CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
|Solubility (25°C)||DMSO ≥ 100 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Hsiao-Hui Kuo, et al. Cell Div. Heat shock factor 1 suppression induces spindle abnormalities and sensitizes cells to antimitotic drugs
 Samir Parekh. Clin Cancer Res. Targeting HSF1: A Prime Integrator of Proteotoxic Stress Response in Myeloma
 Jacqueline H L Fok, et al. Clin Cancer Res. HSF1 Is Essential for Myeloma Cell Survival and A Promising Therapeutic Target
 Nicola E A Chessum, et al. J Med Chem. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)
 Matthew D Cheeseman, et al. J Med Chem. Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen
|Related HSP Products|
Arimoclomol (BRX-220 free base) is a heat shock protein (HSP) co-inducer. arimoclomol protects motor neurons by enhancing Hsp expression, thereby directly affecting protein aggregation and removing misfolded and misassembled proteins through the ubiquitin-proteasome system.
DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities.
TAS-116 is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L).
WAY-270444 is a Hsp90 inhibitor/ inhibits histidine kinases C. crescentus CckA
VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM.
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