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Art. -Nr.: HY-187168

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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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CAS. Nr.: 2407654-72-0
Formel: C₃₀H₃₀N₈O₃
Molecular Weight:550.61

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

KAT2A degrader-1 Chemical Structure

CAS. Nr.: 2407654-72-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

KAT2A

89 nM (DC₅₀)

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In Vitro

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

CAS. Nr. 2407654-72-0
Molecular Weight 550.61
Formel C₃₀H₃₀N₈O₃
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Ojeda S, et al. Degron-independent recruitment of KAT2A expands the target space of CRBN molecular glues. Science (New York, N.Y.). 2026 Jul 09;393(6807):188-194. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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KAT2A degrader-1

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