2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. HDAC6-IN-75

HDAC6-IN-75 is a selective HDAC6 inhibitor with an IC50 of 0.17 nM against HDAC6. HDAC6-IN-75 induces the accumulation of acetylated α-tubulin in glioma cells. HDAC6-IN-75 triggers cell cycle changes, increases the SubG1 cell population, and promotes apoptosis in glioma cells and glioblastoma stem cells. HDAC6-IN-75 is applicable for glioma-related research.

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HDAC6-IN-75

HDAC6-IN-75 Chemical Structure

CAS No. : 400078-78-6

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HDAC6-IN-75 Related Antibodies

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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-75 is a selective HDAC6 inhibitor with an IC50 of 0.17 nM against HDAC6. HDAC6-IN-75 induces the accumulation of acetylated α-tubulin in glioma cells. HDAC6-IN-75 triggers cell cycle changes, increases the SubG1 cell population, and promotes apoptosis in glioma cells and glioblastoma stem cells. HDAC6-IN-75 is applicable for glioma-related research[1].

IC50 & Target[1]

HDAC6

0.17 nM ()

In Vitro

HDAC6-IN-75 (compound 3a) (0.0032-50 μM; 24-72 h) exhibits time-dependent cytotoxicity in glioma cell lines, with GI50 values ranging from 0.8 μM to 5.3 μM after 72 h of incubation, and induces total growth inhibition in HOG, T98G, and U251MG cells at 72 h[1].
HDAC6-IN-75 (compound 3a) (34.0 μM HOG, 16.2 μM T98G, 50 μM U87MG, 28.9 μM U251MG; 24 h) increases acetyl-α-tubulin levels in all four tested glioma cell lines and acetyl-histone H3 levels in HOG, T98G, and U251MG cells after 24 h of treatment, consistent with its HDAC6 inhibitory activity and concurrent class I HDAC inhibition at cellular concentrations[1].
HDAC6-IN-75 (compound 3a) (34.0 μM HOG, 16.2 μM T98G, 50 μM U87MG, 28.9 μM U251MG; 24 h) induces DNA fragmentation (SubG1 accumulation) in T98G and U251MG cells, and modulates cell cycle progression by shifting populations from G0/G1 to G2/M in U87MG, U251MG, and HOG cells after 24 h of treatment[1].
HDAC6-IN-75 (compound 3a) (34.0 μM HOG, 16.2 μM T98G, 50 μM U87MG, 28.9 μM U251MG; 24 h) reduces viability and induces late apoptosis and necrosis in HOG and U251MG glioma cells after 24 h of treatment[1].
HDAC6-IN-75 (compound 3a) (0.0032-50 μM; 72 h) exhibits cytotoxicity against glioblastoma stem cells, with an IC50 of 3.725 μM in proneural GSC23 cells and 12.90 μM in mesenchymal GG16 cells after 72 h of treatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HDAC6-IN-75 Related Antibodies

Western Blot Analysis[1]

Cell Line: Glioma cell lines HOG, T98G, U87MG, U251MG
Concentration: 34.0 μM (HOG); 16.2 μM (T98G); 50 μM (U87MG); 28.9 μM (U251MG)
Incubation Time: 24 h
Result: Significantly promoted accumulation of acetyl-α-tubulin in HOG, T98G, U87MG, and U251MG cells.
Significantly promoted accumulation of acetyl-histone H3 in HOG, T98G, and U251MG cells, with activity comparable to vorinostat in these cell lines.

Cell Cycle Analysis[1]

Cell Line: Glioma cell lines HOG, T98G, U87MG, U251MG
Concentration: 34.0 μM (HOG); 16.2 μM (T98G); 50 μM (U87MG); 28.9 μM (U251MG)
Incubation Time: 24 h
Result: Increased the percentage of cells in the SubG1 phase in T98G and U251MG cells.
Decreased the percentage of cells in the G0/G1 phase and increased the percentage in the G2/M phase in U87MG and U251MG cells.
Decreased the percentage of cells in the G0/G1 phase in HOG cells.

Apoptosis Analysis[1]

Cell Line: Glioma cell lines HOG, T98G, U87MG, U251MG
Concentration: 34.0 μM (HOG); 16.2 μM (T98G); 50 μM (U87MG); 28.9 μM (U251MG)
Incubation Time: 24 h
Result: Decreased cell viability in all four glioma cell lines.
Increased the percentage of late apoptotic and necrotic cells in HOG and U251MG cells.
Molecular Weight

292.31

Formula

C13H12N2O4S
CAS No.
SMILES

O=C(NO)C1=CC=C(NS(=O)(C2=CC=CC=C2)=O)C=C1
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Purity & Documentation
References
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HDAC6-IN-75 Related Classifications

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  • 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-75400078-78-6HDACApoptosisHistone deacetylasesclass I HDACsHDAC6gliomaglioma cellsapoptosisglioblastomaglioblastoma stem cellsHDAC10acetylated α-tubulincell cycleInhibitorinhibitorinhibit

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