1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  2. HDAC
    CDK
    Apoptosis
  3. HDAC1/2 and CDK2-IN-1

HDAC1/2 and CDK2-IN-1 

Cat. No.: HY-143497
Handling Instructions

HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity.

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

HDAC1/2 and CDK2-IN-1 Chemical Structure

HDAC1/2 and CDK2-IN-1 Chemical Structure

CAS No. : 2418559-01-8

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Description

HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity[1].

IC50 & Target[1]

HDAC1

70.7 nM (IC50)

HDAC2

23.1 nM (IC50)

CDK2

0.80 nM (IC50)

In Vitro

HDAC1/2 and CDK2-IN-1 (compound 14d) shows excellent antiproliferative activities against H460, A375, HepG2, HCT116 and Hela cells with IC50 values of 1.59, 0.47, 0.86, 0.58 and 1.05 μM, respectively[1].
HDAC1/2 and CDK2-IN-1 (0.5 μM, 48 h) significantly inhibits the migration of H460 and A375 cells[1].
HDAC1/2 and CDK2-IN-1 (0-2 μM, 24 h) significantly blocks the cell cycle in the G2/M phase[1].
HDAC1/2 and CDK2-IN-1 (0-2 μM, 48 h) promotes cancer cell apoptosis in a dose-dependent manner[1].
HDAC1/2 and CDK2-IN-1 (1 μM, 12 h) inhibits CDK2 and HDAC activity, causing cancer cell death[1].
HDAC1/2 and CDK2-IN-1 (1 μM, 24 h) strongly increases ROS levels in A375 cells, causes cancer cell death by improving intracellular ROS levels[1].

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

Cell Cycle Analysis

Cell Line: A375, HCT116, H460 and Hela cells[1]
Concentration: 0, 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Significantly blocked the cell cycle, induced a loss of G0/G1 phase cells and an increase of G2/M phase cells, led to an apparent accumulation of cells in G2/M phase at 0.5 μM (A375, the percentage from 13.70 to 57.03%; HCT116, from 27.46 to 76.99%; Hela, from 7.89% to 51.85%).

Apoptosis Analysis

Cell Line: A375, HCT116, H460 and Hela cell lines[1]
Concentration: 0, 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Promoted cancer cell apoptosis in a dose-dependent manner, with the apoptosis rates of 91.99% (A375), 89.60% (HCT116), 59.10% (H460), and 22.36% (Hela) respectively at the concentration of 2 μM.

Immunofluorescence

Cell Line: A375 cells[1]
Concentration: 1 μM
Incubation Time: 12 h
Result: Significantly inhibited CDK2 and increased the acetylation level of histone H3, inhibited CDK2 and HDAC activity, causing cancer cell death.
In Vivo

HDAC1/2 and CDK2-IN-1 (BALB/c nude mice, 0-100 mg/kg, IP, once daily for 21 days) significantly inhibits the tumor growth[1].
HDAC1/2 and CDK2-IN-1 (compound 14d) (ICR mice; 4 mg/kg, IV; 20 mg/kg, IP) exhibits desirable pharmacokinetic properties[1].
Pharmacokinetic Parameters of HDAC1/2 and CDK2-IN-1 in male ICR mice[1].

Dose (mg/kg) 4 20
Administration IV IP
T1/2 (h) 1.48 2.84
Tmax (h) 2
Cmax (ng/mL) 1360
AUC0-t (ng/mL*h) 2850 7240
MRT0-t (h) 0.563 4.54
CL (mL/(min/kg)) 23.3
F (%) 50.8

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

Animal Model: Male ICR mice (n = 9)[1]
Dosage: 4 mg/kg (IV), 20 mg/kg (IP)
Administration: IV, IP, once (Pharmacokinetic Analysis)
Result: Exhibited desirable pharmacokinetic properties.
Animal Model: BALB/c nude mice (5-6 weeks, HCT116 xenograft model)[1]
Dosage: 0, 25, 50 and 100 mg/kg
Administration: IP, once daily for 21 days
Result: Significantly inhibited the tumor growth, the tumor growth inhibitions were 28%, 40% and 44% at doses of 25, 50 and 100 mg/kg, respectively.
Molecular Weight

483.95

Formula

C26H22ClN7O

CAS No.
SMILES

O=C(NC1=CC=CC=C1N)C2=CC=C(CN3C=NC4=C(NC5=CC=C(C)C=C5)N=C(Cl)N=C34)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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HDAC1/2 and CDK2-IN-1
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HY-143497
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