Ro 5-3335

Cat. No. 4694

Ro 5-3335 C13H10ClN3O [30195-30-3]

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Alternative Name: CBFβ-Runx1 inhibitor II

Chemical Name: 7-Chloro-1,3-dihydro-5-(1H-pyrrol-2-yl)-2H-1,4-benzodiazepin-2-one

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
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
30195-30-3

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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-CBFß interaction. Proc.Natl.Acad.Sci.USA 109 14592. PMID: 22912405.

Okuda et al (2001) RUNX1/AML1: a central player in hematopoiesis. Int. J. Hematol. 74 252. PMID: 11721959.

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.

If you know of a relevant reference for Ro 5-3335 please let us know.

Citations are publications that use Tocris products. Selected citations for Ro 5-3335 include:

Luo et al (2016) Runt-related Transcription Factor 1 (RUNX1) Binds to p50 in Macrophages and Enhances TLR4-triggeredInflammation and Septic Shock. Journal of Biological Chemistry. PMID: 27573239.

Do you know of a great paper that uses Ro 5-3335 from Tocris? If so please let us know.

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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, Tocris Bioscience, Other Transcription Factor products

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