HDAC1-IN-15
HDAC1-IN-15 is a HDAC1 inhibitor with activity against hHDAC1, PfHDAC1 and HDAC8. HDAC1-IN-15 inhibits the proliferation of asexual blood-stage Plasmodium falciparum and reduces the survival rate of stage IV-V gametocytes of Plasmodium falciparum. HDAC1-IN-15 is applicable to malaria-related research.
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- CAS. Nr.: 3055432-86-2
- Formel: C22H22N6O5
- Molecular Weight:450.45
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Plasmodium |
hHDAC1 |
hHDAC8 |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
50 μM
Compound: 4h
|
Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 to 72 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 to 72 hrs by MTT assay
|
[PMID: 37989057] |
| Jurkat | IC50 |
1.5 μM
Compound: 4h
|
Cytotoxicity against human Jurkat cells assessed as cell growth inhibition incubated for 24 to 72 hrs by MTT assay
Cytotoxicity against human Jurkat cells assessed as cell growth inhibition incubated for 24 to 72 hrs by MTT assay
|
[PMID: 37989057] |
| MCF7 | IC50 |
50 μM
Compound: 4h
|
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 24 to 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 24 to 72 hrs by MTT assay
|
[PMID: 37989057] |
| NAMALVA | IC50 |
0.8 μM
Compound: 4h
|
Cytotoxicity against human NAMALVA cells assessed as cell growth inhibition incubated for 24 to 72 hrs by MTT assay
Cytotoxicity against human NAMALVA cells assessed as cell growth inhibition incubated for 24 to 72 hrs by MTT assay
|
[PMID: 37989057] |
In Vitro
HDAC1-IN-15 (compound 12) (0.005-5 μM; 72 h) potently inhibits proliferation of Plasmodium falciparum 3D7 (IC50 = 0.086 μM) and Chloroquine (HY-17589A)-resistant Dd2 (IC50 = 0.064 μM) asexual blood stages in vitro, with no measurable cytotoxicity against HEK293T cells at concentrations up to 5 μM[1].
HDAC1-IN-15 (5 μM; 72 h) impairs survival of Plasmodium falciparum NF54 stage IV-V gametocytes, resulting in 47.55% survival[1].
HDAC1-IN-15 potently inhibits recombinant Plasmodium falciparum PfHDAC1 (96% inhibition at 1 μM, 99% at 10 μM) and human rhHDAC1, rhHDAC8 enzymes in a cell-free enzymatic assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS. Nr. 3055432-86-2
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Molecular Weight 450.45
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Formel C22H22N6O5
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SMILES
COC1=CC(NC2=C3N=CN(C3=NC=N2)CC4=CC=C(C=C4)C(NO)=O)=CC(OC)=C1OC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)