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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- CAS No.: 3109965-54-7
- Formule: C26H40N2O4S
- Masse moléculaire:476.67
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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HDAC6 0.37 μM (IC50) |
HDAC2 7.5 μM (IC50) |
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.
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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.
Chemical Information
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CAS No. 3109965-54-7
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Masse moléculaire 476.67
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AC-340 Related Classifications
HY-178336 Related Classifications
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