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Chemical Structure : PRT382
Catalog No.: PC-49559Not For Human Use, Lab Use Only.
PRT382 (PRT-382) is a potent, selective and SAM-competitive PRMT5 inhibitor with IC50 of 2.8 nM in filtration binding assays with recombinant human PRMT5/MEP50 and histone H2A as the protein substrate.
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PRT382 (PRT-382) is a potent, selective and SAM-competitive PRMT5 inhibitor with IC50 of 2.8 nM in filtration binding assays with recombinant human PRMT5/MEP50 and histone H2A as the protein substrate.
PRT382 displays no significant activity against 38 other methyltransferases (e.g DNMTs, MLL1-4 complexes, EZH1 and EZH2 complexes, NRMTs, NSD, SUVs, SMYs, SETs, PRDM9), and other members of the PRMT family.
PRT382 exhibits an IC50 of 27 nM in a reducing sDMA assay in the Granta-519 lymphoma cell line.
PRT382 demonstrated anti-proliferative efficacy in the leukemia and lymphoma cell lines CCMCL-1, JVM-2, U-2932, RL, and KARPAS-422 with IC50 values of 0.01-0.5 uM.
PRT382 demonstrated low clearance and high oral bioavailability in mice, rats, and dogs (F% = 70–80%), and high AUC levels (1175 h*kg*ng/mL/mg) in mice.|
PRT382 demonstrated anti-proliferative potency in HG3 and Mec-1 cells when compared to SAM-competitive PRMT5 inhibitor compounds JNJ-64619178, LLY-283, and PF-06855800.
PRT382 (10 mg/kg, 0.5% methylcellulose) displayed antileukemic activity in an aggressive model of CLL/RT.
| M.Wt | 441.27 | |
| Formula | C18H18Cl2N4O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Hing ZA, et al. Nat Commun. 2023 Jan 6;14(1):97.
2. Sloan SL, et al. Blood. 2023 Jun 2:blood.2022019419.
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