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 Ki 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.
For research use only. We do not sell to patients.
- CAS No.: 2370980-52-0
- Formula: C18H17ClN2O2
- Molecular Weight:328.79
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
KLK1 5.1 μM (IC50) |
KLK1 2.4 μM (IC50) |
In Vitro
KLK6-IN-1 (compound 42) noncompetitively and reversibly inhibits purified KLK6 with an IC50 of 1.57 μM and a Ki of 0.8 μM, while competitively and reversibly inhibiting purified plasmin and KLK1 with IC50 values of 7.4 μM (Ki = 1.3 μM) and 5.1 μM (Ki = 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. Further protocols information, click here.
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Cell Line:primary mouse cortical neurons, primary mouse striatal neurons
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Concentration:10, 25, 50, 100 μM
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Incubation Time:24 h
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Result:Showed no significant cytotoxicity at 10 μM or 25 μM, with cell survival comparable to vehicle controls.
Reduced cell survival to ~65-70% of vehicle control at 50 μM and 100 μM.
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Cell Line:CG4 mCherry/GFP oligodendrocyte precursor cell line
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Concentration:1, 2, 3, 4, 5 μM
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Incubation Time:4 days
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Result:Increased the number of mature mCherry-positive oligodendrocytes significantly at 5 μM.
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Cell Line:primary rat oligodendrocyte precursor cell (OPC) cultures
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Concentration:5 μM
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Incubation Time:4 days
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Result:Induced a significant increase in the number of MBP-positive mature oligodendrocytes relative to N1-only controls.
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Cell Line:primary rat microglial cultures
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Concentration:0.5, 1.5, 5, 10 μM (combined with 10 ng/mL LPS)
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Incubation Time:24 h
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Result:Significantly reduced LPS-induced TNFα secretion relative to LPS-only controls at 0.5 μM.
Significantly reduced LPS-induced IL-1β secretion relative to LPS-only controls at 0.5 μM and 1.5 μM.
Chemical Information
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CAS No. 2370980-52-0
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Molecular Weight 328.79
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Formula C18H17ClN2O2
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SMILES
O=C(C1=CC2=C(C=C1O)C=CC=C2)NC3=CC=C(CN)C=C3.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)