Ro 5-3335 | RUNX1 transcription factor inhibitor

Ro 5-3335 chemical structure

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Ro 5-3335 (30195-30-3) was identified in a screen for inhibitors of the RUNX1-CBFβ interaction. It represses RUNX1/CBFB-dependent transactivation in reporter assays and runx1-dependent hematopoiesis in zebrafish embryos.1  Ro 5-3335 slows disease progression in various models including acute kidney injury2, acute myocardial infarction3 and  osteoarthritis4 among others5. It synergizes with an HDAC inhibitor enhancing the activation of latent HIV-1 in both cell lines and patient PBMCs.6

References/Citations:

  1. Cunningham et al. (2012), 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 14592
  2. Fontecha-Barriuso et al. (2024), Runt-related transcription factor 1 (RUNX1) is a mediator of acute kidney injury; J. Pathol., 264 396
  3. Chen et al. (2024), Pharmacological inhibition of RUNX1 reduces infarct size after acute myocardial infarction in rats and underlying mechanism revealed by proteomics implicates repressed cathepsin levels; Funct. Integr. Genomics, 24 113
  4. Ye et al. (2023), Kartogenin potentially protects temporomandibular joints from collagenase-induced osteoarthritis via core binding factor β and runt-related transcription factor 1 binding – A rat model study; J. Dent. Sci., 18 1553
  5. Li et al. (2016), Runx1 contributes to neurofibromatosis type 1 neurofibroma formation; Oncogene, 35 1468
  6. Klase et al. (2014), Activation of HIV-1 from latent infection via synergy of RUNX1 inhibitor Ro5-3335 and SAHA; PLoS Pathog., 10 e1003997
30195-30-3, RINX1-CBFß interaction inhibitor, Ro 5-3335, Ro 5-3335 supplier, Ro5-3335

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Ro 5-3335 (30195-30-3) was identified in a screen for inhibitors of the RUNX1-CBFβ interaction. It represses RUNX1/CBFB-dependent transactivation in reporter assays and runx1-dependent hematopoiesis in zebrafish embryos.1  Ro 5-3335 slows disease progression in various models including acute kidney injury2, acute myocardial infarction3 and  osteoarthritis4 among others5. It synergizes with an HDAC inhibitor enhancing the activation of latent HIV-1 in both cell lines and patient PBMCs.6

References/Citations:

  1. Cunningham et al. (2012), 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 14592
  2. Fontecha-Barriuso et al. (2024), Runt-related transcription factor 1 (RUNX1) is a mediator of acute kidney injury; J. Pathol., 264 396
  3. Chen et al. (2024), Pharmacological inhibition of RUNX1 reduces infarct size after acute myocardial infarction in rats and underlying mechanism revealed by proteomics implicates repressed cathepsin levels; Funct. Integr. Genomics, 24 113
  4. Ye et al. (2023), Kartogenin potentially protects temporomandibular joints from collagenase-induced osteoarthritis via core binding factor β and runt-related transcription factor 1 binding – A rat model study; J. Dent. Sci., 18 1553
  5. Li et al. (2016), Runx1 contributes to neurofibromatosis type 1 neurofibroma formation; Oncogene, 35 1468
  6. Klase et al. (2014), Activation of HIV-1 from latent infection via synergy of RUNX1 inhibitor Ro5-3335 and SAHA; PLoS Pathog., 10 e1003997