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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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HDAC6 0.009 μM (IC50) |
Cellular Effect
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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
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[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] |
In Vitro
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. Further protocols information, click here.
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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.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC6-IN-42 Related Classifications
HY-161516 Related Classifications
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