GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM, 500-fold greater against a panel of 300 kinases.
IOX4 is a selective PHD2 inhibitor,IC50 With a value of 1.6 nM, HIFα expression is induced in cells and wild-type mice to permeate the blood-brain barrier. IOX4 competes with and displaces 2-oxoglutaric acid (2OG) at the PHD2 active site.
Indacaterol is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36.
Shogaol ([6]-Shogaol) is an active substance isolated from ginger and has a variety of biological activities, including anti-cancer, anti-inflammatory and antioxidant activities.
PF-4708671 is a novel cell-permeable inhibitor of S6K1 with Ki/IC50 value of 20 nM/160 nM. PF4708671 inhibits MSK1 (IC50 of 0.95 μM) 4-fold more weakly than S6K1.
Nisoxetine hydrochloride is a potent, selective norepinephrine transporter inhibitor (Ki = 5.1 nM).
13-Dehydroxyindaconitine is a natural alkaloid with antioxidant activity.
Methyl cinnamate (Methyl 3-phenylpropenoate) is an active ingredient in peppercorns and a versatile natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) has antibacterial activity and is a tyrosinase inhibitor that prevents browning of food.
TPT-260 dihydrochloride is a thiophene thiourea derivative with molecule weight 260.00 in free base form, there is no formal name yet.
Fluorescein diacetate (FDA), a fluorescent probe used for vital staining, is a fluorescently activated by esterolytic activity of human Pi-class glutathione S-transferase (hGSTP1) selectively among various cytosolic GSTs.
BMOV is a potent oral vanadium complex with anti-diabetic properties andinsulin-mimicking effects.BMOV is shown to improve cardiac dysfunctions in diabetic models.
SR8278 represents a unique chemical tool for probing REV-ERB function and may serve as a point for initiation of further optimization to develop REV-ERB antagonists with the ability to explore circadian and metabolic functions.