Activators & Inhibitors

ABT 702 hydrochloride (Legacy Tebubio ref. 282T38346). Potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase). Displays oral activity in animal models of pain and inflammation.

Zelkovamycin (Legacy Tebubio ref. 282T38347). Zelkovamycin is a cyclic peptide antibiotic isolated from Streptomyces, known to inhibit growth of X. oryzae, P. oryzae, S. aureus, and A. laidlawii in a concentration-dependent manner at concentrations ranging from 0.01 to 300 μg/ml.

α-Lipomycin (Legacy Tebubio ref. 282T38348). α-Lipomycin, an acyclic polyene antibiotic, is isolated from the Gram-positive bacterium Streptomyces aureofaciens Tü117.

Talaromycesone A (Legacy Tebubio ref. 282T38349). Talaromycesone A is a fungal metabolite originally isolated fromTalaromyces.1It is active againstS. epidermidisand methicillin-resistantS. aureus(MRSA) bacteria (IC50s = 3.70 and 5.48 μM, respectively). Talaromycesone A inhibits acetylcholinesterase (AChE) in a cell-free assay (IC50= 7.49 μM for the human enzyme).

1-(3,4-Dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane-3,5-diyl diacetate (Legacy Tebubio ref. 282T3835). 1-(3,4-Dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane-3,5-diyl diacetate is a natural product for research related to life sciences. The catalog number is T3835 and the CAS number is 1269839-26-0.

TAS 205 (Legacy Tebubio ref. 282T38350). TAS 205 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS; IC50= 55.8 nM).1It is selective for H-PGDS over lipocalin-type PGDS (L-PGDS) at 100 μM, as well as over enzyme and receptor panels at 10 μM. TAS 205 inhibits production of prostaglandin D2induced by A23187 in KU812 human and RBL-2H3 rat basophils with IC50values of 78.3 and 181.3 nM, respectively. It inhibits ovalbumin-induced nasal lavage fluid eosinophil infiltration and late-phase nasal obstruction in an ovalbumin-sensitized guinea pig model of allergic rhinitis when administered at a dose of 30 mg/kg.

DYn-2 (Legacy Tebubio ref. 282T38351). Mild oxidation can convert the sulfhydryl group of cysteine residues on proteins to cysteine-sulfenic acid derivatives (Cys-SOH). Protein sulfenylation, then, is a post-translational modification that is relevant to redox signaling. DYn-2 is a chemoselective probe for detecting sulfenylated proteins in intact cells. DYn-2 consists of 1,3-cyclohexanedione coupled to an alkyne moiety by a 3-carbon spacer. The cyclohexanedione group selectively reacts with protein sulfenic acid modifications. The alkyne group of DYn-2 can then be detected using azide-bearing tags by standard click chemistry. This approach offers superior sensitivity relative to using azide-modified probes with alkynyl detection tags.

Ebelactone A (Legacy Tebubio ref. 282T38352). Ebelactone A is a β-lactone enzyme inhibitor that was first isolated from a cultured strain of soil actinomycetes. It can inhibit esterases, lipases, and N-formylmethionine aminopeptidases (IC50s = 0.056, 0.003, and 0.08 μg/ml, respectively) found on cell surfaces, which has been shown to stimulate host defense in immune cells. Ebelactone A is also reported to inhibit cutinases produced by fungal pathogens, thus demonstrating a plant-protective function.

Pyrenocine A (Legacy Tebubio ref. 282T38353). Pyrenocine A is a fungal metabolite that has been found inP. terrestrisand has diverse biological activities.1It inhibits the asexual spore germination of the plant pathogenic fungiF. oxysporum,F. solani,M. hiemalis, andR. stolonifer(EC50s = 14, 20, 20, and 25 μg/ml, respectively). Pyrenocine A is active againstB. subtilis,S. aureus, andE. coli(IC50s = 30, 45, and 200 μg/ml, respectively). It inhibits onion seedling elongation (EC50= 4 μg/ml). Pyrenocine A is also a phytotoxin that inhibits lettuce seed germination and rice seedling elongation.2,3