PRMT inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| E1349 | TNG908 (Ralometostat) | Ralometostat (TNG908) is a potent, selective, and brain-penetrant inhibitor of PRMT5 with an IC50 of 4 μM, acting through an MTA-cooperative mechanism. It also shows antitumor activity in a xenograft model. | ||
| S8664 | GSK3326595 (Pemrametostat, EPZ015938) | Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumour growth in vitro and in vivo in animal models. |
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| S8883 | LLY-283 | LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. It shows antitumor activity. |
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| S6737 | C7280948 | C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro. |
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| S8858 | GSK3368715 3HCl | GSK3368715 3HCl is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp values ranging from 1.5 to 81 nM. |
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| S0855 | TC-E 5003 | TC-E 5003 (NSC 30176, Compound 2e) is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1) with IC50 of 1.5 μM. This compound modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signalling pathways and can possibly be further developed as an anti-inflammatory compound. |
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| E1024 | MRTX1719 (Navlimetostat) | MRTX1719 is a potent, selective inhibitor of the protein arginine methyltransferase 5·methylthioadenosine phosphorylase complex (PRMT5•MTA), a potentially tumour-selective target for therapeutic intervention. |
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| E1088 | TP-064 |
TP-064 is a potent and selective small molecule inhibitor of PRMT4 with IC50 < 10 nM, >100 fold more selective for PRMT4 than other PRMTs. |
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| E1007 | BRD0639 |
BRD0639 is a first-in-class PBM-competitive small molecule inhibitor that disrupts the PRMT5-RIOK1 complex with IC50s of 7.5 μM and 16 μM in permeabilised and living cells, respectively. |
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| E7603 | Furamidine dihydrochloride | Furamidine dihydrochloride (DB75 dihydrochloride, NSC 305831 dihydrochloride) is a potent and selective inhibitor of protein arginine methyltransferase 1 (PRMT1) with an IC50 of 9.4 μM. It is also a potent inhibitor of tyrosyl-DNA phosphodiesterase (Tdp1). It exhibits potent anti-Plasmodium vivax and antiparasitic activity in vitro and in vivo, and its ability to disrupt mitochondrial membranes also supports its use as an antimicrobial agent. | ||
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