Inhibitor of valosin-containing protein (VCP or p97)
     
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Inhibitor of valosin-containing protein (VCP or p97)

4-[[4-(3-pyridyl)thiazol-2-yl]amino]phenol 

Potent drug-like inhibitor of valosin-containing protein (VCP; also known as p97) with IC50 values of 0.30 ?M.

nw-ter_atpase_inhibitor2

OTAVAchemicals Catalogue Number:   7211760110

CAS Registry Number: N/A

Purity: 100%

Ref.: M. G. Bursavich et al. 2-Anilino-4-aryl-1,3-thiazole inhibitors of valosin-containing protein (VCP or p97). Bioorg. Med. Chem. Lett. 20 (2010) 16771679.

Abstract: Valosin-containing protein (VCP; also known as p97) is amember of the AAA ATPase family with a central role in the ubiquitin-degradation of misfolded proteins. VCP also exhibits antiapoptotic function and metastasis via activation of nuclear factor kappa-B signaling pathway. We have discovered that 2-anilino-4-aryl-1,3-thiazoles are potent drug-like inhibitors of this enzyme. The identi?ed compounds show low nanomolar VCP potency, demonstrate SAR trends, and show activity in a mechanism based cellular assay. This series of compounds represents the ?rst steps towards a novel, small molecule VCP inhibitor as a cancer therapeutic.


 
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