HDAC-IN-49
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.
For research use only. We do not sell to patients.
- CAS No.: 3035173-63-5
- Formula: C26H27FN4O4
- Molecular Weight:478.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
HDAC1 13 nM (IC50) |
HDAC2 14 nM (IC50) |
HDAC3 21 nM (IC50) |
HDAC4 1880 nM (IC50) |
HDAC6 10 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HAL-01 | IC50 |
0.375 μM
Compound: 10h
|
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
|
[PMID: 36351184] |
| HL-60 | IC50 |
0.218 μM
Compound: 10h
|
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
|
[PMID: 36351184] |
| Jurkat | IC50 |
0.285 μM
Compound: 10h
|
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
|
[PMID: 36351184] |
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.
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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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Molecular Weight 478.52
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)