Vergleich

LRRK2-IN-1

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mM/1mL
ArtNr HY-10875-10mM
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
CAS
1234480-84-2
MWt
570.69
Formula
C31H38N8O3
Solubility
DMSO : >= 50 mg/mL (87.61 mM)
Clinical Information
No Development Reported
Research Area
Neurological Disease, Cancer
Pathway
Apoptosis, Autophagy
Target
Apoptosis, LRRK2
SMILES
O=C(C1=CC(OC)=C(NC2=NC=C3C(N(C4=C(C(N3C)=O)C=CC=C4)C)=N2)C=C1)N5CCC(CC5)N6CCN(CC6)C
Biological Activity
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.
IC50 & Target: IC50: 13 nM (WT), 6 nM (G2019S)
In Vitro: Wild-type and G2019S transduction results in 2.5 fold higher TR-FRET signal which can be inhibited by LRRK2-IN-1 in a dose-dependent manner with IC50 values of 0.08 uM and 0.03 uM, respectively[1]. LRRK2-IN-1 possessed an IC50 of 45 nM for inhibition of DCLK2 and exhibits an IC50 of greater than 1 uM when evaluated in biochemical assays for AURKB, CHEK2, MKNK2, MYLK, NUAK1, and PLK1. LRRK2-IN-1 is confirmed to inhibit MAPK7 with an EC50 of 160 nM. LRRK2-IN-1 induces a dose dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells[2]. LRRK2-IN-1 is moderately cytotoxic with IC50 of 49.3 uM in HepG2 cells. LRRK2-IN-1 exhibits genotoxicity in the presence and absence of S9 at 15.6 and 3.9 uM, respectively[3]. LRRK2-IN-1 inhibits proliferation, migration, and induces cell death with hallmarks of apoptosis of HCT116 and AsPC-1 cells[4].
In Vivo: LRRK2-IN-1 (100 mg/kg, i.p.) induces dephosphorylation of LRRK2 in the kidney of the mice[2]. Peritumoral injection of LRRK2-IN-1 (100 mg/kg) results in a significant decrease in tumor volume and weight of AsPC-1 tumor xenografts[4].

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Menge: 10mM/1mL
Lieferbar: In stock
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