PRMT
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S7748 | EPZ015666(GSK3235025) | <1 mg/mL | 60 mg/mL | 48 mg/mL |
| S8147 | MS049 | 56 mg/mL | 56 mg/mL | 50 mg/mL |
| S8340 | SGC2085 | <1 mg/mL | 62 mg/mL | 62 mg/mL |
| S7820 | EPZ020411 2HCl | 81 mg/mL | 100 mg/mL | 100 mg/mL |
| S7832 | SGC707 | <1 mg/mL | 59 mg/mL | 59 mg/mL |
| S8883 | LLY-283 | 5 mg/mL | 68 mg/mL | 3 mg/mL |
| S8858 | GSK3368715 (EPZ019997) 3HCl | 81 mg/mL | 81 mg/mL | '81 mg/mL |
| S6737 | C7280948 | <1 mg/mL | 55 mg/mL | 5 mg/mL |
| S8112 | MS023 | <1 mg/mL | 57 mg/mL | 57 mg/mL |
| S5445 | AMI-1, free acid | -1 mg/mL | 20 mg/mL | -1 mg/mL |
| S8664 | GSK3326595 (EPZ015938) | <1 mg/mL | 90 mg/mL | 90 mg/mL |
| S8111 | GSK591 | <1 mg/mL | 76 mg/mL | '76 mg/mL |
| S8209 | HLCL-61 HCL | <1 mg/mL | 76 mg/mL | 76 mg/mL |
| S8624 | JNJ-64619178 | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S7884 | AMI-1 | 10 mg/mL | 100 mg/mL | <1 mg/mL |
| S0184 | XY1 | ˂1 mg/mL | 59 mg/mL | 1 mg/mL |
PRMT製品
| 製品コード | 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. |
(B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.
|
|
| S8147 |
MS049MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. |
||
| S8340 |
SGC2085SGC2085 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. |
||
| S7820 |
EPZ020411 2HClEPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. |
||
| S7832 |
SGC707SGC707 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. |
||
| S8883新 |
LLY-283LLY-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. |
||
| S8858新 |
GSK3368715 (EPZ019997) 3HClGSK3368715 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. |
||
| S6737新 |
C7280948C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro. |
||
| S8112 |
MS023MS023 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. |
||
| S5445 |
AMI-1, free acidAMI-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. |
||
| S8664 |
GSK3326595 (EPZ015938)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 |
GSK591GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM. |
Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5-catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control.
|
|
| S8209 |
HLCL-61 HCLHLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia. |
||
| S8624 |
JNJ-64619178JNJ-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. |
||
| S7884 |
AMI-1AMI-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. |
Effects of microinjection of AMI-1 into the RVLM on cardiovascular activity in the Ang II-induced hypertensive rats. The representative original tracings (A)
|
|
| S0184新 |
XY1XY1 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. |
| 製品コード | 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. |
(B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.
|
|
| S8147 |
MS049MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. |
||
| S8340 |
SGC2085SGC2085 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. |
||
| S7820 |
EPZ020411 2HClEPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. |
||
| S7832 |
SGC707SGC707 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. |
||
| S8883新 |
LLY-283LLY-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. |
||
| S8858新 |
GSK3368715 (EPZ019997) 3HClGSK3368715 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. |
||
| S6737新 |
C7280948C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro. |
||
| S8112 |
MS023MS023 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. |
||
| S5445 |
AMI-1, free acidAMI-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. |
||
| S8664 |
GSK3326595 (EPZ015938)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 |
GSK591GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM. |
Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5-catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control.
|
|
| S8209 |
HLCL-61 HCLHLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia. |
||
| S8624 |
JNJ-64619178JNJ-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. |
||
| S7884 |
AMI-1AMI-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. |
Effects of microinjection of AMI-1 into the RVLM on cardiovascular activity in the Ang II-induced hypertensive rats. The representative original tracings (A)
|
| 製品コード | 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 |
|---|---|---|---|
| S0184新 |
XY1XY1 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. |
