Inhibitor of valosin-containing protein (VCP or p97)
Potent drug-like inhibitor of valosin-containing protein (VCP; also known as p97) with IC50 values of 0.30 μM.
OTAVAchemicals Catalogue Number: 7211760110
CAS Registry Number: N/A
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) 1677–1679.
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 identiﬁed compounds show low nanomolar VCP potency, demonstrate SAR trends, and show activity in a mechanism based cellular assay. This series of compounds represents the ﬁrst steps towards a novel, small molecule VCP inhibitor as a cancer therapeutic.