A benzodiazepine that modulates the RUNX1-CBFβ protein-protein interaction
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Product Type

Ro 5-3335

Item No. 45709

Technical Information
Formal Name
7-chloro-1,3-dihydro-5-(1H-pyrrol-2yl)-2H-1,4-benzodiazepin-2-one
CAS Number
30195-30-3
Synonyms
  • NSC 66020
Molecular Formula
C13H10ClN3O
Formula Weight
Purity
≥98%
A solid
SMILES
O=C1NC2=C(C(C3=CC=CN3)=NC1)C=C(Cl)C=C2
InChi Code
InChI=1S/C13H10ClN3O/c14-8-3-4-10-9(6-8)13(11-2-1-5-15-11)16-7-12(18)17-10/h1-6,15H,7H2,(H,17,18)
InChi Key
XWNMORIHKRROGW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Ro 5-3335 is a benzodiazepine that modulates the protein-protein interaction between RUNX family transcription factor 1 (RUNX1) and core-binding factor subunit β (CBFβ).1 It inhibits transactivation of the CSF-1 receptor (CSF-1R) promoter, a target of RUNX1 and CBFβ, in a reporter assay. Ro 5-3335 reduces viability of leukemia cells harboring CBF or RUNX1 fusion proteins (IC50s = 1.1-21.7 µM) to a greater extent than non-CBF leukemia cells (IC50s = 54.6->200 µM). It also inhibits RUNX1/CBFβ-dependent hematopoiesis in zebrafish embryos.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cunningham, L., Finckbeiner, S., Hyde, R.K., 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. USA 109(36), 14592-14597 (2012).