2393881-77-9
Chemical Structure
GSK951
- CAS No.: 2393881-77-9
- Formula:C22H19BF3N3O3
- Molecular Weight:441.21
IUPAC Name: potassium 6-amino-2-(5-(2-ammonio-6-((4-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)butyl)amino)hexanamido)pentyl)-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinoline-5,8-disulfonate
InChIKey: NWAGTUQRZPXSNY-LJQANCHMSA-N
SMILES: OB1C2=CC(C(F)(F)F)=CC=C2C[C@@](C3=CC(OCC4=CN=CC=C4)=C(C=C3)C(N)=N)([H])O1
Biological Activity: 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.
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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. | |||||||||||||||||||||
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Keywords
