5628.

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