85-2072-01　CBF beta-Runx1 Inhibitor II, Ro5-3335 ([7-chloro-5-(2-pyrryl)-3H-1,4 benzodiazapin-2-(H)-one], Ro53335, CBFalpha-CBFbeta Inhibitor II) 10mg　CAS No:30195-30-3　217258

特徴

• A cell-permeable benzodiazepine that suppresses CBFalpha/Runx1-CBFbeta transactivation activity (25uM; 293-0 cells) via direct bindings to both subunits of the heterodimeric transcription factor complex. Shown to inhibit oncogenic fusion CBFB-MYH11-, TEL-RUNX1-, and RUNX1-ETO-, dependent leukemia cells proliferation (IC50 = 1.1 to 21.7uM) in vitro and more effectively reduce peripheral blood c-kit+ population (300mg/kg/d via animal feed) than Cytarabine in a murine Cbfb-MYH11 leukemia model in vivo. Comparing to CBFbeta-Runx1 Inhibitor I, Ro5-3335 modulates the Runx1-CBFbeta heterodimer formation without completely disrupting the subunits interaction.
• Solubility:DMSO
• Primary Target:RUNX1 and CBF→
• Primary Target IC50:0.5uM
• Molar Mass:259.69
• Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.