Bioactivity | CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity[1]. |
Invitro | CARM1-IN-4 (compound 11f) 在 HCT116 细胞系中表现出显着的抗增殖活性 (IC50=3.13 μM)[1]。CARM1-IN-4 (0.625-5 μM;72 小时) 在 HCT116 细胞中引起剂量依赖性细胞凋亡[1]。CARM1-IN-4 (0.625-10 μM; 48小时) 有效抑制 CARM1 的甲基转移酶活性,影响细胞环境中 CARM1 底物的不对称去甲基化水平[1]。CARM1-IN-4 表现出相对较高的线粒体稳定性,在小鼠线粒体中的半衰期较长 (T1/2=217 分钟)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CARM1-IN-4 相关抗体: Apoptosis Analysis[1] Cell Line: |
In Vivo | CARM1-IN-4 (compound 11f;10、25 mg/kg/天;腹腔注射;持续 12 天) 对皮下 HCT116 异种移植物的 BALB/c 裸鼠显示出明显的肿瘤抑制作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 2878481-07-1 |
Formula | C24H42N2O4 |
Molar Mass | 422.60 |
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]. Chenyu Liu, et al. Structure-based discovery of potent CARM1 inhibitors for colorectal cancer therapy. Eur J Med Chem. 2024 Mar 4:269:116288. |