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PRMT
PRMT製品
- All (25)
- PRMT阻害剤 (23)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|---|
| 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. |
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| S8664 | Pemrametostat (GSK3326595) | 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. | ||
| S8111 | GSK591 | GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM. |
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| 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. | ||
| 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. |
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| 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. | ||
| S6737 | C7280948 | C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro. | ||
| 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 favorable pharmacokinetics and safety properties. | ||
| 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 vaules ranging from 1.5 to 81 nM. | ||
| S8883 | LLY-283 | LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity. | ||
| S7820 | EPZ020411 2HCl | EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. | ||
| S8209 | HLCL-61 HCL | HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia. | ||
| S8147 | MS049 | MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. | ||
| 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. TC-E 5003 modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signaling pathways and can possibly be further developed as an anti-inflammatory compound. | ||
| 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. | ||
| S8479 | LLY-284 | LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. LLY-284 is much less active than LLY-283 and can be used as a negative control for LLY-283. | ||
| E1600New | 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 tumor cells by suppressing PRMT5, with an IC50 of 0.107 μM, while sparing normal cells that possess wild-type MTAP. AMG-193 also exhibits antitumor 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. | ||
| 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. | ||
| E1024 | MRTX1719 | MRTX1719 is a potent, selective inhibitor of the protein arginine methyltransferase 5·methylthioadenosine phosphorylase complex (PRMT5•MTA), a potentially tumor-selective target for therapeutic intervention. | ||
| S0184 | XY1 | XY1 is an inactive, close analog of SGC707 that can be used as the negative control for 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. | ||
| E4701New | 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 exhibit potential for research into treatment for EBV+ lymphomas and other B-cell NHL subtypes. | ||
| E1349New | TNG908 | 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. | ||
| E1658New | 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. | ||
| 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. | ||
| 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. |
|
|
| S8664 | Pemrametostat (GSK3326595) | 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. | ||
| S8111 | GSK591 | GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM. |
|
|
| 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. | ||
| 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. | ||
| S6737 | C7280948 | C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro. | ||
| 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 favorable pharmacokinetics and safety properties. | ||
| 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 vaules ranging from 1.5 to 81 nM. | ||
| S8883 | LLY-283 | LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity. | ||
| S7820 | EPZ020411 2HCl | EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. | ||
| S8209 | HLCL-61 HCL | HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia. | ||
| S8147 | MS049 | MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. | ||
| 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. TC-E 5003 modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signaling pathways and can possibly be further developed as an anti-inflammatory compound. | ||
| 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. | ||
| E1600New | 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 tumor cells by suppressing PRMT5, with an IC50 of 0.107 μM, while sparing normal cells that possess wild-type MTAP. AMG-193 also exhibits antitumor 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. | ||
| 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. | ||
| E1024 | MRTX1719 | MRTX1719 is a potent, selective inhibitor of the protein arginine methyltransferase 5·methylthioadenosine phosphorylase complex (PRMT5•MTA), a potentially tumor-selective target for therapeutic intervention. | ||
| E4701New | 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 exhibit potential for research into treatment for EBV+ lymphomas and other B-cell NHL subtypes. | ||
| E1349New | TNG908 | 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. | ||
| E1658New | 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. | ||
| 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. | ||
| E1600New | 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 tumor cells by suppressing PRMT5, with an IC50 of 0.107 μM, while sparing normal cells that possess wild-type MTAP. AMG-193 also exhibits antitumor activity. | ||
| E4701New | 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 exhibit potential for research into treatment for EBV+ lymphomas and other B-cell NHL subtypes. | ||
| E1349New | TNG908 | 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. | ||
| E1658New | 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. |
PRMT阻害剤の選択性比較
Tags: PRMT inhibitor | PRMT activator | PRMT inhibition
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