Cathepsin K inhibitor 2 是一种 cathepsin K 的有效抑制剂。其中 Cathepsin K (Cat K) 是一种半胱氨酸蛋白酶,在 CTSK 基因调控下表达,与骨质疏松症密切相关,能够水解胶原蛋白。Cathepsin K inhibitor 2 对骨关节炎表现出研究潜力。
Acyline is a novel GnRH antagonist found in animal studies to be a potent suppressor of circulating gonadotropin and testosterone (T) levels. Acyline inhibits basal and GnRH-stimulated serum testosterone concentrations in male dogs. Acyline prevented ovulation, but did not affect ovarian follicular development or gestational corpora lutea in the domestic cat. A single dose of the potent gonadotropin-releasing hormone antagonist acyline suppresses gonadotropins and testosterone for 2 weeks in healthy young men.
Prostaglandin F2α ethanolamide (PGF2α-EA) is produced by COX-2 metabolism of the endogenous cannabinoid, arachidonoyl ethanolamide (AEA), found in brain, liver, and other mammalian tissues. AEA can be metabolized directly by the sequential action of COX-2 and specific PG synthases to produce ethanolamide congeners of the classical PGs. PGF2α-EA has also been reported to be biosynthesized by this mechanism when AEA was infused into the lung and liver of living mice. PGF2α-EA is a potent dilator (EC50 = 58 nM) of the cat iris sphincter, which is a model system for testing potential intraocular hypotensive agents.
Potent inhibitor of CDK16 and CDK14 (IC50 values are 6 and 140 nM, respectively in kinase activity assay; IC50 = 563 nM for CDK14 in BRET assay). Also binds CDK2 (IC50 = 493 nM). Inhibition reversible upon compound wash-out. Control for FMF-04-159-2 (Cat. No. 7158).
Fluorescently labelled peptide derived from human ACE2 (SBP1, Cat. No. 7233). Composed of SBP1 conjugated to FITC (Fluorescein-5-isothiocyanate; Cat. No. 5440). SBP1 binds receptor binding domain (RBD) of insect-derived SARS-CoV-2 spike protein (KD = 1.3 μM for N-terminal biotinylated, insect-derived spike protein RBD; see Zhang et al preprint publication). Please note - unpublished, in-house data suggests SBP1 has approximately 75-fold lower affinity for insect-derived SARS-CoV-2 RBD than reported by Zhang et al.