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.
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- Fòrmula: C23H26FN7O3
- Peso molecular:467.50
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Actividad biológica
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (female, 6–8 weeks old) were inoculated with 105 P. berghei ANKA\r\nparasite-infected erythrocytes via intraperitoneal injection (i.p.) on\r\nday 0.[1]
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Dosage:30 mg/kg
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Administration:i.p.; daily; 4 days
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Result:Showed no detectable parasitemia until day 11, with parasitemia levels remaining markedly lower than the DMSO control group.
Chemical Information
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Peso molecular 467.50
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Fòrmula C23H26FN7O3
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SMILES
O=C(C1=CN=C(N2CCN(C(CN3CC(C4=CC(F)=CC=C4N5C)=C5CC3)=O)CC2)N=C1)NO
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC1-IN-12 Related Classifications
HY-181010 Related Classifications
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- HDAC1-IN-12
- HDAC
- Parasite
- Plasmodium falciparum histone deacetylase 1
- histone H3 acetylation
- human HepG2 cells
- Plasmodium falciparum
- GB4
- PfHDAC1
- artemisinin-resistant ring-stage parasites
- P. falciparum egress
- Plasmodium berghei ANKA-infected model
- 6267
- malaria invasion-related gene
- P. falciparum 3D7
- BALB/c mice
- HEK293T cells
- erythrocyte invasion
- multidrug-resistant P. falciparum strains
- Quisinostat
- P. falciparum histone H3
- P. falciparum parasites
- CP286
- Inhibitor
- inhibitor
- inhibit