KLK6-IN-1 

KLK6-IN-1 is a reversible small‑molecule inhibitor of KLK6, KLK1, and plasmin. KLK6-IN-1 shows IC₅₀ values of 1.57 μM (KLK6), 5.1 μM (KLK1), 7.4 μM (plasmin), and K_i values of 0.8 μM (KLK6), 2.4 μM (KLK1), 1.3 μM (plasmin). KLK6-IN-1 is highly selective for KLK6 and its proteolytic network. KLK6-IN-1 induces oligodendrocyte differentiation by promoting oligodendrocyte precursor cell maturation. KLK6-IN-1 can be used for the research of multiple sclerosis^[1].

KLK6-IN-1 (compound 42) noncompetitively and reversibly inhibits purified KLK6 with an IC₅₀ of 1.57 μM and a K_i of 0.8 μM, while competitively and reversibly inhibiting purified plasmin and KLK1 with IC₅₀ values of 7.4 μM (K_i = 1.3 μM) and 5.1 μM (K_i = 2.4 μM), respectively^[1].
KLK6-IN-1 (10 μM; 15 min preincubation, enzymatic reaction at 37 °C) displays high selectivity for KLK6, KLK1, and plasmin, with minimal inhibition of most tested CNS-related proteases^[1].
KLK6-IN-1 (10-100 μM; 24 h) is noncytotoxic to both primary mouse cortical and striatal neurons at concentrations up to 25 μM, and exhibits only mild cytotoxicity at 50 μM and above^[1].
KLK6-IN-1 (5 μM; 4 days) significantly promotes the differentiation of both CG4 and primary rat oligodendrocyte precursor cells into mature oligodendrocytes^[1].
KLK6-IN-1 (0.5-1.5 μM; 24 h, combined with 10 ng/mL LPS) significantly reduces LPS-induced IL-1β and TNFα secretion from primary rat microglial cultures after 24 h of treatment^[1].

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

328.79

C₁₈H₁₇ClN₂O₂

2370980-52-0

O=C(C1=CC2=C(C=C1O)C=CC=C2)NC3=CC=C(CN)C=C3.Cl

Room temperature in continental US; may vary elsewhere.

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

• [1]. Aït Amiri S, et al. Identification of First-in-Class Inhibitors of Kallikrein-Related Peptidase 6 That Promote Oligodendrocyte Differentiation. J Med Chem. 2021;64(9):5667-5688.