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CARM1-IN-5
CAS No. :
MCE 国际站：CARM1-IN-5
产品活性：CARM1-IN-5 (Compound 17e) 是 CARM1 的高效选择性抑制剂（IC50 = 2±1 nM）。CARM1-IN-5 通过直接与 CARM1 相互作用，有效阻止其对底物蛋白进行甲基化。CARM1-IN-5 对黑色素瘤细胞系具有显著的抗增殖作用。
研究领域：Epigenetics
作用靶点：Histone Methyltransferase
In Vitro: CARM1-IN-5 is selective for CARM1. IC50 is 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).
CARM1-IN-5 antiproliferative activity against two melanoma cell lines was IC50 = 0.55 ± 0.03 μM (A375); 1.74 ± 0.07 μM (A2058).
CARM1-IN-5 (0-5 μM; 72 h) can enter A375 Cells and bind directly to CARM1. CARM1-IN-5 also can affect the level of asymmetric dimethylation of CARM1 substrates in the cellular environment by inhibiting the methyltransferase activity of CARM1.
In vitro metabolic stability in Mouse Liver Microsomes
| t1/2 (min) | Cl (mL/min/kg) |
| 41.5 | 132 |
