PF1070A
PF1070A is a Pf HDAC1 inhibitor with an IC50 of 0.0011 μM. By inhibiting histone deacetylase (HDAC) activity, PF1070A induces histone H4 hyperacetylation and chromatin remodeling, arrests cell cycle progression prior to nuclear division, and exhibits antimalarial activity against multidrug-resistant Plasmodium falciparum strains with high selectivity. PF1070A is suitable for use in malaria research.
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- No. CAS: 146556-41-4
- Fòrmula: C31H44N4O6
- Peso molecular:568.70
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
12 μM
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Cytotoxicity against human HepG2 hepatocarcinoma cells assessed via MTS assay following 48 h incubation.
Cytotoxicity against human HepG2 hepatocarcinoma cells assessed via MTS assay following 48 h incubation.
|
34491031 |
In Vitro
PF1070A (compound 6) potently inhibits the growth of the multidrug-resistant Plasmodium falciparum Dd2 strain and the drug-sensitive Plasmodium falciparum 3D7 strain after 48-72 h of treatment, with EC50 values of 0.091 μM and 0.069 μM, respectively. Furthermore, PF1070A exhibits much higher selectivity for the parasite than for human HepG2 cells, with a selectivity index of 150[1].
PF1070A (24-48 h) exerts a reversible anti-proliferative inhibitory effect on asynchronous Plasmodium falciparum strain Dd2; parasite parasitemia rebounds following the removal of PF1070A after 24 h or 48 h of treatment[1].
PF1070A (2 h) potently inhibits the catalytic activity of recombinant PfHDAC1, with an IC50 of 0.0011 μM[1].
PF1070A (4 h) induces hyperacetylation of histone H4 in synchronized cultures of Plasmodium falciparum 3D7 at the trophozoite stage[1].
PF1070A induces perinuclear histone H4 hyperacetylation and rearrangement of the microtubule cytoskeleton in synchronized cultures of Plasmodium falciparum 3D7, which is consistent with chromatin remodeling mediated by HDAC inhibition[1].
After incubation with mouse liver microsomes for 1 h, the remaining percentage of PF1070A (0.1 mM; 1 h for the microsomal stability assay; 200 μM; 24 h for the kinetic solubility assay) is 30.3%, and its kinetic solubility in PBS (pH 7.4) at room temperature is 51.8 μM[1].
PF1070A (50-500 µg; 4 days) inhibits root growth of Tachinagaha soybean seedlings in a concentration-dependent manner[2].
PF1070A (10-80 µg; 1 week) induces chlorosis in Tachinagaha soybean leaves in a concentration-dependent manner over a 1-week incubation period[2].
PF1070A (50-500 µg; 4 days) inhibits root growth of Fukuyutaka, Enrei, and Harosoy soybean seedlings, with similar IC50 values (721, 741, and 754 µg/mL, respectively) over the 4-day incubation period, despite differences in the susceptibility of these soybean cultivars to Calonectria ilicicola[2].
PF1070A (administered for 1 month) is produced by the Calonectria ilicicola strain, and its yield ranges from 0.01 to 4.46 mg/100 mL after 1 month of cultivation in PDB at 25°C in the dark[2].
When PF1070A (9 μM; 8-24 h) is combined with zinc ions, cadmium ions, or Dexamethasone (HY-14648), it synergistically enhances the activity of the MT-I promoter and the level of MT-I mRNA in mouse L13-17 cells[3].
PF1070A (30 μM; 24 h) activates the mouse MT-I promoter in mouse Ltk− cells via two specific regions (positions -150/-149 and -49/-43), and this mechanism differs from the MREs-mediated zinc activation mechanism[3].
PF1070A (3-9 μM; 24 h) enhances the activity of the MT-I promoter in mouse L13-17 cells[3].
PF1070A (90 μM) induces the production of MT mRNA and MT protein in human HeLa-S3 cells, an effect similar to that observed in mouse L13-17 cells[3].
PF1070A (90 μM, 9 μM + 70 μM ZnCl2; 6 h) does not modulate the intracellular zinc concentration in mouse L13-17 cells, indicating that its metallothionein (MT) induction activity is independent of zinc mobilization[3].
PF1070A (5 nM; combined with 10 nM CdCl2) induces exogenous BCL-6 expression, thereby suppressing endogenous BCL-6 levels in BT549 breast cancer cells[4].
PF1070A (added at 6, 18, 30, or 42 HPI) inhibits the growth of Plasmodium falciparum Dd2 across all intraerythrocytic stages prior to late schizogony, with the strongest inhibitory effect when administered before the trophozoite stage; administration at 6 HPI results in cell cycle arrest prior to nuclear division[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse L13-17 cells
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Concentration:9 μM
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Incubation Time:8 h
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Result:Enhanced MT-I mRNA levels in mouse L13-17 cells when combined with zinc ions, cadmium ions, or Dexamethasone.
Chemical Information
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No. CAS 146556-41-4
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Peso molecular 568.70
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Fòrmula C31H44N4O6
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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)