CCT251236 : pirin ligand of PIR
Protein target names: PIR
Mechanism of action: pirin ligand
In Vitro Validations
DOI Reference: 10.1021/acs.jmedchem.6b01055
In Cell Validations
In Vivo Data
SERP ratings and comments
This is a useful probe for Pirin - useful to study Pirin function both in cells and in vivo. There is a correlation of molecule binding to Pirin and cellular activity. Active and inactive versions of the molecule have been reported, and the inactive version should be used as a control.
(last updated: 26 Mar 2017 )
CCT251236 has been thoroughly investigated and characterized as a cellular probe for Pirin (target) and HSF (pathway) and is supported by a robust and transparent set of data. My only concern is for possible in vivo use where there is an apparent non-linear pharcacokinetic response in mouse (20 mg/kg, oral dose gave a 3-fold lower AUC than a 5 mg/kg dose, albeit in a different mouse strain). I suggest users run a pilot PK study in their strain of interest to ensure the required exposures can be achieved with their dose.
(last updated: 12 Jun 2017 )
While CCT251236 clearly shows potent binding (SPR) to human pirin, displays potent inhibition of Hsp72 induction in a cell-based assay (ELISA), and shows activity in an SK-OV-3 mouse xenograft study, this chemical probe may well be active against other targets, since the anti-proliferative activity against a panel of cancer cell lines is often more potent than the potency measured by the assays outlined above. The enduser should thus use caution when interpreting cell-based or in vivo results obtained using CCT251236.
(last updated: 12 Mar 2021 )