| Bioactivity | Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation[1]. | ||||||||||||
| Target | RUNX1-CBFβ interaction | ||||||||||||
| Invitro | Ro5-3335 has antiproliferative activity against human CBF leukemia cell lines, with IC50s of 1.1 μM, 21.7 μM and 17.3 μM for ME-1, Kasumi-1 and REH, respectively[1]. Ro5-3335 inhibits definitive hematopoiesis in zebrafish embryos[1].Ro5-3335 does not completely break apart RUNX1-CBFβ interaction, but changes the conformation of their complex or increases the distance between RUNX1 and CBFβ in the complex[1]. | ||||||||||||
| In Vivo | Ro5-3335 is identified as an inhibitor of RUNX1–CBFβ function in zebrafish models[1].Ro5-3335 rescues preleukemic phenotype in a RUNX1-ETO transgenic zebrafish[1].Ro5-3335 (300 mg/kg/d; p.o; for 30 days) reduces leukemia burden in a mouse CBFB-MYH11 leukemia model[1]. Animal Model: | ||||||||||||
| Name | Ro5-3335 | ||||||||||||
| CAS | 30195-30-3 | ||||||||||||
| Formula | C13H10ClN3O | ||||||||||||
| Molar Mass | 259.69 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Cunningham L, et al. Identification of benzodiazepine Ro5-3335 as an inhibitor of CBF leukemia through quantitative high throughput screen against RUNX1-CBFβ interaction. Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14592-7. |