1256094-72-0

1256094-72-0 structure

Name: AI-10-49
Chemical Name: 2,2'-[Oxybis(2,1-ethanediyloxy-5,2-pyridinediyl)]bis[6-(trifluoromethoxy)-1H-benzimidazole]
CAS Number: 1256094-72-0
Molecular Formula: C₃₀H₂₂F₆N₆O₅
Molecular Weight: 660.523
Catalog: Research Areas Cancer
Create Date: 2018-11-30 15:53:33
Modify Date: 2024-01-11 10:43:31
AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.IC50 value: 0.26 uM [1]Target: CBFβ-SMMHC/RUNX1 interaction inhibitorAI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics,and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death. These data suggest that direct inhibition of the oncogenic CBFβ-SMMHC fusion protein may be an effective therapeutic approach for inv(16) AML, and they provide support for transcription factor targeted therapy in other cancers.

Name	2,2'-[Oxybis(2,1-ethanediyloxy-5,2-pyridinediyl)]bis[6-(trifluoromethoxy)-1H-benzimidazole]
Synonyms	AI-10-49 1H-Benzimidazole, 2,2'-[oxybis(2,1-ethanediyloxy-5,2-pyridinediyl)]bis[5-(trifluoromethoxy)- 2,2'-[Oxybis(2,1-ethanediyloxy-5,2-pyridinediyl)]bis[5-(trifluoromethoxy)-1H-benzimidazole]

Description	AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.IC50 value: 0.26 uM [1]Target: CBFβ-SMMHC/RUNX1 interaction inhibitorAI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics,and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death. These data suggest that direct inhibition of the oncogenic CBFβ-SMMHC fusion protein may be an effective therapeutic approach for inv(16) AML, and they provide support for transcription factor targeted therapy in other cancers.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cancer
References	[1]. Illendula A, et al. Chemical biology. A small-molecule inhibitor of the aberrant transcription factor CBFβ-SMMHC delays leukemia in mice. Science. 2015 Feb 13;347(6223):779-84.