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AES-350 is a potent and orally active HDAC6 inhibitor (IC50 and Ki of 0.0244 μM and 0.035 μM, respectively), also exhibiting activity against HDAC-3, -8, and -11 in an enzymatic assay with IC50 values of 0.187 μM, 0.245 μM, and >1 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $107 | In Stock | |
5 mg | $263 | In Stock | |
10 mg | $379 | In Stock | |
25 mg | $683 | In Stock | |
50 mg | $959 | In Stock | |
100 mg | $1,330 | In Stock |
Description | AES-350 is a potent and orally active HDAC6 inhibitor (IC50 and Ki of 0.0244 μM and 0.035 μM, respectively), also exhibiting activity against HDAC-3, -8, and -11 in an enzymatic assay with IC50 values of 0.187 μM, 0.245 μM, and >1 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research. |
Targets&IC50 | HDAC6:24.4 nM, HDAC11:245 nM , HDAC3:187 nM |
In vitro | AES-350 (0.25-4 μM;?18 hours) induces MV4-11 cells apoptosis in a dose-dependent manner.?The late apoptosis ratios are 8.74%, 11.7%,16.08%, 30.97%, and 38.48%, respectively at 0.25 μM-4 μM.?AES-350 has submicromolar activity (IC50=0.58±0.13 μM) against MV4-11 cells than to that of vorinostat (IC50=0.31±0.061 μM).?AES-350 is more ligand efficient and exemplifies a large therapeutic index (IC50>30 μM in noncancerous MRC-9 cells).?AES-350 is also shown to be effective in AML-3 (acute myeloid leukemia) cells (IC50=0.73 ± 0.12 μM).?An ELISA is performed using HeLa cervical cancer cell lysates, and HeLa cells highly express HDAC6 and are sensitive to AES-350.?Correspondingly, ELISA assays depicted a dose-dependent increase in HDAC6 inhibition (IC50=0.58±0.13 μM), Western blot analysis shows that AES-350 (0.1-10 μM) induces a dose-dependent increase in acetylated α-tubulin (Ac-α-tubulin), a substrate of HDAC. |
Molecular Weight | 312.36 |
Formula | C18H20N2O3 |
Cas No. | 847249-57-4 |
Smiles | CC(C)(C)c1ccc(cc1)C(=O)Nc1ccc(cc1)C(=O)NO |
Relative Density. | 1.218 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (320.14 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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