CCT251236
HSF stress pathway inhibitor / Inhibitor of the Heat Shock Transcription Factor 1 (HSF1) stress pathway (IC50 = 19 nM Inhibition HSF-1 mediated HSP72 induction, IC50 = 40 nM HSPA1A induction).1 It displayed efficacy in a human ovarian carcinoma xenograft mouse model (SK-OV 3 cells) and inhibited migration of WM266.4 melanoma cells @ 100 nM. CCT251236 showed high affinity for the protein pirin (Ki = 28 nM), but this target was not shown conclusively to be the cause of the anticancer activity. It also showed efficacy in vitro against primary patient-derived myeloma cells and H929 human myeloma xenograft models.2
Biochemicals & reagents
1693731-40-6
Cheeseman et al. (2017), Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen; J. Med. Chem., 60 180 Fok et al. (2018), HSF-1: Essential for Myeloma Cell Survival and A Promising Therapeutic Target; Cancer Res., 124 2395
-20°C
TARGET: Transcription factor; HSP (Heat shock protein) -- PATHWAY: Transcription -- RESEARCH AREA: Cellular stress -- DISEASE AREA: Cancer