LRRK2-IN-21
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.
For research use only. We do not sell to patients.
- CAS No.: 3018825-60-7
- Formula: C17H19F3N6O2
- Molecular Weight:396.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
LRRK2-IN-21 (Compound 12) inhibits LRRK2 Ser935 dephosphorylation in unbound primary human PBMCs with an IC50 of 40 nM[1].
LRRK2-IN-21 exhibits high metabolic stability in rat, dog, and human hepatocytes with intrinsic clearance values of 26, <14, and <6 mL/min/kg respectively[1].
LRRK2-IN-21 inhibits hERG channels with an IC50 of 30 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
Chemical Information
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CAS No. 3018825-60-7
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Molecular Weight 396.37
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Formula C17H19F3N6O2
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SMILES
CC1=NN(C(N2)=C1OC[C@@H]3COC[C@H]3NC4=NC2=NC=C4C(F)(F)F)C5CC5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LRRK2-IN-21 Related Classifications
HY-182928 Related Classifications
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