纯度:98% by HPLC;NMR (Conforms)
分子式:C32H32N4O5
分子量:552.63
溶剂:DMSO (5 mg/ml)
性状:Off-white/beige solid
存储:-20°C
Activity (short version):HSF stress pathway inhibitor
Function / Pharmacology: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