HDAC-IN-49
Based on 1 publication(s) in Google Scholar
HDAC-IN-49 is a potent unselective HDAC (HDAC) inhibitor with IC50s of 13 nM, 14 nM, 21 nM, 1880 nM, and 10 nM for HDAC1, HDAC2, HDAC3, HDAC4, and HDAC6. HDAC-IN-49 demonstrates prominent antileukemic activity with low cytotoxic activity toward healthy cells.
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- CAS No.: 3035173-63-5
- Formule: C26H27FN4O4
- Masse moléculaire:478.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) HDAC-IN-49
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Activité biologique
Description
IC50 & Target
[1]|
HDAC1 13 nM (IC50) |
HDAC2 14 nM (IC50) |
HDAC3 21 nM (IC50) |
HDAC4 1880 nM (IC50) |
HDAC6 10 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HAL-01 | IC50 |
0.375 μM
Compound: 10h
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Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 36351184] |
| HL-60 | IC50 |
0.218 μM
Compound: 10h
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Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 36351184] |
| Jurkat | IC50 |
0.285 μM
Compound: 10h
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Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 36351184] |
In Vitro
HDAC-IN-49 (compound 10h) shows remarkable cytotoxic potential against different therapy-resistant leukemia cell lines, with IC50 values of 0.375 μM, 0.218 μM, and 0.285 μM for HAL01, HL60 and Jurkat cells, respectively.
HDAC-IN-49 (compound 10h; 1-5 μM; 48 h) treatment results in a significant apoptosis induction in HL60 cells[1].
HDAC-IN-49 (compound 10h; 6-36 μM; 24 h) shows a dose-dependent increase in the level of acetylation of α-tubulin and histone 3 (H3) in HL60 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HL60 cells
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Concentration:1 μM and 5 μM
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Incubation Time:48 h
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Result:Resulted in a significant apoptosis induction.
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Cell Line:HL60 cells
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Concentration:6 μM, 12 μM, 24 μM, 36 μM
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Incubation Time:24 h
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Result:Increased in the level of acetylation of α-tubulin and histone 3 (H3).
Chemical Information
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CAS No. 3035173-63-5
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Masse moléculaire 478.52
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Formule C26H27FN4O4
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SMILES
O=C(NO)C1=CC=C(CN(CC(NCC2=CC=CC=C2)=O)C(C3=CC=C(N(C)C)C=C3)=O)C(F)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC-IN-49 Related Classifications
HY-151897 Related Classifications
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