HDAC1-IN-3
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.
- CAS No.: 2482998-35-4
- Formula: C22H24ClN7O2
- Molecular Weight:453.92
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
More
Biological Activity
|
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) |
Plasmodium |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
1.21 μM
Compound: JX35
|
Cytotoxicity against HEK293T cells incubated for 72 hrs by CCK-8 assay
Cytotoxicity against HEK293T cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 35175762] |
| HepG2 | IC50 |
1.02 μM
Compound: JX35
|
Cytotoxicity against human HepG2 cells incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human HepG2 cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 35175762] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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.
-
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.
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 |
MedChemExpress (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.
Chemical Information
-
CAS No. 2482998-35-4
-
Molecular Weight 453.92
-
Formula C22H24ClN7O2
-
SMILES
O=C(C1=CN=C(N(CC2)CC32CN(CC4=CN(C)C5=C4C=CC(C#N)=C5)C3)N=C1)NO.[H]Cl
-
Shipping
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)