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GSK951

GSK951 is a potent and selective Kallikrein-5 (KLK5) inhibitor amenable to epidermal delivery. GSK951 shows an IC50 of 250 pM for KLK5 and greater than 100-fold selectivity over KLK7 and KLK14. GSK951 can reduce transepidermal water loss, and decrease proinflammatory cytokine expression. GSK951 can be used for the researches of inflammation and immunology, such as Netherton syndrome[1].

Product Specifications

CAS Number

[2393881-77-9]

UNSPSC

12352005

Target

Kallikrein

Related Pathways

Immunology/Inflammation

Field of Research

Inflammation/Immunology

Smiles

OB1C2=CC(C(F)(F)F)=CC=C2C[C@@](C3=CC(OCC4=CN=CC=C4)=C(C=C3)C(N)=N)([H])O1

Molecular Formula

C22H19BF3N3O3

Molecular Weight

441.21

References & Citations

[1]Liddle J, et al. A Potent and Selective Kallikrein-5 Inhibitor Delivers High Pharmacological Activity in Skin from Patients with Netherton Syndrome. J Invest Dermatol. 2021 Sep;141 (9) :2272-2279.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

KLK5

Curated Selection

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