LRRK2
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 | ||
| S2882 | IKK-16 (IKK Inhibitor VII) | <1 mg/mL | 97 mg/mL | <1 mg/mL |
| S9694 | MLi-2 | 76 mg/mL | 76 mg/mL | 8 mg/mL |
| S6534 | CZC-54252 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7343 | URMC-099 | <1 mg/mL | 84 mg/mL | 6 mg/mL |
| S7368 | GNE-9605 | <1 mg/mL | 89 mg/mL | 12 mg/mL |
| S2002 | CZC-25146 | <1 mg/mL | 98 mg/mL | <1 mg/mL |
| S7367 | GNE-0877 | <1 mg/mL | 67 mg/mL | <1 mg/mL |
| S7584 | LRRK2-IN-1 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8202 | PF-06447475 | <1 mg/mL | 61 mg/mL | <1 mg/mL |
| S7528 | GNE-7915 | <1 mg/mL | 22 mg/mL | <1 mg/mL |
| S7664 | GSK2578215A | <1 mg/mL | 79 mg/mL | <1 mg/mL |
LRRK2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 |
|---|---|---|---|
| S2882 |
IKK-16 (IKK Inhibitor VII)IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. IKK-16 also inhibits LRRK2 Ser935 phosphorylation in cells and LRRK2 kinase activity in vitro with IC50 of 50 nM. |
Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
|
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| S9694 |
MLi-2MLi-2 is an orally active and highly selective inhibitor of LRRK2. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro with IC50 of 0.76 nM, a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 with IC50 of 1.4 nM, and a radioligand competition binding assay with IC50 of 3.4 nM. |
||
| S6534 |
CZC-54252CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for human wild type LRRK2 and G2019S LRRK2, respectively. |
||
| S7343 |
URMC-099URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy. |
||
| S7368 |
GNE-9605GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively. |
||
| S2002 |
CZC-25146CZC-25146 is a potent and selective LRRK2 inhibitor with IC50 of 4.76 nM and 6.87 nM for human wild type LRRK2 and G2019S LRRK2, respectively. |
||
| S7367 |
GNE-0877GNE-0877 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM. |
||
| S7584 |
LRRK2-IN-1LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively. |
||
| S8202 |
PF-06447475PF-06447475 is a potent, selective, and brain penetrant LRRK2 kinase inhibitor with IC50 of 3 nM. |
||
| S7528 |
GNE-7915GNE-7915 is a highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor, with IC50 and Ki of 9 nM and 1 nM, respectively. |
||
| S7664 |
GSK2578215AGSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), 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 |
|---|---|---|---|
| S2882 |
IKK-16 (IKK Inhibitor VII)IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. IKK-16 also inhibits LRRK2 Ser935 phosphorylation in cells and LRRK2 kinase activity in vitro with IC50 of 50 nM. |
Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
|
|
| S9694 |
MLi-2MLi-2 is an orally active and highly selective inhibitor of LRRK2. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro with IC50 of 0.76 nM, a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 with IC50 of 1.4 nM, and a radioligand competition binding assay with IC50 of 3.4 nM. |
||
| S6534 |
CZC-54252CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for human wild type LRRK2 and G2019S LRRK2, respectively. |
||
| S7343 |
URMC-099URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy. |
||
| S7368 |
GNE-9605GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively. |
||
| S2002 |
CZC-25146CZC-25146 is a potent and selective LRRK2 inhibitor with IC50 of 4.76 nM and 6.87 nM for human wild type LRRK2 and G2019S LRRK2, respectively. |
||
| S7367 |
GNE-0877GNE-0877 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM. |
||
| S7584 |
LRRK2-IN-1LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively. |
||
| S8202 |
PF-06447475PF-06447475 is a potent, selective, and brain penetrant LRRK2 kinase inhibitor with IC50 of 3 nM. |
||
| S7528 |
GNE-7915GNE-7915 is a highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor, with IC50 and Ki of 9 nM and 1 nM, respectively. |
||
| S7664 |
GSK2578215AGSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively. |
