lrr

BC-1258 is a unique small molecule F-box/LRR-repeat protein 2 (FBXL2) activator.

Boc-LRR-AMC is a fluorogenic substrate for the trypsin-like activity of the 26S proteasome or 20S proteolytic core. Upon enzymatic cleavage by the 26S proteasome or 20S proteolytic core, amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify 26S proteasome or 20S proteolytic core trypsin-like activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.

Boc-LRR-AMC TFA is a fluorescent protease substrate used to detect the trypsin-like activity of the 26S proteasome or 20S proteasome core.

LRRK2 inhibitor 1 is a selective and potent LRRK2 inhibitor with an IC50 of 13 nM.LRRK2 inhibitor 1 inhibits DCLK1 kinase with an IC50 value of 2.61 nM.

LRRK2-IN-7 is a selective, CNS permeable and potent LRRK2 kinase inhibitor (IC50: 0.9 nM) for the study of Parkinson's disease.

LRRK2-IN-15 is an inhibitor of LRRK2. It exhibits an IC50 value of 5 nM in PBMC cells and 1.5 μM for BCRP. This compound is utilized in the research of Parkinson's disease.

LRRK2-IN-16 (compound 25) is an inhibitor of the LRRK2 kinase with an IC50 value of less than 5 μM. It is applicable for research in neurodegenerative and autoimmune diseases.

LRRK2-IN-17 is an orally active LRRK2 inhibitor with IC50 values of 3.5 nM for WT and 3.3 nM for G2019S, and it also inhibits RET kinase with an IC50 of 59 nM. LRRK2-IN-17 is utilized in research related to cancer and Parkinson's disease (PD).

LRRK2-IN-19 is a PROTAC-targeted protein ligand utilized in the synthesis of PROTAC JH-XII-03-02. JH-XII-03-02 acts as an effective and selective LRRK2 PROTAC degrader, which is applicable for research in Parkinson's disease.

LRRK2-IN-20 (EX. 4.64) is a selective inhibitor of LRRK2 with a potency of pIC50 at 0.7921 nM. This compound is applicable in research studies focused on Parkinson's Disease (PD).

LRRK2-IN-1 is an effective and selective LRRK2 inhibitor.

LRRK2-IN-6 (compound 22) is an orally active, selective leucine-rich repeat protein kinase 2 (LRRK2) inhibitor with blood-brain barrier permeability, inhibiting GS LRRK2 (IC50: 4.6 μM) and WT LRRK2 (IC50: 49 μM). LRRK2-IN-6 exhibited inhibitory effects on the autophosphorylation of LRRK2 at Ser1292 and Ser925.

LRRK2-IN-5 (compound 25) is an orally active, blood-brain barrier-penetrating, selective leucine-rich repeat protein kinase 2 (LRRK2) inhibitor, effective for GS LRRK2 (IC50: 1.2 μM) and WT LRRK2 (IC50: 16 μM), and can inhibit the autophosphorylation of LRRK2 at Ser1292 and Ser925.

LRRK2-IN-3 is a potent, selective, orally active LRRK2 inhibitor that crosses the blood-brain barrier with an IC50 value of 0.6 nM in hPBMCs. LRRK2-IN-3 can be used to study Parkinson's disease.

LRRK2-IN-4 is a potent, selective, orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor that crosses the blood-brain barrier with an IC50 value of 2.6 nM. LRRK2-IN-3 has shown investigational potential in [Parkinson's disease].

LRRK2-IN-2 is a selective, potent, and orally active LRRK2 inhibitor (IC50: 0.6 nM) that crosses the blood-brain barrier. LRRK2-IN-2 can be used to study Parkinson's disease.

LRRK2/NUAK1/TYK2-IN-1 (compound 226) exhibits inhibitory activity against LRRK2 (Wt), LRRK2 (G2019), TYK2, and NUAK1, demonstrating IC50 values below 10 nM. This compound is useful for research into autoimmune diseases.

LRRK2-IN-10 (compound 34) is a potent, mutation-selective, brain-penetrant inhibitor targeting G2019S-LRRK2 kinase with IC50 values of 11 nM for G2019S-LRRK2 pS935 and 5.2 nM for G2019S-LRRK2 pS1292, holding promise for research into Parkinson's disease [1].

N-myristoyl-RKRTLRRL is a compound that impedes the binding of protein kinase C (PKC) substrates and inhibits calcium (Ca2+)- and phosphatidylserine (PS)-dependent phosphorylation of histones, exhibiting an IC50 of 5 μM. Additionally, it demonstrates an inhibitory effect on histone phosphorylation with an IC50 of 80 μM [1] [2].

HSDAVFTDNYTRLRRQLAVRRYLNSILN-NH2 is a peptide with anti-inflammatory properties [1].

The compound AVSEHQLLHDKGKSIQDLRRRFFLHHLI-{Aib}-EIHTAYRFGG facilitates bone ossification and has potential applications in the study of conditions associated with osteogenic insufficiency or diminished bone mineral density (BMD), including osteoporosis [1].

LRRKtide, a peptide substrate for leucine-rich repeat kinase 2 (LRRK2)—an enzyme often mutated in Parkinson's disease patients—corresponds to amino acids 550-564 of the membrane-organizing extension spike protein (moesin). It serves to identify inhibitors of LRRK2.

LRRK2-IN-12 (compound 1) is a potent inhibitor of LRRK2 (G20195) with an IC 50 of 0.45 nM, LRRK2 WT with an IC 50 of 1.1 nM, and LRRK2 WT ADP-Glo with an IC 50 of 0.46 nM. This compound is utilized in research related to Alzheimer's Disease [1].

LRRK2-IN-13 (Compound 13), with an IC50 value of 0.57 nM, serves as an inhibitor of LRRK2 and exhibits properties that allow it to penetrate the brain [1].