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Biological Activity
Core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). Represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Reduces leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. Also a Tat antagonist; inhibits HIV-1 replication in vitro.
Technical Data
| M. Wt | 259.63 |
| Formula | C13H10ClN3O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 30195-30-3 |
| PubChem ID | 64983 |
| InChI Key | XWNMORIHKRROGW-UHFFFAOYSA-N |
| Smiles | O=C1CN=C(C3=CC=CN3)C2=C(C=CC(Cl)=C2)N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.96 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 259.63. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.85 mL | 19.26 mL | 38.52 mL |
| 5 mM | 0.77 mL | 3.85 mL | 7.7 mL |
| 10 mM | 0.39 mL | 1.93 mL | 3.85 mL |
| 50 mM | 0.08 mL | 0.39 mL | 0.77 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Cunningham et al (2012) Identification of benzodiazepine Ro5-3335 as an inhibitor of CBF leukemia through quantitative high throughput screen against RUNX1-CBF beta interaction. Proc.Natl.Acad.Sci.USA 109 14592 PMID: 22912405
Cupelli et al (1995) The human immunodeficiency virus type 1 Tat antagonist, Ro 5-3335, predominantly inhibits transcription initiation from the viral promoter. J.Virol. 69 2640 PMID: 7884917
Okuda et al (2001) RUNX1/AML1: a central player in hematopoiesis. Int. J. Hematol. 74 252 PMID: 11721959
Keywords: Ro 5-3335, supplier, Ro5-3335, CBF, core, binding, factor, Leukemia, inhibitors, inhibits, runt-related, transcription, factor, 1, RUNX1, acute, myeloid, leukemia, protein, AML1, CBFβ, CBFα, hematopoiesis, HIV-1, replication, antiviral, CBFβ-Runx1, II, CBFbeta-Runx1, inhibitor, II, Antivirals, Other, Transcription, Factors, Other, Transcription, Factors, Tocris Bioscience
