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.
For research use only. We do not sell to patients.
- CAS No.: 2407654-72-0
- Formula: C30H30N8O3
- Molecular Weight:550.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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KAT2A 89 nM (DC50) |
KAT2A degrader-1 enhances CRBN-KAT2A dimerization and eliminates CRBN-GSPT1 dimerization in a cell-free TR-FRET assay[1].
KAT2A degrader-1 (1 nM-100 μM; 6 h) induces degradation of endogenous KAT2A in Kelly cells with a DC50 of 89 nM and 71% maximum degradation after 6 hours of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2407654-72-0
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Molecular Weight 550.61
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Formula C30H30N8O3
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KAT2A degrader-1 Related Classifications
HY-187168 Related Classifications
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