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-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].

LRRK2-IN-14 (Compound 8), an orally active inhibitor of LRRK2, exhibits an IC 50 of 6.3 nM against LRRK2(G2019S) cell activity and demonstrates inhibitory effects on hERG with an IC 50 of 22 μM. Additionally, LRRK2-IN-14 is permeable to the blood-brain barrier [1].

LRRKtide serves as a substrate for LRRK kinase.