HDAC6-IN-42
HDAC6-IN-42 (compound 2b) is an HDAC6 inhibitor (IC50=0.009 μM). HDAC6-IN-42 shows significant anti-leukemia activity and synergistic effect with Decitabine (HY-A0004). HDAC6-IN-42 can be used for the AML research.
For research use only. We do not sell to patients.
- Formula: C24H28FN3O4
- Molecular Weight:441.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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HDAC6 0.009 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HAL-01 | IC50 |
2.32 μM
Compound: 2b
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Cytotoxicity against human HAL-01 cells measured for 72 hrs by celltiter-glo assay
Cytotoxicity against human HAL-01 cells measured for 72 hrs by celltiter-glo assay
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[PMID: 38714044] |
| HL-60 | IC50 |
2.04 μM
Compound: 2b
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Cytotoxicity against human HL-60 cells measured for 72 hrs by celltiter-glo assay
Cytotoxicity against human HL-60 cells measured for 72 hrs by celltiter-glo assay
|
[PMID: 38714044] |
| Jurkat | IC50 |
3.08 μM
Compound: 2b
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Cytotoxicity against human Jurkat cells measured for 72 hrs by celltiter-glo assay
Cytotoxicity against human Jurkat cells measured for 72 hrs by celltiter-glo assay
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[PMID: 38714044] |
HDAC6-IN-42 increases in antiproliferative activity against the three leukemia cell lines (HAL01: 2.32±0.77 μM, HL60: 2.04±0.62 μM, Jurkat: 3.08±0.59 μM) which is more than five times higher than HPOB[1].
HDAC6-IN-42 shows even higher selectivity for HDAC6 against HDAC2 (IC50=0.787 μM; SIHDAC2/6=87) and HDAC3 (IC50= 0.520 μM; SIHDAC3/6=58) compared to HDAC1 (IC50=0.228 μM; SIHDAC1/6=25)[1].
HDAC6-IN-42 (1, 5 μM; 48 h) exhibits any cytotoxic activity against healthy fibroblasts and exhibits a significant increase in the percentage of late apoptotic cells[1].
HDAC6-IN-42 excels significantly in inducing specific drug synergy with Decitabine (HY-A0004) against AML cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HAL01 (B-cell acute lymphoblastic leukemia or B-ALL), HL60 (acute myeloid leukemia or AML), and Jurkat (T-cell acute lymphoblastic leukemia or T-ALL)
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Concentration:
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Incubation Time:
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Result:Exhibited antiproliferative activities in the single digit micromolar range against all three cell lines and thus exceeded the activity of HPOB.
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Cell Line:leukemic cell lines (K562, DND41, Jurkat, SUPB15, REH, Kasumi 2, 697, PEER, HAL01, MV4-11, MOLM13 and HL60) and healthy fibroblasts (F107 and F188)
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Concentration:0.2, 0.4, 0.8, 1.3 μM
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Incubation Time:24 h
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Result:Increased α-tubulin acetylation while affecting H3 acetylation to a lesser extent.
Chemical Information
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Molecular Weight 441.50
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Formula C24H28FN3O4
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SMILES
O=C(CN(C1=CC=CC=C1C)C(CC2=C(F)C=C(C(NO)=O)C=C2)=O)NC3CCCCC3
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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)