AC-340
AC-340 is a potent hybrid VDR agonist/HDAC inhibitor. AC-340 superinduces VDR target genes (e.g., CYP24A1) and inhibits HDAC6 (IC50 = 0.37 μM) with ~10-fold selectivity over HDAC2. AC-340 induces VDR hyperagonism by causing widespread protein hyperacetylation (e.g., tubulin and H3K9/K27), which leads to elevated H3K27 acetylation on VDR target genes. AC-340 can be used for melanoma cancer research.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3109965-54-7
- 分子式: C26H40N2O4S
- 分子量:476.67
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
HDAC6 0.37 μM (IC50) |
HDAC2 7.5 μM (IC50) |
体外実験
AC-340 (10 μM, 6 h) induces robust protein hyperacetylation in B16-F10 cells, such as tubulin acetylation (targeted by HDAC6) and acetylation of histone H3 lysines 9 and 27[1].
AC-340 (10 μM, 24 h) upregulates both VDR gene and protein expression in mouse B16-F10 cells, but in human A375 and SK-MEL-28 cells, it enhances VDR protein without affecting its gene expression[1].
AC-340 (2 h) induces VDR recruitment to the Spp1 VDRE to a level similar to Calcitriol (1,25D) (HY-10002), but it uniquely leads to a significant induction of H3K27 acetylation at this locus in B16-F10 cells[1].
AC-340 binds the VDR by forming more extensive interactions with the coactivator binding surface than the natural ligand 1,25D[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:B16-F10 cells
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Concentration:10 μM
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Incubation Time:6 h
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Result:Induced robust protein hyperacetylation in B16-F10 cells.
Significantly increased Ac-Tubulin, AcH3K9 and AcH3K27 levels.
化学情報
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CAS 番号 3109965-54-7
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分子量 476.67
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分子式 C26H40N2O4S
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SMILES
CCC(CC)(C1=CC=C(C=C1)OCCCC(NO)=O)C2=NC(C)=C(S2)CCC(C(C)(C)C)O
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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.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)