LRRK2

LRRK2製品

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  • LRRK2阻害剤 (14)
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S2882 IKK-16 IKK-16 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.
Life Sci Alliance, 2024, 10.26508/lsa.202101282
Cell, 2023, 186(22):4851-4867.e20
J Clin Invest, 2023, 133(4)e162190
S7343 URMC-099 URMC-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.
Cell Commun Signal, 2023, 21(1):82
Oncogene, 2023, 42(14):1132-1143.
Oncogenesis, 2023, 12(1):35
S7584 LRRK2-IN-1 LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
ACS Chem Neurosci, 2021, 10.1021/acschemneuro.1c00399
Dev Dyn, 2021, 10.1002/dvdy.316
E0998 PFE-360 PFE-360(PF-06685360) is a brain-penetrant and selective LRRK2 small-molecule kinase inhibitors.
Viruses, 2022, 14(9)2058
S7367 GNE-0877 (DNL201) GNE-0877 (DNL201) is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM.
Cancer Discov, 2020, CD-20-0160
S7528 GNE-7915 GNE-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.
Am J Physiol Renal Physiol, 2018, 315(5):F1465-F1477
S7664 GSK2578215A GSK2578215A 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.
J Exp Med, 2017, 214(10):3051-3066
S0726 XMD8-85 (ERK5-IN-1) XMD8-85 (ERK5-IN-1) is a selective and potent inhibitor of ERK5 and LRRK2 with IC50s of 0.162 μM and 0.339 μM, respectively.
S9694 MLi-2 MLi-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-54252 CZC-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.
S7368 GNE-9605 GNE-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-25146 CZC-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.
S8202 PF-06447475 PF-06447475 is a potent, selective, and brain penetrant LRRK2 kinase inhibitor with IC50 of 3 nM.
S2948 HG-10-102-01 HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2 with IC50 of 23.3 nM and the G2019S mutant with IC50 of 3.2 nM.
S2882 IKK-16 IKK-16 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.
Life Sci Alliance, 2024, 10.26508/lsa.202101282
Cell, 2023, 186(22):4851-4867.e20
J Clin Invest, 2023, 133(4)e162190
S7343 URMC-099 URMC-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.
Cell Commun Signal, 2023, 21(1):82
Oncogene, 2023, 42(14):1132-1143.
Oncogenesis, 2023, 12(1):35
S7584 LRRK2-IN-1 LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
ACS Chem Neurosci, 2021, 10.1021/acschemneuro.1c00399
Dev Dyn, 2021, 10.1002/dvdy.316
E0998 PFE-360 PFE-360(PF-06685360) is a brain-penetrant and selective LRRK2 small-molecule kinase inhibitors.
Viruses, 2022, 14(9)2058
S7367 GNE-0877 (DNL201) GNE-0877 (DNL201) is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM.
Cancer Discov, 2020, CD-20-0160
S7528 GNE-7915 GNE-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.
Am J Physiol Renal Physiol, 2018, 315(5):F1465-F1477
S7664 GSK2578215A GSK2578215A 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.
J Exp Med, 2017, 214(10):3051-3066
S0726 XMD8-85 (ERK5-IN-1) XMD8-85 (ERK5-IN-1) is a selective and potent inhibitor of ERK5 and LRRK2 with IC50s of 0.162 μM and 0.339 μM, respectively.
S9694 MLi-2 MLi-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-54252 CZC-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.
S7368 GNE-9605 GNE-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-25146 CZC-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.
S8202 PF-06447475 PF-06447475 is a potent, selective, and brain penetrant LRRK2 kinase inhibitor with IC50 of 3 nM.
S2948 HG-10-102-01 HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2 with IC50 of 23.3 nM and the G2019S mutant with IC50 of 3.2 nM.

LRRK2阻害剤の選択性比較

Tags: LRRK2 inhibitor|LRRK2 agonist|LRRK2 activator|LRRK2 inducer|LRRK2 antagonist|LRRK2 signaling pathway|LRRK2 assay kit