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.
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- CAS. Nr.: 2370980-52-0
- Formel: C18H17ClN2O2
- Molecular Weight:328.79
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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KLK1 5.1 μM (IC50) |
KLK1 2.4 μM (IC50) |
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.
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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. Nr. 2370980-52-0
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Molecular Weight 328.79
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)