KLK5-IN-1
KLK5-IN-1 is a selective kallikrein 5 (KLK5) inhibitor with an IC50 of 14 nM and a Ki of 11 nM. KLK5-IN-1 reduces KLK5-mediated PAR2-dependent calcium mobilization. KLK5-IN-1 improves epithelial barrier integrity. KLK5-IN-1 can be used in research related to atopic dermatitis and Netherton syndrome.
For research use only. We do not sell to patients.
- Formula: C69H96N20O21S2
- Molecular Weight:1605.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
KLK5 14 nM (IC50) |
PAR2 |
In Vitro
KLK5-IN-1 (Compound 7) potently and selectively inhibits purified KLK5 with an IC50 of 14 nM and a Ki of 11 nM, with no activity against KLK7, KLK8, or KLK14 at concentrations above 1 μM[1].
KLK5-IN-1 (2.5-40 μM; 1 h) dose-dependently inhibits rKLK5-mediated PAR2 activation in N/TERT keratinocytes, with complete inhibition observed at 10 μM[1].
KLK5-IN-1 (100 nM-10 μM) dose-dependently inhibits elevated endogenous KLK5 activity in NS keratinocytes but has no significant effect on KLK5 activity in healthy donor keratinocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Molecular Weight 1605.75
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Formula C69H96N20O21S2
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Sequence
cyclo(Gly-Phe-Cys-Thr-Arg-Ser-Asn-Pro-Pro-Glu-Cys-Trp-Pro-Asn) (Disulfide bridge: Cys3-Cys11)
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Sequence Shortening
cyclo(GFCTRSNPPECWPN) (Disulfide bridge: Cys3-Cys11)
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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.
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TPA/Croton Oil Ear Edema and Dermatitis
The TPA (12-O-tetradecanoylphorbol-13-acetate) and croton oil-induced mouse ear edema model is a well-established acute cutaneous inflammation system used to evaluate topical anti-inflammatory activity by measuring edema formation, neutrophil infiltration, vascular permeability, and cytokine-mediated skin responses in vivo. The inflammatory response is triggered by topical application of phorbol esters (TPA) or croton oil constituents, leading to rapid activation of protein kinase C signaling, leukocyte recruitment, and increased vascular permeability, which can be quantified by ear thickness, weight, dye extravasation, and biochemical markers such as myeloperoxidase (MPO) activity and pro-inflammatory mediators in ear tissue homogenates. This model is widely used for screening anti-inflammatory agents, where reductions in edema and inflammatory biomarkers reflect suppression of acute dermal inflammation and immune cell infiltration. Histological evaluation typically confirms epidermal
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)