PR5-LL-CM01

Research use only, not for human use.

PR5-LL-CM01 is a novel selective, small-molecule inhibitor of PRMT5 methyltransferase with IC50 of 7.5 uM.

PR5-LL-CM01 is a novel selective, small-molecule inhibitor of PRMT5 methyltransferase with IC50 of 7.5 uM; displays >10-fold selectivity over PRMT3, and no inhibitory activity over PRMT1/4/6/8; exhibits cell viability inhibition with IC50 of 2-4 uM in PDAC cells, IC50 of 10-11 uM in CRC cells, more potent than EPZ015666; significantly inhibits NF-κB activation in PDAC and CRC cells, and shows dramatic anti-tumor efficacy in vivo.

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.PR5-LL-CM01 inhibits NF-κB activation and its target gene expression in PDAC and CRC cells.PR5-LL-CM01 (0-15 μM) dramatically decreases TNFα and IL8 expression in both PANC1 and HT29 cells.

PR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect. Animal Model:6-8 weeks old Male NSG mice (bearing PANC1 or HT29 cells)Dosage:20 mg/kg (drug stock dissolved in 1:1 Cremophor:ethanol solution)Administration:Intraperitoneally 3 times per week; 32 days (PANC1 model); 10 days (HT29 model)Result:Led to significant tumor inhibition in both PANC1 and HT29 xenografted mice. Did not visibly affect the mice body weight.

PR5-LL-CM01

Chromatin/Epigenetic

HMTase

HMTase

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1005307-86-7

401.518

C23H27N7

>98% (HPLC)

In Vitro:?DMSO : 11.11 mg/mL (27.67 mM)

CC1=CC=C(NC2=C3C(N(C4=CC=CC=C4)N=C3)=NC(NCCN(C)C)=N2)C=C1C

N6-(2-(dimethylamino)ethyl)-N4-(3,4-dimethylphenyl)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine-4,6-diamine

(-20℃)

With Ice Pack

≥ 2 years