Description
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.
Product information
Molecular Weight: 240.26
Formula: C12H12N6
Chemical Name: N, N-dimethyl-4-(pyrazolo[1, 5-b]pyridazin-3-yl)pyrimidin-2-amine
Smiles: CN(C)C1=NC(=CC=N1)C1C=NN2N=CC=CC2=1
InChiKey: IFLBFWBMAWIBBZ-UHFFFAOYSA-N
InChi: InChI=1S/C12H12N6/c1-17(2)12-13-7-5-10(16-12)9-8-15-18-11(9)4-3-6-14-18/h3-8H,1-2H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 inhibits tau phosphorylation with an IC50 value of 0.59 μM. DYRK1-IN-1 exhibits good permeability and cellular activity without P-glycoprotein liability. DYRK1-IN-1 has good physicochemical properties and has demonstrated high levels of enzymatic potency, favorable aqueous solubility, exquisite kinome selectivity, and promising on-target in vitro inhibition. DYRK1-IN-1 (HEK293 cells) demonstrates acceptable cellular activity, with IC50 of 434 nM compared to the enzymatic IC50 of 75 nM.
In Vivo:
DYRK1-IN-1 (1 mg/kg; i.v.) shows high clearance.
Products are for research use only. Not for human use.
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