CBFb-Runx1 Inhibitor II, Ro5-3335

CBFβ-Runx1 Inhibitor II, Ro5-3335
[7-chloro-5-(2-pyrryl)-3H-1,4 benzodiazapin-2-(H)-one], Ro53335, CBFα-CBFβ Inhibitor II
A cell-permeable benzodiazepine that suppresses CBFα/Runx1-CBFβ transactivation activity (25 µM; 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 21.7 µM) in vitro and more effectively reduce peripheral blood c-kit+ population (300 mg/kg/d via animal feed) than Cytarabine (Cat. No. 251010) in a murine Cbfb-MYH11 leukemia model in vivo. Comparing to CBFβ-Runx1 Inhibitor I (Cat. No. 219505), Ro5-3335 modulates the Runx1-CBFβ heterodimer formation without completely disrupting the subunits interaction.
产品信息
Form  Off-white solid
Primary Target  RUNX1 and CBF→
Primary Target IC50  0.5&ndash
Molar mass  259.69
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥98% by HPLC
Solubility  DMSO
CAS number  30195-30-3
商店和运输信息
Storage  +2°C to +8°C
Ship  Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling