Description
MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 5 nM.
Product information
CAS Number: 1314893-26-9
Molecular Weight: 425.88
Formula: C18H18ClF2N5OS
Chemical Name: N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-4-{6-chloropyrazolo[1,5-a]pyrimidin-3-yl}-5-methylthiophene-2-carboxamide
Smiles: CC1SC(=CC=1C1C=NN2C=C(Cl)C=NC2=1)C(=O)N[C@@H]1[C@H](N)CCCC1(F)F
InChiKey: NGFGTMFVWSDFPS-UKRRQHHQSA-N
InChi: InChI=1S/C18H18ClF2N5OS/c1-9-11(12-7-24-26-8-10(19)6-23-16(12)26)5-14(28-9)17(27)25-15-13(22)3-2-4-18(15,20)21/h5-8,13,15H,2-4,22H2,1H3,(H,25,27)/t13-,15-/m1/s1
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:
MARK-IN-2 (Compound 27) is a potent MARK inhibitor. Inhibition of MARK represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease. MARK-IN-2 inhibits MARK3 with an IC50 of 5 nM. MARK-IN-2 also inhibits MARK3 in primary cell culture of rat cortical neurons with an IC50 of 280 nM.
In Vivo:
Characterization of the i.v. pharmacokinetic properties of MARK-IN-2 in rat and dog reveals reasonable volumes of distribution but moderate to high clearance and short half-lives. MARK-IN-2 (Compound 27) has moderate terminal elimination half-life (t1/2=0.7 h, and 1 h for rat and dog) .
Products are for research use only. Not for human use.
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