Shopping Cart
- Remove All
- Your shopping cart is currently empty
HDAC-IN-76 (compound 6i), a histone deacetylase (HDAC) inhibitor, demonstrates robust antimalarial activity, particularly against the asexual blood stages of Plasmodium. The compound exhibits potent efficacy with IC 50 values of 30 nM and 98 nM against Pf3D7 (chloroquine drug-susceptible strain) and PfDd2 (chloroquine drug-resistant strain), respectively. Moreover, HDAC-IN-76 shows selective inhibition towards parasites, displaying IC 50 values of 7 nM and 9 nM against human HDAC1 and HDAC6, respectively, and effectively inhibits PfHDAC1.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
Description | HDAC-IN-76 (compound 6i), a histone deacetylase (HDAC) inhibitor, demonstrates robust antimalarial activity, particularly against the asexual blood stages of Plasmodium. The compound exhibits potent efficacy with IC 50 values of 30 nM and 98 nM against Pf3D7 (chloroquine drug-susceptible strain) and PfDd2 (chloroquine drug-resistant strain), respectively. Moreover, HDAC-IN-76 shows selective inhibition towards parasites, displaying IC 50 values of 7 nM and 9 nM against human HDAC1 and HDAC6, respectively, and effectively inhibits PfHDAC1. |
Targets&IC50 | hHDAC6:9 nM, hHDAC1:7 nM |
In vitro | HDAC-IN-76 exhibits low cytotoxicity in HEK293 cells. At a concentration of 1 μM, HDAC-IN-76 effectively inhibits PfHDAC1 with an inhibition rate of 70.2%. It shows minimal activity against liver-stage parasites (IC 50 PbEEF [Plasmodium berghei exo-erythrocytic form]=0.25 μM), displays good microsomal stability (t 1/2 > 60 min) and has low toxicity in HEK293 cells (IC 50 =136 μM, selectivity index SI=544). Additionally, HDAC-IN-76 readily penetrates HepG2 cells and inhibits HDAC activity. |
Molecular Weight | 470.52 |
Formula | C27H26N4O4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.