LRRK2

LRRK2製品

All (14)
LRRK2阻害剤 (14)
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
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.	Br J Pharmacol, 2024, 10.1111/bph.17305 Life Sci Alliance, 2024, 10.26508/lsa.202101282 Immunobiology, 2024, 229(5):152843
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 K_i 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 K_i 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.	Exp Neurobiol, 2024, 33(1):36-45
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 K_i 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.	Br J Pharmacol, 2024, 10.1111/bph.17305 Life Sci Alliance, 2024, 10.26508/lsa.202101282 Immunobiology, 2024, 229(5):152843
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 K_i 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 K_i 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.	Exp Neurobiol, 2024, 33(1):36-45
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 K_i 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