HDAC1-IN-12 

HDAC1-IN-12 is a Plasmodium falciparum HDAC1 (PfHDAC1) inhibitor with an IC₅₀ of 4.1 nM against Pf3D7. HDAC1-IN-12 inhibits PfHDAC1, upregulates histone H₃ acetylation in P. falciparum parasites, downregulates malaria invasion-related gene expression, and exhibits favorable safety profiles, improved physicochemical properties, and potent in vivo antimalarial activity. HDAC1-IN-12 can be used for the research of malaria^[1].

HDAC1-IN-12 (compound 5ac) (72 h) potently inhibits P. falciparum 3D7 growth with high selectivity over human HepG2 and HEK293T cells (IC₅₀ = 4.1 nM for P. falciparum 3D7, 1.5 μM for HepG2, 15 μM for HEK293T)^[1].
HDAC1-IN-12 (72 h; 6 h) retains potency against multidrug-resistant P. falciparum strains and inhibits artemisinin-resistant ring-stage parasites (IC₅₀ = 3.9 nM for GB4, 6 nM for CP286, 5.3 nM for 6267)^[1].
HDAC1-IN-12 (5 nM, 50 nM; 3 h) increases the acetylation level of P. falciparum histone H₃^[1].
HDAC1-IN-12 (5-50 nM; 3 h) downregulates invasion-related genes and blocks P. falciparum egress and erythrocyte invasion^[1].

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

HDAC1-IN-12 (compound 5ac) (30 mg/kg; i.p.; daily; 4 days) exhibits clear in vivo antimalarial efficacy in BALB/c mice Plasmodium berghei ANKA-infected model^[1].

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

467.50

C₂₃H₂₆FN₇O₃

O=C(C1=CN=C(N2CCN(C(CN3CC(C4=CC(F)=CC=C4N5C)=C5CC3)=O)CC2)N=C1)NO

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ni H, et al. Discovery of γ-Tetrahydrocarboline Derivatives as Plasmodium falciparum Histone Deacetylase Inhibitors for Treatment of Malaria. J Med Chem. 2026 Jan 22;69(2):1434-1453.  [Content Brief]