| Bioactivity | 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]. |
| Invitro | 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]. Cell Cytotoxicity Assay[1] Cell Line: |
| 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 |
| Name | HDAC1-IN-3 |
| Formula | C22H24ClN7O2 |
| Molar Mass | 453.92 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Wang M, et al. Drug Repurposing of Quisinostat to Discover Novel Plasmodium falciparum HDAC1 Inhibitors with Enhanced Triple-Stage Antimalarial Activity and Improved Safety. J Med Chem. 2022; 65(5):4156-4181. |