1. Cell Cycle/DNA Damage Epigenetics Autophagy Apoptosis
  2. HDAC Autophagy Apoptosis
  3. HDAC6-IN-76

HDAC6-IN-76 (Compound G25) is a selective HDAC6 inhibitor with an IC50 of 12 nM. HDAC6-IN-76 induces Autophagy in a p53-dependent manner. HDAC6-IN-76 induces Apoptosis in a p53-dependent manner. HDAC6-IN-76 exhibits anticancer activity against hematologic malignancies, including acute myeloid leukemia.

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HDAC6-IN-76

HDAC6-IN-76 Chemical Structure

CAS No. : 3110559-06-0

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Description

HDAC6-IN-76 (Compound G25) is a selective HDAC6 inhibitor with an IC50 of 12 nM. HDAC6-IN-76 induces Autophagy in a p53-dependent manner. HDAC6-IN-76 induces Apoptosis in a p53-dependent manner. HDAC6-IN-76 exhibits anticancer activity against hematologic malignancies, including acute myeloid leukemia[1].

IC50 & Target[1]

HDAC6

12 nM (IC50)

In Vitro

HDAC6-IN-76 is a potent and selective HDAC6 inhibitor with an IC50 of 12 nM[1].
HDAC6-IN-76 exhibits broad-spectrum and potent antiproliferative activity against both leukemia and solid tumor cell lines, with particularly prominent activity against MV4-11 cells, with an IC50 of 0.028 μM[1].
HDAC6-IN-76 (0.1-1 μM; 24 h) effectively inhibits the migration of HCT116 colon cancer cells in a dose-dependent manner[1].
HDAC6-IN-76 (0.1-1 μM; 24 h) induces autophagy in a concentration-dependent manner in MV4-11 and HL60 leukemia cells[1].

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

Western Blot Analysis[1]

Cell Line: MV4-11 and HL60 leukemia cells
Concentration: 0.1-1 μM
Incubation Time: 24 h
Result: Led to a concentration-dependent increase in LC3B-II expression (conversion of LC3B-I to LC3B-II) in both MV4-11 and HL60 cells.
Caused a concentration-dependent decrease in p62 expression in both MV4-11 and HL60 cells, indicating enhanced autophagic flux.

Cell Cycle Analysis[1]

Cell Line: MV4-11 (p53-wild type) and HL60 (p53-null) leukemia cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Arrested MV4-11 cells in the G0/G1 phase, with 86.71% of cells in this phase.
Arrested HL60 cells in the G2/M phase, with 34.13% of cells in this phase.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t MRT0-∞ Bioavailability C0
Rat[1] 2 mg/kg i.v. 0.208 h 0.0833 h 123 ng/mL 39.3 ng·h/mL 40.8 ng·h/mL 0.178 h 0.220 h / 213 ng/mL
Rat[1] 10 mg/kg i.p. 0.305 h 0.25 h 221 ng/mL 135 ng·h/mL 137 ng·h/mL 0.540 h 0.566 h 67.3 % /
In Vivo

HDAC6-IN-76 (20 mg/kg; i.p.; once daily) shows antileukemic activity in a
MOLM-13-Luc acute myeloid leukemia xenograft mouse model, as evidenced by suppressed tumor progression and a trend toward prolonged survival[1].

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

Molecular Weight

460.52

Formula

C24H32N2O7

CAS No.
SMILES

C[C@@]12O[C@]3(O[C@@H]([C@@H]([C@]([H])(CC[C@H]([C@@H]4CC2)C)[C@@]34OO1)C)OCC5=CC=CC(/C=C/C(NO)=O)=N5)[H]

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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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