MW 304.3 Da, Purity >98%. A potent, selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 9.4 μM). Displays selectivity over PRMT5, PRMT6 and CARM1 (IC50 values are 166, 283 and >400 μM respectively). Inhibits cell proliferation in leukemia cell lines.
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AI838772, ANM1_HUMAN, AW493413, DHQV, DIA6, EC 1.10.99.2, FLJ11090, HCP 1, HMT 2, HMT1 (hnRNP methyltransferase S. cerevisiae) like 2, HMT1 hnRNP methyltransferase, HMT1 hnRNP methyltransferase like 2, HMT1 hnRNP methyltransferase like 2 (S. cerevisiae), HRMT1 L2, Heterogeneous nuclear ribonucleoprotein methyltransferase 1 like 2, Heterogeneous nuclear ribonucleoproteins methyltransferase like 2, Histone-arginine N-methyltransferase PRMT1, Human mRNA for suppressor for yeast mutant, Human mRNA for suppressor for yeast mutant complete cds, IR1 B4, Interferon receptor 1-bound protein 4, MGC104252, MGC112732, MGC94180, Mrmt 1, NAD(P)H dehydrogenase quinone 2, NAD(P)H menadione oxidoreductase 1 dioxin inducible 2, NAD(P)H menadione oxidoreductase 2 dioxin inducible, NMOR2, NQO2_HUMAN, NRH dehydrogenase, NRH dehydrogenase [quinone] 2, NRH:quinone oxidoreductase 2, OTTHUMP00000015948, OTTHUMP00000015949, OTTHUMP00000015953, Ox 2, Protein arginine N-methyltransferase 1, Protein arginine methyltransferase 1, QR2, Quinone, Quinone reductase 2, R1B4, RP24-311F12.2, Ribosyldihydronicotinamide dehydrogenase, Ribosyldihydronicotinamide dehydrogenase [quinone], S. cerevisiae like 2, SCAN1, TYDP, TYDP1_HUMAN, Tyr-DNA phosphodiesterase 1, Tyrosyl-DNA phosphodiesterase 1
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Biological function summary
Protein Arginine Methyltransferase 1 modifies histones by methylating arginine residues affecting gene expression. PRMT1 often interacts with other proteins to form complexes that regulate transcription. TDP1 is essential in rescuing stalled topoisomerase I-DNA complexes by cleaving DNA-tyrosyl covalent linkages playing a role in DNA repair. NQO2 interacting with several cellular compounds protects cells by reducing orthoquinone substrates contributing to antioxidant defenses. This collaboration with other proteins enhances the cell's ability to maintain genomic integrity and regulate stress responses.
Pathways
PRMT1 is involved with the methylation pathway influencing gene regulation linked to arginine metabolism alongside proteins like PRMT5. TDP1 functions in the DNA repair pathways specifically the single-strand break repair mechanism working closely with proteins such as XRCC1. NQO2 is part of the detoxification pathway contributing to the cellular response to oxidative stress and working in concert with quinone reductase pathways. These pathways establish the important connections among these proteins and their partners driving essential cellular functions.
Publications (3)
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Journal of medicinal chemistry 57:2611-22 PubMed24564570
2014
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Antimicrobial agents and chemotherapy 55:2352-61 PubMed21402852
2011
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Nucleic acids research 35:4474-84 PubMed17576665
2007
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