| Bioactivity | CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC50 = 2±1 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines[1]. |
| Invitro | CARM1-IN-5 对 CARM1 具有选择性。IC50 分别为 2 ± 1 nM (CARM1), 213 ± 45 nM (PRMT1), 942 ± 78 nM (PRMT3), 64 ± 9 nM (PRMT6), 73 ± 8 nM (PRMT8), >100,000 nM (PRMT5), >100,000 nM (PRMT7)[1]。CARM1-IN-5 对两种黑色素瘤细胞系的抗增殖活性为 IC50 = 0.55 ± 0.03 μM (A375); 1.74 ± 0.07μM (A2058)[1]。CARM1-IN-5 (0-5 μM; 72 h) 可以进入 A375 Cells 并直接与 CARM1 结合。可以通过抑制 CARM1 的甲基转移酶活性，在细胞环境中影响 CARM1 底物的不对称二甲基化水平[1]。体外代谢稳定性[1] t1/2 (min) |
| In Vivo | CARM1-IN-5 (i.p.; 10 mg/kg/day 和 25 mg/kg/day; 14 天) 显著抑制 BALB/c 皮下移植 A375 的裸鼠的肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C22H26ClN3O2S |
| Molar Mass | 431.98 |
| 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]. Liu Z, et al. Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma. J Med Chem. 2024 Apr 25;67(8):6313-6326. |