Eniluracil (also known as 5-Ethynyluracil; GW776C85) is a novel and potent uracil analog and also a mechanism-based irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), which increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity.

Talampanel (also known as LY300164; LY-300164 and GYKI-53773) is a novel, potent, orally bioavailable and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity. It is also a glutamate receptor inhibitor. Talampanel (IVAX) has neuroprotective effects in rodent stroke models. Talampanel attenuates caspase-3 dependent apoptosis in mouse brain. Talampanel (GYKI 53405) was being investigated for the […]

Fenazaquin (EL-436; XDE-436) is a quinazoline-based insecticide/acaricide which exhibits contact and ovicidal activity against a broad spectrum of mites in grapes, pome fruit, citrus, peaches, cucurbits, tomatoes, cotton and ornamentals. It is a new acaricide, was determined in field trials in the UK to be as effective against Panonychus ulmi on apple at 100 and […]

RETV804M inhibitor is a novel, potent and selective RET/KDR inhibitor with IC50 of 7 nM. Reference: ACS Med Chem Lett . 2020 Feb 28;11(4):497-505 (compound 5).

Ochratoxin A (OTA) is a natural and nephrotoxic mycotoxin extracted from several fungal species such as Aspergillus ochraceus, A. carbonarius, A. niger and Penicillium verrucosum. It acts as an inhibitor of phenylalanyl-tRNA synthetases Reference: [1]. Crockett SL, et al. Role of dopamine and selective dopamine receptor agonists on mouse ductus arteriosus tone and responsiveness. Pediatr […]

SJA710-6 (a Hepatic Differentiation Inducer) is a novel, potent and cell-permeable small molecule imidazopyridinamine compound that is able to induce the differentiation of rat MSCs (rMSCs) toward hepatocyte-like cells (~47% at 5 µM).in vitro, where rMSCs treated with SJA710-6 have typical morphological and functional characteristics of hepatic cells, including glycogen storage, urea secretion, uptake of […]

Isocanadine is an isomer of canadine. Canadine which is also known as tetrahydroberberine and xanthopuccine and is a benzylisoquinoline alkaloid (BIA), of the protoberberine subgroup, and is present in many plants from the family Papaveraceae, such as Corydalis yanhusuo and C. turtschaninovii.

Debrisoquine sulfate (Ro5-3307; Debrisochinum; Tendor), the sulfate salt of Debrisoquin which is a guanidine derivative, is a potent antihypertensive and adrenergic neuron-blocking drug similar to guanethidine. Debrisoquine is commonly used as an indicator for phenotyping the drug metabolizing enzyme CYP2D6 enzyme.

Onalespib (formerly also known as AT13387; AT-13387) is an orally bioavailable small-molecule Hsp90 inhibitor (IC50 = 18 nM in A375 cells) with long-lasting anti-tumor activity. AT13387 selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated […]

EXP-3174 (also known as losartan aarboxylic acid), a physiologically active metabolite of losartan produced by cytochrome P450 isoforms in the liver, is a non-peptide, potent angiotensin II (AII) receptor, type 1 (AT1) antagonist, which inhibits the AII induced cellular responses. Like the parent compound losartan, EXP-3174 is a potent AT1 antagonist with Kis of 0.57 […]