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PRMT5-IN-33 (compound A8) is a selective inhibitor of PRMT5 that competes with SAM, exhibiting an IC50 of 10.9 nM. It induces apoptosis and inhibits the proliferation of Z-138 and MOLM-13 cells, demonstrating antitumor activity.
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| Description | PRMT5-IN-33 (compound A8) is a selective inhibitor of PRMT5 that competes with SAM, exhibiting an IC50 of 10.9 nM. It induces apoptosis and inhibits the proliferation of Z-138 and MOLM-13 cells, demonstrating antitumor activity. |
| Targets&IC50 | PRMT5:10.9 nM, PRMT1:6.89 μM |
| In vitro | PRMT5-IN-33 inhibits the proliferation of cells Z-138 and MOLM-13, with IC50 values of 123.2 nM and 248.6 nM, respectively. Additionally, PRMT5-IN-33 reduces sDMA levels in a dose-dependent manner. |
| In vivo | Administered orally twice daily for 13 days at doses ranging from 60 to 120 mg/kg, PRMT5-IN-33 inhibits the growth of MOLM-13 xenograft tumors in BALB/c mice in a dose-dependent manner without causing weight loss. |
| Formula | C25H24BrN5O3S |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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