MK 1256

MK 1256 is a highly selective and orally active inhibitor of tissue protease K (Cat K) with an IC50 of 0.62 nM. MK 1256 shows extremely high selectivity towards other tissue proteases (all > 1100 times), with only a slightly lower selectivity for tissue protease F (Cat F) (110 times) . MK 1256 exhibits strong anti-bone resorption activity in the osteoporosis model of rhesus monkeys with ovariectomy. MK 1256 can be used for research on osteoporosis[1].

Product Specifications

CAS Number

[919109-76-5]

UNSPSC

12352005

Target

Cathepsin

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Smiles

O=C([C@H]1[C@H](C2=NN(CC(F)(F)F)C=C2C3=CC=C(S(=O)(C)=O)C=C3)CCC(Cl)(Cl)C1)NC4(C#N)CC4

Molecular Formula

C23H23Cl2F3N4O3S

Molecular Weight

563.42

References & Citations

[1]Robichaud J, et al. Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis. J Med Chem. 2008 Oct 23;51 (20) :6410-20.