Bioactivity | HDAC-IN-49 is a potent unselective HDAC (HDAC) inhibitor with IC50s of 13 nM, 14 nM, 21 nM, 1880 nM, and 10 nM for HDAC1, HDAC2, HDAC3, HDAC4, and HDAC6. HDAC-IN-49 demonstrates prominent antileukemic activity with low cytotoxic activity toward healthy cells[1]. |
Invitro | HDAC-IN-49 (compound 10h) shows remarkable cytotoxic potential against different therapy-resistant leukemia cell lines, with IC50 values of 0.375 μM, 0.218 μM, and 0.285 μM for HAL01, HL60 and Jurkat cells, respectively.HDAC-IN-49 (compound 10h; 1-5 μM; 48 h) treatment results in a significant apoptosis induction in HL60 cells[1].HDAC-IN-49 (compound 10h; 6-36 μM; 24 h) shows a dose-dependent increase in the level of acetylation of α-tubulin and histone 3 (H3) in HL60 cells[1]. Apoptosis Analysis[1] Cell Line: |
Name | HDAC-IN-49 |
Formula | C26H27FN4O4 |
Molar Mass | 478.52 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Nina Reßing, et al. Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. J Med Chem. 2022 Nov 24;65(22):15457-15472. |