PR5-LL-CM01

• CAT Number: I034984
• CAS Number: 1005307-86-7
• Molecular Formula: C23H27N7
• Molecular Weight: 401.51
• Purity: ≥95%
• Synonyms: 6-N-[2-(dimethylamino)ethyl]-4-N-(3,4-dimethylphenyl)-1-phenylpyrazolo[3,4-d]pyrimidine-4,6-diamine
• InChI: InChI=1S/C23H27N7/c1-16-10-11-18(14-17(16)2)26-21-20-15-25-30(19-8-6-5-7-9-19)22(20)28-23(27-21)24-12-13-29(3)4/h5-11,14-15H,12-13H2,1-4H3,(H2,24,26,27,28)
• InChIKey: UPAZOMJFUXPAJI-UHFFFAOYSA-N
• SMILES: CC1=C(C=C(C=C1)NC2=C3C=NN(C3=NC(=N2)NCCN(C)C)C4=CC=CC=C4)C

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].

Reference

[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.
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