| Bioactivity | HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis[1]. |
| Invitro | HDACs/EZH2-IN-1 (5 μM, 48-120 h) 对携带 EZH2 Y641N 突变的 DLBCL 细胞 SU-DHL-6 具有强抗增殖效应，IC50 为 1.04 μM (48 h) 和 0.17 μM (120 h) [1]。HDACs/EZH2-IN-1 (0.1-100 μM, 48 h) 可抑制 AML 细胞的生长，IC50分别为 1.39 μM (MV4-11)、2.45 μM (U937) 和 1.32 μM (OCI-AML3)[1]。HDACs/EZH2-IN-1 (0.1-100 μM, 48 h) 可提高 HDAC1/2/3 的底物乙酰组蛋白 H3 (AC-HH3) 和 HDAC6 的底物乙酰-α-微管蛋白 (AC-α-tubulin) 的细胞内水平[1]。HDACs/EZH2-IN-1 (2 μM, 48 h) 可诱导 MOLM13 细胞分化，增加两种髓系成熟标志物 CD11b 和 CD14 的表达[1]。HDACs/EZH2-IN-1 (2-4 μM, 48 h) 诱导 MOLM13 细胞发生剂量依赖性凋亡[1]。HDACs/EZH2-IN-1 (1-2 μM) 协同抗 AML 化合物 (阿糖胞苷 (HY-13605), 柔红霉素 (HY-13062A), 吉瑞替尼 (HY-12432)) 对 MOLM13 细胞发挥抗癌作用[1]。HDACs/EZH2-IN-1 在人体和大鼠血浆中具有良好的代谢稳定性，其 T1/2 分别大于 180 min 和 138 min[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> HDACs/EZH2-IN-1 相关抗体: Cell Viability Assay[1] Cell Line: |
| Formula | C29H36BrN7O4 |
| Molar Mass | 626.54 |
| 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]. Zhang J, et al. Discovery of epigenetic modulators targeting HDACs and EZH2 simultaneously for the treatment of hematological malignancies. Bioorganic chemistry, 2024, 153, 107964. |