GSK951
GSK951 is a highly potent, selective, and reversibly covalent KLK5 inhibitor, with an IC50 of approximately 250 pM and a pIC50 of 9.6 against hKLK5. It exhibits over 100-fold selectivity over KLK7, KLK14, matriptase, and elastase. GSK951 binds to the catalytic site of KLK5 via covalent interaction with the catalytic serine, with a slow dissociation rate. GSK951 improves skin barrier function, reduces transepidermal water loss, decreases the expression of proinflammatory cytokines, and inhibits the elevated KLK5 protease activity in the stratum corneum. GSK951 can be used in studies related to skin barrier dysfunction.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2393881-77-9
- 分子式: C22H19BF3N3O3
- 分子量:441.21
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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KLK5 250 pM (IC50) |
KLK5 9.6 (pIC50) |
KLK7 4.1 (pIC50) |
KLK14 7.5 (pIC50) |
matriptase 5.9 (Kd) |
GSK951 potently and selectively inhibits human KLK5 with an IC50 of 250 pM. It forms key catalytic site interactions with KLK5 orthologs and exhibits over 100-fold selectivity against related skin serine proteases[1].
GSK951 (0.3% w/w cream formulation; 16 h) reaches a high average concentration of 471 μM in the epidermis of ex vivo healthy human skin after 16 hours[1].
GSK951 exhibits over 100-fold selectivity for KLK5 over KLK7, KLK14, matriptase, and elastase, with pIC50 values of 4.1, 7.5, 5.9, and <4, respectively, against these counter-targets[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hemizygous transgenic human KLK5 (Tg-KLK5) mice[1]
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Dosage:0.3% w/w (KLK5 activity inhibition); 0.3% w/w (TEWL); 0.3% w/w (proinflammatory cytokine expression)
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Administration:topical; single dose; 3 hours (KLK5 activity inhibition); topical; twice daily; 3 days (TEWL); topical; twice daily; 21 days (proinflammatory cytokine expression)
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Result:Significantly reduced KLK5-dependent fluorescent signal in the stratum corneum relative to vehicle.
Reduced transepidermal water loss by approximately 50% within 24 hours of the first dose and maintained this reduction throughout the dosing period relative to vehicle.
Significantly reduced mRNA expression of proinflammatory mediators: IL-17A, IL-17F, S100A8, and S100A9 relative to vehicle.
化学情報
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CAS 番号 2393881-77-9
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分子量 441.21
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分子式 C22H19BF3N3O3
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SMILES
OB1C2=CC(C(F)(F)F)=CC=C2C[C@@](C3=CC(OCC4=CN=CC=C4)=C(C=C3)C(N)=N)([H])O1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
GSK951 関連分類
HY-150085 関連分類
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