1. Epigenetics
  2. Histone Methyltransferase
  3. PR5-LL-CM01

PR5-LL-CM01 

Cat. No.: HY-109963
Handling Instructions

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

For research use only. We do not sell to patients.

PR5-LL-CM01 Chemical Structure

PR5-LL-CM01 Chemical Structure

CAS No. : 1005307-86-7

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Description

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

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 weeks old Male NSG mice (bearing PANC1 or HT29 cells)[1]
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.
Molecular Weight

401.51

Formula

C₂₃H₂₇N₇

CAS No.
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PR5-LL-CM01
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