PRMT Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S8664 | GSK3326595 (Pemrametostat, EPZ015938) | Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models. |
|
|
| 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. |
|
|
| S6737 | C7280948 | C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
||
| 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. | ||
| E1871New | TNG-462 | TNG-462 is an orally active, potent and selective inhibitor of methylthioadenosine (MTA)-cooperative PRMT5. It exhibits significant antitumor activity, including durable regressions and complete responses, against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation solid tumours. | ||
| E1600 | AMG 193 | AMG-193 is an orally active and MTA-cooperative inhibitor of PRMT5 with potent biochemical and cellular activity. AMG-193, in combination with MTA, selectively targets and inhibits the growth of MTAP-deficient tumour cells by suppressing PRMT5, with an IC50 of 0.107 μM, while sparing normal cells that possess wild-type MTAP. AMG-193 also exhibits antitumour activity. | ||
| E2887 | MS023 hydrochloride | MS023 hydrochloride (Compound 3) is a potent, selective and cell-active inhibitor of human type I protein arginine methyltransferases (PRMT), with IC50 values of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively. | ||
| E1481New | AM-9747 | AM-9747 (PRMT5-IN-25) is a potent inhibitor of PRMT5 with a Ki of 0.06 nM. It exhibits antiproliferative activity and a significant oral antitumor effect in mouse models employing patient-derived xenografts (PDX). | ||
| E4612 | iCARM1 | iCARM1 (CARM1-IN-6) is a potent and selective inhibitor of protein arginine methyltransferase CARM1 (PRMT4) with an IC50 of 12.3 μM. It potently suppresses breast cancer cell growth both in vitro and in vivo and can be used in cancer research. | ||
| E4701 | CMP-5 | CMP5 is a potent and selective small molecule inhibitor of PRMT5. It is found to selectively block S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. It also exhibits potential for research into treatment for EBV+ lymphomas and other B-cell NHL subtypes. | ||
| 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. | ||
| E1658 | PRT543 | PRT543 is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) with broad antitumor activity in vitro and in vivo. It also inhibits the methyltransferase activity of the PRMT5/MEP50 complex with an IC50 of 10.8 nM. | ||
| E1429 | T1-44 | T1-44 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It exhibits anti-tumour activity in pancreatic cancers. | ||
| S7748 | EPZ015666 (GSK3235025) | EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. |
|
|
| S8112 | MS023 | MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively. |
|
|
| S8111 | GSK591 | GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with an IC50 of 4 nM. |
|
|
| S8624 | Onametostat (JNJ-64619178) | Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favourable pharmacokinetics and safety properties. |
|
|
| S7884 | AMI-1 | AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. |
|
|
| S7832 | SGC707 | SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively. |
|
|
| S8147 | MS049 | MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. |
|
|
| S7820 | EPZ020411 2HCl | EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. |
|
|
| S8340 | SGC2085 | SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs. |
|
|
| S8209 | HLCL-61 HCL | HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukaemia. |
|
|
| S5445 | AMI-1 (free acid) | AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. |
Products are for research use only. Not for human use. We do not sell to patients.
©Copyright 2013 Selleck Chemicals. All Rights Reserved.