2407654-72-0
Chemical Structure
KAT2A degrader-1
- CAS No.: 2407654-72-0
- Formula:C30H30N8O3
- Molecular Weight:550.61
InChIKey: GVUHLKICOYDINP-UHFFFAOYSA-N
SMILES: O=C(N1)CCC(N2CC(C(NC3=C(N=CN4C(C)C)C4=NC(NC5=CC(CCC6)=C6C=C5)=N3)=CC=C7)=C7C2=O)C1=O
Biological Activity: KAT2A degrader-1 is a molecular glue degrader targeting KAT2A, with a DC50 of 89 nM in Kelly cells. KAT2A degrader-1 recruits KAT2A to cereblon (CRBN) in a degron-independent manner, forms a ternary complex with KAT2A and CRBN, and drives the polyubiquitination and proteasome-dependent degradation of KAT2A. KAT2A degrader-1 reduces the level of histone H3 lysine 9 acetylation (H3K9Ac). KAT2A degrader-1 induces antiproliferative effects in acute myeloid leukemia cells, while enhancing KAT2A-CRBN dimerization activity and eliminating the targeting effect on GSPT1. KAT2A degrader-1 can be used for research related to acute myeloid leukemia[1].
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KAT2A degrader-1 | KAT2A degrader-1 is a molecular glue degrader targeting KAT2A, with a DC50 of 89 nM in Kelly cells. KAT2A degrader-1 recruits KAT2A to cereblon (CRBN) in a degron-independent manner, forms a ternary complex with KAT2A and CRBN, and drives the polyubiquitination and proteasome-dependent degradation of KAT2A. KAT2A degrader-1 reduces the level of histone H3 lysine 9 acetylation (H3K9Ac). KAT2A degrader-1 induces antiproliferative effects in acute myeloid leukemia cells, while enhancing KAT2A-CRBN dimerization activity and eliminating the targeting effect on GSPT1. KAT2A degrader-1 can be used for research related to acute myeloid leukemia. | |||||||||||||||||||||
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Keywords
