LRRK2-IN-1 | B2940

LRRK2-IN-1 is a potent inhibitor of Leucine-rich repeat kinase 2 (LRRK2). Mutations in LRRK2 are associated with Parkinson's disease. LRRK2-IN-1 inhibits wild-type and G2019S mutant LRRK2 with IC₅₀ values of 13 nM and 6 nM, respectively. It suppresses LRRK2 kinase activity in vivo leading to dephosphorylation of Ser910/Ser935, loss of 14-3-3 binding and accumulation of LRRK2 within aggregate structures. It stimulates autophagy in H4 neuroglioma cells.

LRRK2-IN-1 is a potent inhibitor of Leucine-rich repeat kinase 2 (LRRK2). Mutations in LRRK2 are associated with Parkinson's disease. LRRK2-IN-1 inhibits wild-type and G2019S mutant LRRK2 with IC₅₀ values of 13 nM and 6 nM, respectively. It suppresses LRRK2 kinase activity in vivo leading to dephosphorylation of Ser910/Ser935, loss of 14-3-3 binding and accumulation of LRRK2 within aggregate structures. It stimulates autophagy in H4 neuroglioma cells.

B2940 | LRRK2-IN-1 DataSheet

Alternate Name/Synonyms: 5,11-dihydro-2-[[2-methoxy-4-[[4-(4-methyl-1-piperazinyl)- 1-piperidinyl]carbonyl] phenyl]amino]- 5,11-dimethyl-6H-pyrimido[4,5-b][1,4] benzodiazepin-6-one; 2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one; Leucine-rich repeat kinase 2 IN-1; LRRK2IN1

Appearance: A crystalline solid

Formulation:

CAS Number: 1234480-84-2

Structure Available?: True

Peptide sequence:

Salt Form: false

Molecular Formula: C₃₁H₃₈N₈O₃

Molecular Weight: 570.69

Cell-Permeable?: True

Purity: 99.38%

Solubilities: ~25 mg/ml in in Ethanol, ~20 mg/ml in DMF in 0, ~16 mg/ml in in DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: An inhibitor of LRRK2

MDL Number:

PubChem CID: 46843906

SMILES: CN1CCN(CC1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)NC4=NC=C5C(=N4)N(C6=CC=CC=C6C(=O)N5C)C)OC

InChi: InChI=1S/C31H38N8O3/c1-35-15-17-38(18-16-35)22-11-13-39(14-12-22)29(40)21-9-10-24(27(19-21)42-4)33-31-32-20-26-28(34-31)36(2)25-8-6-5-7-23(25)30(41)37(26)3/h5-10,19-20,22H,11-18H2,1-4H3,(H,32,33,34)

InChi Key: IWMCPJZTADUIFX-UHFFFAOYSA-N