HDAC6-IN-65
HDAC6-IN-65 is a selective HDAC6 inhibitor (IC50 = 0.9 nM) and also exhibits a certain suppressive effect on HDAC3 (IC50 = 39.4 nM). HDAC6-IN-65 can induce the accumulation of α-tubulin (ac-tubulin) and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) in Neuro-2a cells. HDAC6-IN-65 can be used for the study of melanoma.
For research use only. We do not sell to patients.
- CAS No.: 3028442-70-5
- Formula: C20H18ClN3O4S
- Molecular Weight:431.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
HDAC6 0.9 nM (IC50) |
HDAC3 39.4 nM (IC50) |
In Vitro
HDAC6-IN-65 (Compound 14) exhibits significant antiproliferative activity against leukemia cell line (MV4-11, IC50 = 0.57 μM), as well as significant antiproliferative activity against other tumor cells (MM.1S, IC50 = 2.45 μM) (Neuro-2a, IC50 = 6.24 μM) (SH-SY5Y, IC50 = 3.75 μM), and low toxicity to normal cells (HEK-293, IC50 = 6.09 μM) (pNHF, IC50 = 16.24 μM) (MRC9, IC50 = 19.08 μM)[1].
HDAC6-IN-65 (0.05-5 μM) significantly induces the accumulation of α-tubulin (ac-tubulin) in Neuro-2a cells at a concentration of 50 nM (a marker of HDAC6 inhibition), and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) was also increased at a concentration of 1 μM[1].
HDAC6-IN-65 (0.5 μM, 6-72 h), despite its weaker or more transient inhibition of class I HDACs, may exhibit PD effects that persist beyond its systemic exposure in RDES cell line[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:RDES cell line
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Concentration:0.5 μM
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Incubation Time:6 h, 12 h, 24 h, 48 h, 72 h
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Result:Significantly increased ac-tubulin levels in RDES cells at 6 h, which persist until 48 h, and begin to decline at 72 h. Ac-histone H3 levels increased at 6 and 12 h, but returned to baseline at 24 h.
Parmacokinetics
| Species | Dose | Route | Tmax | T1/2 | Cmax | AUClast |
|---|---|---|---|---|---|---|
| Mice | 20 mg/kg | i.p. | 0.25 h | 1.66 h | 4839 ng/mL | 2935 ng·h/mL |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 female mice were injected subcutaneously with 106 in vivo passaged SM1 melanoma cells suspended in 100 μL of PBS[1].
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Dosage:25 mg/kg
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Administration:I.p., once daily for 14 days, M-F
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Result:The mean tumor growth inhibition rate (TGI) was 56%.
All mice showed normal body weight and organ function, with no signs of toxicity.
Flow cytometry revealed an increase in CD4+ and CD8+ T cells, NK cells, and M1 macrophages, and a decrease in M2 macrophages in the tumor microenvironment.
Chemical Information
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CAS No. 3028442-70-5
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Molecular Weight 431.89
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Formula C20H18ClN3O4S
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SMILES
O=S(N(CC1=CN=CC=C1)CC2=CC=C(C=C2)C(NO)=O)(C3=C(C=CC=C3)Cl)=O
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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-65 Related Classifications
HY-178110 Related Classifications
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