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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- 分子式: C25H44N6O2
- 分子量:460.66
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
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.
化学情報
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分子量 460.66
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分子式 C25H44N6O2
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SMILES
COC1=CC2=C(C(NCCCCCCN(C)C)=NC(NCCCCCN(C)C)=N2)C=C1OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
UNC6535 関連分類
HY-168992 関連分類
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