UNC6535
UNC6535 is a covalent ligand targeting the SETDB1 triple Tudor domain (3TD) with negative allosteric modulator properties, with an IC50 of 3.4 μM and a Kd of 4.2 μM. UNC6535 inhibits the methyltransferase activity of recombinant SETDB1 protein lacking the 3TD domain. UNC6535 reversibly binds to the aromatic cages of both TD2 and TD3 subdomains of SETDB1 3TD simultaneously, displacing the endogenous H3K9Me2K14Ac histone tail ligand. UNC6535 can be used in research on cancer and neurodegenerative diseases.
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- Fòrmula: C25H44N6O2
- Peso molecular:460.66
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
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Actividad biológica
UNC6535 weakly inhibits the methyltransferase activity of full-length SETDB1 in in vitro radiometric assays, with an IC50 of 84 μM, and inhibits the methyltransferase activity of a SETDB1 truncation lacking the 3TD domain, with an IC50 of 30 μM[1].
UNC6535 displaces the H3 peptide from the 3TD-truncated SETDB1 with an IC50 value of 8.6 μM in FP assays[1].
UNC6535 binds to the SETDB1 tripartite Tudor domain with a Kd value of 4.2 μM, and occupies the aromatic cages of TD2 and TD3 simultaneously[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Peso molecular 460.66
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Fòrmula C25H44N6O2
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SMILES
COC1=CC2=C(C(NCCCCCCN(C)C)=NC(NCCCCCN(C)C)=N2)C=C1OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Ficha de datos (264 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Uguen M, et al. Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells. Nat Commun. 2025;16(1):1905. Published 2025 Feb 24. [Content Brief]
[2]. Uguen M, et al. Tudor-Containing Methyl-Lysine and Methyl-Arginine Reader Proteins: Disease Implications and Chemical Tool Development. ACS Chem Biol. 2025;20(1):33-47. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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