MARK-IN-2


Catalog No. Size PriceQuantity
M33356-C Contact sales@xcessbio.com for quotation $100Unavailable

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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