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MARK-IN-2 

Cat. No.: HY-101934
Handling Instructions

MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 5 nM.

For research use only. We do not sell to patients.

MARK-IN-2 Chemical Structure

MARK-IN-2 Chemical Structure

CAS No. : 1314893-26-9

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Description

MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 5 nM.

IC50 & Target

IC50: 5 nM (MARK)[1]

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[1].

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) [1].

Molecular Weight

425.88

Formula

C₁₈H₁₈ClF₂N₅OS

CAS No.

1314893-26-9

SMILES

O=C(C1=CC(C2=C3N=CC(Cl)=CN3N=C2)=C(C)S1)N[[email protected]]4C(F)(F)CCC[[email protected]]4N

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Cell Assay
[1]

The cell biochemical potency of the below described MARK inhibitors (e.g., MARK-IN-2) is evaluated by measuring their ability to block the phosphorylation of Tau at S262 in primary cell culture of rat cortical neurons induced by the action of Okadaic acid[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rats[1]
Male Sprague-Dawley Rats are via a previously implanted venous catheter at 1 mL/kg and by gastric gavage at 5 mL/kg. Male Beagle Dogs are dosed via a saphenous vein indwelling catheter at 0.5 mL/kg and by gastric gavage at 5 mL/kg. Blood samples are collected into tubes containing EDTA at pre-dose and at 5 (intravenously administered drugs only), 15, and 30 min and 1, 2, 4, 6, 8, 12, and 24 h after drug administration. After sampling, whole blood is centrifuged at 14,000 rpm for 5 min, and plasma was stored frozen at -20ºC until the day of analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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