Molibresib

• Product Name Alternative:

  I-BET762; GSK525762; GSK525762A

• UNSPSC Description:

  Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.

• Target Antigen:

  Epigenetic Reader Domain

• Type:

  Reference compound

• Related Pathways:

  Epigenetics

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/GSK-525762A.html

• Purity:

  99.94

• Solubility:

  DMSO : 200 mg/mL (ultrasonic)

• Smiles:

  ClC1=CC=C(C2=N[C@@H](CC(NCC)=O)C3=NN=C(C)N3C4=CC=C(OC)C=C24)C=C1

• Molecular Weight:

  423.90

• References & Citations:

  [1]Nicodeme E, et al. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23.|[2]Asangani IA, et al. Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature. 2014 Jun 12;510(7504):278-82.|[3]Chaidos A, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Phase 2

• CAS Number:

  1260907-17-2