1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. HDAC6-IN-83

HDAC6-IN-83 is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 value of 11.49 nM. HDAC6-IN-83 selectively increases the acetylation level of α-tubulin without affecting histone H3. HDAC6-IN-83 induces cell apoptosis, induces cell cycle arrest, inhibits cancer cell proliferation, suppresses cancer cell invasion and inhibits angiogenesis. HDAC6-IN-83 can be used in non-small cell lung cancer research.

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HDAC6-IN-83

HDAC6-IN-83 Chemical Structure

CAS No. : 3053098-60-2

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Description

HDAC6-IN-83 is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 value of 11.49 nM. HDAC6-IN-83 selectively increases the acetylation level of α-tubulin without affecting histone H3. HDAC6-IN-83 induces cell apoptosis, induces cell cycle arrest, inhibits cancer cell proliferation, suppresses cancer cell invasion and inhibits angiogenesis. HDAC6-IN-83 can be used in non-small cell lung cancer research[1].

IC50 & Target[1]

HDAC6

11.49 nM (IC50)

In Vitro

HDAC6-IN-83 (Compound P21) (0.27-5.92 μM; 48 h) exhibits broad-spectrum antiproliferative activity against various cancer cell lines, with IC50 values ranging from 0.27 μM to 5.92 μM, and shows favorable safety profiles in normal HEK293 cells[1].
HDAC6-IN-83 (0.01-0.2 μM; 12 h) selectively increases the acetylation level of α-tubulin in RPMI 8226 cells after 12 h of treatment, without affecting the acetylation of histone H3[1].
HDAC6-IN-83 (0.1-10 μM; 24-48 h) dose-dependently inhibits the invasive ability of A549 cells, with significant inhibition observed at concentrations as low as 1 μM[1].
HDAC6-IN-83 (0.01-1.25 μM; 24 h) dose-dependently induces apoptosis in Jurkat cells[1].
HDAC6-IN-83 (0.05-0.25 μM; 24 h) induces G2/M cell cycle arrest in Jurkat cells following treatment with 0.25 μM for 24 h[1].
HDAC6-IN-83 (0.1-10 μM; 6 h) dose-dependently inhibits angiogenesis in human umbilical vein endothelial cells (HUVEC)[1].

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

Apoptosis Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.01, 0.05, 0.25, 1.25 μM
Incubation Time: 24 h
Result: Induced apoptosis in Jurkat cells in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.05, 0.25 μM
Incubation Time: 24 h
Result: Induced cycle arrest in Jurkat cells.
In Vivo

HDAC6-IN-83 (Compound P21) (25-50 mg/kg; i.p.; once every two days; 14 days) exhibits dose-dependent in vivo antiproliferative efficacy in A549 PDX models[1].

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

Animal Model: BALB/c-nu (male, 4-6 weeks old)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: i.p.; once every two days; 14 days
Result: Significantly inhibited tumor volume compared to the control group.
Halted tumor growth at 50 mg/kg.
Showed no significant morphological abnormalities in kidney, heart, liver, or lung tissues from the 50 mg/kg treatment group compared to the control group.
Molecular Weight

413.47

Formula

C25H23N3O3

CAS No.
SMILES

COC(C=C1)=CC=C1CN(CC2=CC=C(C(NO)=O)C=C2)C3=C(N=CC=C4)C4=CC=C3

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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References
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HDAC6-IN-83
Cat. No.:
HY-184304
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