GW5074 - CAS 220904-83-6
Catalog number:
220904-83-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Raf
Description:
GW5074 is a c-Raf inhibitor. GW5074 has no direct effect on the activities of several apoptosis-associated kinases when assayed in vitro. In contrast to its effect in vitro, treatment of neurons with GW5074 causes c-Raf activation (when measured in vitro in the absence of the drug) and stimulates the Raf-MEK-ERK pathway. GW5074 prevents neurodegeneration and improves behavioral outcome in an animal model of Huntington's disease. GW5074 could have therapeutic value against neurodegenerative pathologies in humans.
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Synonyms:
GW5074; GW 5074; GW-5074;
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1.GW5074 and PP2 kinase inhibitors implicate nontraditional c-Raf and Lyn function as drivers of retinoic acid-induced maturation.
Jensen HA1, Bunaciu RP2, Varner JD1, Yen A2. Cell Signal. 2015 Aug;27(8):1666-75. doi: 10.1016/j.cellsig.2015.03.014. Epub 2015 Mar 26.
The multivariate nature of cancer necessitates multi-targeted therapy, and kinase inhibitors account for a vast majority of approved cancer therapeutics. While acute promyelocytic leukemia (APL) patients are highly responsive to retinoic acid (RA) therapy, kinase inhibitors have been gaining momentum as co-treatments with RA for non-APL acute myeloid leukemia (AML) differentiation therapies, especially as a means to treat relapsed or refractory AML patients. In this study GW5074 (a c-Raf inhibitor) and PP2 (a Src-family kinase inhibitor) enhanced RA-induced maturation of t(15;17)-negative myeloblastic leukemia cells and rescued response in RA-resistant cells. PD98059 (a MEK inhibitor) and Akti-1/2 (an Akt inhibitor) were less effective, but did tend to promote maturation-uncoupled G1/G0 arrest, while wortmannin (a PI3K inhibitor) did not enhance differentiation surface marker expression or growth arrest. PD98059 and Akti-1/2 did not enhance differentiation markers and have potential, antagonistic off-targets effects on the aryl hydrocarbon receptor (AhR), but neither could the AhR agonist 6-formylindolo(3,2-b)carbazole (FICZ) rescue differentiation events in the RA-resistant cells.
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CAS 220904-83-6 GW5074

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