1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  2. HDAC
    Apoptosis
  3. HDAC-IN-37

HDAC-IN-37 

Cat. No.: HY-146750
Handling Instructions

HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis.

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

HDAC-IN-37 Chemical Structure

HDAC-IN-37 Chemical Structure

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Description

HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis[1].

IC50 & Target[1]

HDAC1

55.1 nM (IC50)

HDAC3

1.24 μM (IC50)

HDAC8

0.948 μM (IC50)

HDAC6

34.2 μM (IC50)

In Vitro

HDAC-IN-37 (compound 9d) exhibits the potent antiproliferative activities on the HCT116, MDA-MB-231, K562 cell lines at IC50s of 0.50, 0.38, 0.12 μM, respectively[1].
HDAC-IN-37 (0 - 10 μM; 24 hours) significantly induces the accumulation of acetylated histones at H3K9 and H4K5 in HCT-116 cells[1].
HDAC-IN-37 (0 - 10 μM; 24 hours) induces cell apoptosis in HCT-116 cells by 35.22%, 58.34, 80.7% at 0.5, 1, 5 μM, mainly occurring in early apoptosis[1].
HDAC-IN-37 (0 - 10 μM; 6, 12, 24 hours) causes G0/G1 phase arrest of HCT-116 cells in a time-dependent manner, effectively preventing cell cycle progression[1].
HDAC-IN-37 (0, 0.1, 0.5, 1, 5 and 10 μM; 0, 6, 12, 24, 36, 48 hours) down-regulates the levels of CDK2, Cyclin D1 and the up-regulates P21 with dose- and time-dependent manners in HCT-116 cells, and decreases Bcl-2 of Bcl-2 family in dose- and time-dependent manners[1].

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

Cell Proliferation Assay

Cell Line: HCT-116, MDA-MB-231, HepG2, A549, SGC7901 and K562[1]
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Exhibited the potent antiproliferative activities on the HCT116, MDA-MB-231, K562 cell lines at IC50 of 0.50, 0.38, 0.12 μM, respectively.

Western Blot Analysis

Cell Line: HCT-116[1]
Concentration: 0, 0.1, 0.5, 1, 5 and 10 μM
Incubation Time: 24 hours
Result: Significantly induced the accumulation of acetylated histones at H3K9 and H4K5 in HCT-116 cells.

Apoptosis Analysis

Cell Line: HCT-116[1]
Concentration: 0.1, 0.5, 1, 5 and 10 μM
Incubation Time: 24 hours
Result: Induced cell apoptosis in HCT-116 cells by 35.22%, 58.34, 80.7% at 0.5, 1, 5 μM, mainly occurring in early apoptosis.

Cell Cycle Analysis

Cell Line: HCT-116[1]
Concentration: 0.1, 0.5, 1, 5 and 10 μM
Incubation Time: 0, 6, 12 and 24 hours
Result: Caused G0/G1 phase arrest of HCT-116 cells in a time-dependent manner, effectively preventing cell cycle progression.
Molecular Weight

449.94

Formula

C23H24ClN7O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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HDAC-IN-37
Cat. No.:
HY-146750
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