MK2-IN-1 (hydrochloride) Chemical Properties

storage temp. 

Inert atmosphere,Store in freezer, under -20°C

solubility 

insoluble in DMSO; ≥16.5 mg/mL in EtOH with ultrasonic; ≥37.4 mg/mL in H2O

form 

A crystalline solid

color 

Light yellow to pink

MK2-IN-1 (hydrochloride) Usage And Synthesis

Uses

MK2-IN-1 hydrochloride (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC50 of 0.11 uM for MK2 and an EC50 of 0.35 uM for pHSP27. MK2-IN-1 hydrochloride impaires the phosphorylation level of serine residues in the Tfcp2l1 protein[1][2].

Biological Activity

mk2 inhibitor iv is a highly selective and non-atp competitive mk2 inhibitor with ic50 value of 0.11 μm [1].map kinase-activated protein kinase 2 (mapkapk2 or mk2) is a member of the ser/thr protein kinase family and regulated through direct phosphorylation by p38 map kinase. activation of the p38/mk2 pathway involved in promoting pro-inflammatory cytokine production and related inflammatory diseases [1].mk2 inhibitor iv is a highly selective and non-atp competitive mk2 inhibitor. in a broad panel of 150 protein kinases, mk2 inhibitor iv only significantly inhibited ck1γ3 at greater than 50%. mk2 inhibitor iv also demonstrated no inhibition against a panel of cytochrome p450 (cyp) enzymes up to 30 μm. in the human thp1 acute monocytic leukemia cell line, mk2 inhibitor iv inhibited pro-inflammatory cytokine secretion. mk2 inhibitor iv also dose-dependently inhibited lps-stimulated tnfα and il6 secretion with ic50 values of 4.4 μm and 5.2 μm, respectively. in the sw1353 chondrosarcoma cell line and human primary chondrocyte cultures, mk2 inhibitor iv dose dependently inhibited il1β-stimulated matrixmetalloprotease (mmp)13 secretion with ic50 values of 5.7 μm and 2.2 μm, respectively.

References

[1]. huang x, shipps gw jr, cheng cc, et al. discovery and hit-to-lead optimization of non-atp competitive mk2 (mapkapk2) inhibitors. acs med chem lett. 2011 jun 24;2(8):632-7.