3057216-63-1
Chemical Structure
TDI-11055
- CAS No.: 3057216-63-1
- Formula:C22H24N6O
- Molecular Weight:388.47
InChIKey: QRYISIPABXJVOQ-AWEZNQCLSA-N
SMILES: C[C@H]1CCCN1CC2=CC3=C(N2)C=C(N=C3)NC(C4=CC=C5C(C=NN5C)=C4)=O
Biological Activity: TDI-11055 is a selective and orally active eleven-nineteen leukemia (ENL) inhibitor, which displaces ENL from chromatin by blocking its YEATS domain interaction with acylated histones. TDI-11055 inhibits ENL and AF9 YEATS domains with IC50 values of 50 nM and 70 nM, respectively, and no activity against GAS41 or YEATS2. TDI-11055 decreases chromatin occupancy of ENL-associated complexes, impairs transcription elongation, suppresses key oncogenic gene expression programs, and induces differentiation. TDI-11055 can be used for the research of acute myeloid leukemia[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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TDI-11055 | 99.87% | TDI-11055 is a selective and orally active eleven-nineteen leukemia (ENL) inhibitor, which displaces ENL from chromatin by blocking its YEATS domain interaction with acylated histones. TDI-11055 inhibits ENL and AF9 YEATS domains with IC50 values of 50 nM and 70 nM, respectively, and no activity against GAS41 or YEATS2. TDI-11055 decreases chromatin occupancy of ENL-associated complexes, impairs transcription elongation, suppresses key oncogenic gene expression programs, and induces differentiation. TDI-11055 can be used for the research of acute myeloid leukemia. | ||||||||||||||||||||
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References
- [1]. Liu Y, et al. Small-Molecule Inhibition of the Acyl-Lysine Reader ENL as a Strategy against Acute Myeloid Leukemia. Cancer Discov. 2022;12(11):2684-2709. [Content Brief]
- [2]. Michino M, et al. Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055. ACS Med Chem Lett. 2024;15(4):524-532. Published 2024 Mar 12. [Content Brief]
