PR5-LL-CM01 是一种有效的 (PRMT5) 抑制剂 (IC50= 7.5 μM)。PR5-LL-CM01 具有抗肿瘤活性。
货号:ajcx38600
CAS:1005307-86-7
分子式:C23H27N7
分子量：401.51
溶解度:DMSO : 11.11 mg/mL (27.67 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies[1].

PR5-LL-CM01 has a range of IC50 at 2-4 μM in PDAC cells (PANC1, MiaPaCa2 and AsPC1, and a range of IC50 at 10-11 μM in CRC cells (HT29, HCT116 and DLD1). PR5-LL-CM01 has higher efficacy to specifically inhibit cancer cells and demonstrated low toxicity in normal cells. PR5-LL-CM01 strongly inhibited colony forming ability in both PANC1 and HT29 cells[1].PR5-LL-CM01 inhibits NF-κB activation and its target gene expression in PDAC and CRC cells[1].PR5-LL-CM01 (0-15 μM) dramatically decreases TNFα and IL8 expression in both PANC1 and HT29 cells[1].

PR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect[1].

[1]. Prabhu L, et al. Adapting AlphaLISA high throughput screen to discover a novel small-molecule inhibitor targeting protein arginine methyltransferase 5 in pancreatic and colorectal cancers. Oncotarget. 2017;8(25):39963-39977.