2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. 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.

For research use only. We do not sell to patients.

HDAC6-IN-82

HDAC6-IN-82 Chemical Structure

CAS No. : 1228571-33-2

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HDAC6-IN-82 Related Antibodies

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View All HDAC Isoform Specific Products:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

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[1].

IC50 & Target[1]

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)

In Vitro

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.

HDAC6-IN-82 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: AML U937 cells
Concentration: 0.125 and 0.25 μM
Incubation Time: 24 h, 48 h
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.

Western Blot Analysis[1]

Cell Line: AML U937 cells
Concentration: 0.0675, 0.125 and 0.25 μM
Incubation Time: 48 h
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).

Real Time qPCR[1]

Cell Line: AML U937 cells
Concentration: 0.0675, 0.125 and 0.25 μM
Incubation Time: 48 h
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.
Molecular Weight

409.50

Formula

C22H23N3O3S
CAS No.
SMILES

O=C(CCCCCSC1=NC(C2=CC=C(C=C2)C3=CC=CC=C3)=CC(N1)=O)NO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HDAC6-IN-82 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HDAC6-IN-821228571-33-2HDACApoptosisHistone deacetylasesleukemiaHDAC2HDAC3lymphomaglioblastomaHDAC6HDAC10HDAC11HDAC1HDAC8Inhibitorinhibitorinhibit

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