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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]. | [in vivo]
CARM1-IN-4 (compound 11f; 10, 25 mg/kg/day; ip; for 12 days) shows evident inhibitory effect in BALB/c nude mice bearing subcutaneous HCT116 xenograft[1].
| Animal Model: | 6 to 8-week-old female BALB/c nude mice bearing subcutaneous HCT116 xenograft[1] | | Dosage: | 10, 25 mg/kg | | Administration: | Intraperitoneal injection; daily; for 12 days | | Result: | Showed evident inhibitory effect.
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| [IC 50]
CARM1: 9 nM (IC50); PRMT1: 56 nM (IC50); PRMT6: 30 nM (IC50); PRMT8: 31 nM (IC50); PRMT3: 2637 nM (IC50); PRMT5: >100,000 nM (IC50) | [References]
[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. DOI:10.1016/j.ejmech.2024.116288 |
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