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HDAC-IN-76

HDAC-IN-76
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.
Catalog No. T200090

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HDAC-IN-76

Catalog No. T200090

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.
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight470.52
FormulaC27H26N4O4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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