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.
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- CAS No.: 3028442-70-5
- Formule: C20H18ClN3O4S
- Masse moléculaire:431.89
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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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HDAC6 0.9 nM (IC50) |
HDAC3 39.4 nM (IC50) |
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.
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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.
| 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 |
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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Masse moléculaire 431.89
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Formule 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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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC6-IN-65 Related Classifications
HY-178110 Related Classifications
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