LRRK2 Inhibitor

LRRK2-IN-20 (EX. 4.64) is a LRRK2 inhibitor with a pIC₅₀ of 0.7921 nM. LRRK2-IN-20 can be used in Parkinson's disease (PD) research.

LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC₅₀ of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease.

LRRK2-IN-19 is a PROTAC target protein ligand that can be used to synthesize PROTAC JH-XII-03-02 (HY-155150). JH-XII-03-02 is a highly potent and selective LRRK2 PROTAC degrader, which can be used in Parkinson's disease research.

LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC₅₀ values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier.

LRRK2/JNK3-IN-1 is a brain-penetrant multi-target inhibitor of LRRK2 (including G2019S mutant and wild-type) and JNK3, with enzymatic IC₅₀ values of 3.90 nM against LRRK2^G2019S, 3.24 nM against wild-type LRRK2, and 22.1 nM against JNK3. LRRK2/JNK3-IN-1 displays favorable selectivity in a 97-kinase profiling screen, and also shows inhibitory activity against JNK1, JNK2, and MKNK2. LRRK2/JNK3-IN-1 can be used for the research of Parkinson's disease.

PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor.

STF-3600 is a LRRK2^G2019S inhibitor with an IC₅₀ of 0.9 nM against the human target. It has oral activity and can cross the blood-brain barrier. STF-3600 selectively inhibits kinase activity, including autophosphorylation at Ser935 and Ser1292, as well as phosphorylation of the endogenous substrate Rab10 at Thr73. STF-3600 inhibits vacuolization of type II pulmonary epithelial cells in wild-type/heterozygous mice, while it induces this vacuolization phenotype in homozygous mice. STF-3600 can be used in Parkinson's disease research.

LRRK2-IN-15 is an LRRK2 inhibitor. The IC₅₀ value for PBMC cells is 5 nM, and the IC₅₀ value for BCRP is 1.5 μM. LRRK2-IN-15 can be used for research on Parkinson's disease.

LY2023-001 is a potent G2019S LRRK2 inhibitor with an IC₅₀ of 12.9 nM. LY2023-001 formed stable hydrogen bonds with Glu1948, and Ala1950 in the G2019S LRRK2 protein.

LRRK2-IN-13 (Compound 13) is an inhibitor of LRRK2 (IC₅₀=0.57 nM). LRRK2-IN-13 has brain penetrating properties.

LRRK2-IN-21 is a selective, blood-brain barrier-permeable LRRK2 kinase inhibitor with an IC₅₀ of 0.35 nM. LRRK2-IN-21 inhibits TTK kinase with an IC₅₀ of 70 nM. LRRK2-IN-21 is applicable to the research of Parkinson's disease.

LRRK2-IN-12 (compound 1) inhibits the activity of LRRK2 G20195 (IC₅₀=0.45 nM), LRRK2 WT (IC₅₀=1.1 nM) and LRRK2 WT ADP-Glo (IC₅₀=0.46 nM). LRRK2-IN-12 can be used for Alzheimer's Disease research.

Indazole (Standard) is the analytical standard of Indazole. This product is intended for research and analytical applications. Indazole, also called isoindazole, a heterocyclic aromatic organic compound. Its derivatives display a broad variety of biological activities including anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour properties. Indazole and its derivatives can be used for research of cancer, neurological disorders, cardiovascular diseases, gastrointestinal diseases.

FX 2149 is a blood-brain barrier-permeable LRRK2 inhibitor. FX 2149 inhibits the GTP-binding activity of LRRK2, reduces the kinase activity of LRRK2, and attenuates LPS (HY-D1056)-induced upregulation of LRRK2. FX 2149 alleviates mutant LRRK2-induced neurodegeneration, microglial activation, static aggregation of mitochondria and lysosomes, reduces apoptosis, and improves mitochondrial and lysosomal motility deficits in neurites. FX 2149 can be used in research related to Parkinson's disease.

Multi-kinase-IN-14 is an orally active and blood-brain barrier-permeable multi-kinase inhibitor. Multi-kinase-IN-14 reduces the excessive phosphorylation of α-synuclein by inhibiting four kinases (ABL1, DYRK1A, GSK3β, and LRRK2) and stabilizing microtubules. Multi-kinase-IN-14 is applicable for research on neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease.

CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC₅₀ values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases.

LRRK2 inhibitor 1 (Standard) is the analytical standard of LRRK2 inhibitor 1 (HY-111493). This product is intended for research and analytical applications. LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC₅₀ of 6.8.

LRRK2-IN-1 (Standard) is the analytical standard of LRRK2-IN-1 (HY-10875). This product is intended for research and analytical applications. 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.

LRRK2-IN-9 (compound 78) is a LRRK2 inhibitor that can be used in studies related to Parkinson's disease, Alzheimer's disease, and amyotrophic lateral sclerosis.

IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC₅₀s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC₅₀s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.