2978620-84-5
Chemical Structure
PROTAC EZH2 Degrader-9
- CAS No.: 2978620-84-5
- Formula:C51H59N7O7
- Molecular Weight:882.06
InChIKey: MELSPRKWGAVFDD-UHFFFAOYSA-N
SMILES: O=C1CCC(C(N1)=O)N2C(C3=C(C2=O)C=C(N4CC5(CCN(CC6=CC=CC(C7=CC(C(NCC8=C(C=C(NC8=O)C)C)=O)=C(C)C(N(C9CCOCC9)CC)=C7)=C6)CC5)CC4)C=C3)=O
Biological Activity: PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research[1].
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PROTAC EZH2 Degrader-9 | PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research. | |||||||||||||||||||||
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