1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. HDAC1-IN-3

HDAC1-IN-3 

Cat. No.: HY-144297
Handling Instructions

HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites.

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

HDAC1-IN-3 Chemical Structure

HDAC1-IN-3 Chemical Structure

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Description

HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites[1].

IC50 & Target

HDAC1

2.2 nM (IC50)

HDAC2

5.1 nM (IC50)

HDAC3

5.2 nM (IC50)

HDAC6

85.5 nM (IC50)

HDAC8

29.9 nM (IC50)

In Vitro

HDAC1-IN-3 (compound JX35) shows antimalarial activity with IC50s of 1.26 nM and 1.61 nM for wild-type Plasmodium falciparum (P. falciparum) parasite 3D7 and chloroquine-resistant P. falciparum parasite Dd2, respectively[1].
HDAC1-IN-3 (10 µM; 72 h) shows low cytotoxicity with IC50s of 1.02 µM and 1.21 µM for HepG2, 293T cells, respectively[1].
HDAC1-IN-3 (72 h) shows no cross-resistance with clinical antimalarial drugs with IC50s of 3.06, 2.18, 5.85 nM for GB4, C2A, CP286, respectively[1].
HDAC1-IN-3 (10, 30, 60, 100 nM; 3, 6, 12, 24 h) shows antimalarial activity in a time- and dose-dependent manner with asynchronous 3D7 parasites[1].
HDAC1-IN-3 (40 nM, 4 days; P. falciparum 3D7 cells) shows the killing effects of JX35 on P. falciparum parasites during asexual reproduction stages might be related to the inhibition of schizont growth and reinvasion of RBCs (red blood cells)[1].
HDAC1-IN-3 (5, 20 nM; 4 h) inhibits the expression of Pf HDAC against ART (artemisinin)-resistant parasite strains[1].
HDAC1-IN-3 reduces the inhibition of hHDACs with IC50s of 2.2, 5.1, 5.2, 85.5, 29.9 nM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: HepG2, 293T cells
Concentration: 10 µM
Incubation Time: 72 h
Result: Showed low cytotoxicity with IC50s of 1.02 µM and 1.21 µM for HepG2, 293T cells, respectively.

Western Blot Analysis[1]

Cell Line: P. falciparum 3D7 cells
Concentration: 5, 20 nM
Incubation Time: 4 h
Result: Inhibited the expression of Pf HDAC against ART (artemisinin)-resistant parasite strains.
In Vivo

HDAC1-IN-3 (30, 60, 90 mg/kg; i.p.; once daily for 5 days) shows acceptable therapeutic efficacy and safety[1].
HDAC1-IN-3 (5 mg/kg; i.p.) shows good pharmacokinetic properties[1].
Pharmacokinetic Parameters of HDAC1-IN-3 in Female BALB/c mice[1].

parameter JX35
Cmax (ng/mL) 539
Tmax (h) 0.25
AUC last (h·ng/mL) 638
AUC inf (h·ng/mL) 640
t1/2 (h) 0.91
CLZ/F (L/h/kg) 7.81
VZ/F (L/kg) 10.20
Female BALB/c mice; 5 mg/kg; i.p.

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

Animal Model: 6-8 weeks, BALB/c female mice[1]
Dosage: 30, 60, 90 mg/kg
Administration: I.p., once daily for 5 days
Result: Showed acceptable therapeutic efficacy and safety.
Animal Model: 6-8 weeks, female BALB/c mice[1]
Dosage: 5 mg/kg
Administration: I.p.
Result: Showed good pharmacokinetic properties.
Molecular Weight

453.92

Formula

C22H24ClN7O2

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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HDAC1-IN-3
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HY-144297
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