General
Preferred name
leucettine L41
Synonyms
LeucettineL41 ()
PMID28766366-Compound-Scheme27LeucettineL41 ()
P&D ID
PD048165
CAS
1112978-84-3
Tags
drug candidate
available
Drug indication
Discovery agent
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 ¦ÌM, respectively)[1]. Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by A¦Â25-35 in the hippocampus in a mouse model of Alzheimer¡¯s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by A¦Â25-35 in the same model[2].
PRICE 238
DESCRIPTION Leucettine L41 is a synthetic analogue of the marine sponge derived compound leucettine B . The leucettines act as inhibitors of two families of serine/threonine kinases; dual-specificity, tyrosine phosphorylation-regulated kinases (DYRKs), and cdc2-like kinases (CLKs), which are involved in Alzheimer’sdisease/Down syndrome and in the control of alternative pre-mRNA splicing. (GtoPdb)
DESCRIPTION Leucettine L41 (LeucettineL41) is a selective DYRK1A inhibitor that inhibits DYRK2, CLK1, and CLK3, inducing autophagy linked to CLK inhibition. It is used to study Alzheimer's disease and memory deficits. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
9
Cayman Chemical Bioactives
29225
DrugMAP
DMLX26R
DMBYND6
EUbOPEN Chemogenomics Library
EUB0001025
Guide to Pharmacology
8167
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1802358
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1802358
MedChem Express Bioactive Compound Library
HY-117049
Novartis Chemogenetic Library (NIBR MoA Box)
TargetMol Bioactive Compound Library
T24402
External IDs
18
Properties
(calculated by RDKit )
Molecular Weight
307.1
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
4
Aromatic Ring Count
2
cLogP
2.35
TPSA
71.95
Fraction CSP3
0.06
Chiral centers
0.0
Largest ring
6.0
QED
0.84
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
CDK
DYRK
DYRK1A
DYRK2
CLK1
Member status
member
MOA
CLK1 protein kinase inhibitor
Pathway
Cell Cycle/DNA Damage
Protein Tyrosine Kinase/RTK
Cell Cycle/Checkpoint
Tyrosine Kinase/Adaptors
Recommended Cell Concentration
1 uM
Source data