HDAC6-IN-82
HDAC6-IN-82 is a selective HDAC6 inhibitor with an IC50 of 4.9 nM against HDAC6. HDAC6-IN-82 inhibits HDAC1 (112 nM), HDAC2 (737 nM), HDAC3 (623 nM), HDAC8 (1140 nM), HDAC10 (91.4 nM) and HDAC11 (219 nM). HDAC6-IN-82 reduces cancer cell viability, induces cell cycle arrest, triggers apoptosis, and increases the acetylation levels of H3K9 and α-tubulin. HDAC6-IN-82 can be used in cancer-related research such as leukemia.
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- CAS No.: 1228571-33-2
- Formule: C22H23N3O3S
- Masse moléculaire:409.50
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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 4.9 nM (IC50) |
HDAC1 112 nM (IC50) |
HDAC2 737 nM (IC50) |
HDAC3 623 nM (IC50) |
HDAC4 71300 nM (IC50) |
HDAC5 14900 nM (IC50) |
HDAC7 NI nM (IC50) |
HDAC8 1140 nM (IC50) |
HDAC9 NI nM (IC50) |
HDAC10 33.1 nM (IC50) |
HDAC11 219 nM (IC50) |
HDAC6-IN-82 (Compound 14b) (48 h) reduces cell viability in a panel of human solid tumor and hematologic cancer cell lines, with the strongest potency against HL60 and U937 leukemia cells (CC50 = 1.2 μM and 1.3 μM)[1].
HDAC6-IN-82 (0.125-0.25 μM; 24-48 h) induces apoptosis in U937 acute myeloid leukemia cells in a time- and dose-dependent manner[1].
HDAC6-IN-82 (0.0675-0.25 μM; 48 h) inhibits nuclear and cytoplasmic HDAC activity in U937 acute myeloid leukemia cells[1].
Treatment of U937 acute myeloid leukemia cells with HDAC6-IN-82 (0.0675-0.25 μM; 48 h) modulates the mRNA expression of cell cycle and apoptosis regulators, upregulating p21, Bak and Bax while downregulating cyclin D1 and Bcl-2[1].
HDAC6-IN-82 (0.0675-0.25 μM; 48 h) regulates miRNA expression in U937 acute myeloid leukemia cells after 48 h of treatment, downregulating anti-apoptotic miRNAs involved in apoptosis regulation and upregulating pro-apoptotic miRNAs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AML U937 cells
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Concentration:0.125 and 0.25 μM
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Incubation Time:24 h, 48 h
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Result:Induced a time- and dose-dependent accumulation of cells in the sub-G1 phase: at 24 h, 0.125 μM caused ~30% sub-G1 cells and 0.25 μM caused ~40% sub-G1 cells; at 48 h, 0.125 μM caused ~45% sub-G1 cells and 0.25 μM caused ~70% sub-G1 cells.
Triggered a time- and dose-dependent increase in Annexin V-positive cells: at 24 h, 0.125 μM caused ~40% Annexin V-positive cells and 0.25 μM caused ~50% Annexin V-positive cells; at 48 h, 0.125 μM caused ~80% Annexin V-positive cells and 0.25 μM caused ~90% Annexin V-positive cells.
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Cell Line:AML U937 cells
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Concentration:0.0675, 0.125 and 0.25 μM
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Incubation Time:48 h
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Result:Induced hyperacetylation of histone H3K9 (fold changes relative to DMSO: 3.47 at 0.0675 μM, 5.23 at 0.125 μM, 3.51 at 0.25 μM) and α-tubulin (fold changes relative to DMSO: 3.5 at 0.0675 μM, 4.4 at 0.125 μM, 4.3 at 0.25 μM).
Upregulated the cyclin-dependent kinase inhibitor p21 (fold changes relative to DMSO: 11.1 at 0.0675 μM, 9.9 at 0.125 μM, 6.5 at 0.25 μM).
Downregulated cyclin D1 (fold changes relative to DMSO: 0.42 at 0.0675 μM, 0.53 at 0.125 μM, 0.37 at 0.25 μM).
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Cell Line:AML U937 cells
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Concentration:0.0675, 0.125 and 0.25 μM
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Incubation Time:48 h
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Result:Significantly upregulated mRNA levels of p21, pro-apoptotic Bak, and pro-apoptotic Bax across all tested concentrations.
Significantly downregulated mRNA levels of cyclin D1 and anti-apoptotic Bcl-2 across all tested concentrations.
SAHA showed no significant effect on Bak, Bax, or Bcl-2 mRNA levels.\nSignificantly downregulated anti-apoptotic miRNAs miR-17-5p, miR-18-5p, miR-20a-5p, miR-21-5p, and miR-22-3p across all tested concentrations, with effects stronger than SAHA for miR-18-5p and miR-22-3p.
Significantly upregulated pro-apoptotic miRNAs miR-122-5p, miR-769-5p, miR-181a-5p, and miR-181b-5p across all tested concentrations.
SAHA showed no significant effect on miR-122-5p or miR-181b-5p.
Chemical Information
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CAS No. 1228571-33-2
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Masse moléculaire 409.50
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Formule C22H23N3O3S
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SMILES
O=C(CCCCCSC1=NC(C2=CC=C(C=C2)C3=CC=CC=C3)=CC(N1)=O)NO
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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)
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