Activators & Inhibitors

PNU 142300 (Legacy Tebubio ref. 282T37841). PNU 142300 is an inactive metabolite of the oxazolidinone antibiotic linezolid .

ASB 14780 (Legacy Tebubio ref. 282T37842). Potent and selective cytosolic phospholipase A2 alpha (cPLA2α) inhibitor (IC50 = 20 nM). Selective for cPLA2α over secreted PLA2α (sPLA2α; exhibits no inhibition at 10 μM). Inhibits cPLA2α-dependent inflammatory responses in vitro in guinea pig and human whole-blood assays. Improves diet-induced liver injury and CCl4-induced hepatic fibrosis in vivo. Orally bioavailable.

Australine (hydrochloride) (Legacy Tebubio ref. 282T37843). Australine is a pyrrolizidine alkaloid originally isolated fromC. australethat has enzyme inhibitory activities.1,2,3It is an inhibitor of glucoamylase (IC50= 5.8 μM) that also inhibits glucosidase I, sucrase, maltase, andA. nigerα-glucosidase (IC50s = 20, 28, 35, and 28 μM, respectively).2,3Australine is selective for these enzymes over glucosidase II, α- and β-mannosidase, and α- and β-galactosidase up to 500 μM, β-glucosidase, with only 5% inhibition at 66 μM, as well as isomaltase and trehalase (IC50= 97 and 160 μM, respectively). Australine (500 μg/ml) inhibits glycoprotein processing of viral glycoproteins in influenza virus-infected MDCK cells and induces the accumulation of glycoproteins.2

Kigamicin C (Legacy Tebubio ref. 282T37844). Kigamicins are natural antitumor antibiotics that selectively kill pancreatic cancer PANC-1 cells only under nutrient-starved conditions. They also show antimicrobial activity against Gram-positive bacteria, including methicillin-resistant S. aureus. Kigamicin C inhibits PANC-1 cell survival in nutrient-deprived media at a 100-fold lower concentration than that required for cells maintained in nutrient-rich media. A related compound, kigamicin D, is active in vivo, suppressing the tumor growth of several pancreatic cancer cell lines in nude mice. It blocks the activation of Akt induced in PANC-1 cells placed in nutrient-deprived media. Kigamicin can also induce necrosis in human myeloma cells, but not normal lymphocytes, maintained in nutrient-rich media (CC50 = 100 nM).

3-Sulfo-taurocholic acid disodium salt (Legacy Tebubio ref. 282T37845). 3-Sulfo-taurocholic acid disodium salt (3-Sulfocholyl Taurine disodium salt) is a derivative of bile acid taurocholic acid.

Taurohyocholic Acid (Legacy Tebubio ref. 282T37846). Taurohyocholic acid (THCA) is a taurine-conjugated form of the porcine-specific primary bile acid hyocholic acid .1THCA inhibits precipitation of cholesterol crystals by stabilizing cholesterol in the liquid-crystalline phase.2It prevents cholestasis and cellular necrosis induced by taurolithocholic acid in isolated rat livers.3THCA levels are increased in the urine of patients with hepatitis B-induced cirrhosis.4

Zonisamide-13C2,15N (Legacy Tebubio ref. 282T37847). Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (40 mg/kg, p.o.) prevents MPTP-induced decreases in the level

Brombuterol hydrochloride (Legacy Tebubio ref. 282T37848). Brombuterol is an agonist of the β2-adrenergic receptor (β2-AR).1It has been used as an illicit feed additive to increase the muscle-to-fat ratio of livestock.

Butafosfan (Legacy Tebubio ref. 282T37849). Butafosfan is an organic phosphorus supplement that is given, most commonly with cyanocobalamin, to cattle, swine, horses, and poultry for the prevention or treatment of deficiencies. When given with cyanocobalamin, butafosfan alters lipid metabolism, serving to decrease the prevalence of subclinical ketosis.