Activators & Inhibitors

(±)4(5)-EpDPA methyl ester (Legacy Tebubio ref. 282T37241). (±)4(5)-EpDPA methyl ester is a derivative of (±)4(5)-EpDPA which is stable enough to ship and handle routinely. The active free acid can be regenerated from the methyl ester by careful base hydrolysis. (±)4(5)EpDPA is a CYP450 metabolite of DHA which can be further metabolized to the diol metabolite. There are no published reports on the biological activity of (±)4(5)-EpDPA methyl ester at this time.

(±)5(6)-DiHETE (Legacy Tebubio ref. 282T37242). Eicosapentaenoic acid is an ω-3 polyunsaturated fatty acid that is abundant in marine organisms and fish oils. EPA is metabolized, in part, through cytochrome P450-catalyzed epoxidation followed by conversion to the vicinal diols by epoxide hydrolases. (±)5(6)-DiHETE is a possible metabolite produced from EPA following epoxidation of the α-5 double bond. The biological activity of (±)5(6)-DiHETE has not been documented.

(±)5(6)-DiHETE lactone (Legacy Tebubio ref. 282T37243). Eicosapentaenoic acid is metabolized, in part, through cytochrome P450-catalyzed epoxidation followed by conversion to the vicinal diols by epoxide hydrolases. (±)5(6)-DiHETE is a possible metabolite produced from EPA following epoxidation of the α-5 double bond. (±)5(6)-DiHETE lactone is a 1,5 cyclic ester derived from (±)5(6)-DiHETE. While its biological activity is unknown, the selective capacity of (±)5(6)-DiHETE to form this lactone can be utilized to specifically quantify (±)5(6)-DiHETE in biological samples.

Palmitoyl thio-PC (Legacy Tebubio ref. 282T37244). Thioester analogs of glycerophospholipids, in combination with Ellman's reagent, are convenient colorimetric substrates for the measurement of phospholipase (PL) activity. Palmitoyl thio-PC is a chromogenic PLA2 substrate that contains a palmitoyl thioester at the sn-2 position of the glycerol backbone. Hydrolysis of the thioester by PLA2 yields a free thiol that reacts readily with DTNB (Ellman's reagent) giving a bright yellow product with an absorbance maximum at 412 nm. Palmitoyl thio-PC has been used to measure bee venom sPLA2 activity in a phospholipid:Triton X-100 mixed micelle system.

Palmitoyl-D-carnitine (chloride) (Legacy Tebubio ref. 282T37245). Palmitoyl-D-carnitine is a long-chain acylcarnitine, an isomer of palmitoyl-L-carnitine , and the D enantiomer of palmitoyl-DL-carnitine . It inhibits carnitine palmitoyltransferase with a Ki value of 2.1 mM for 14C-palmitoylcarnitine synthesis by erythrocyte membranes.

Palonosetron N-oxide (Legacy Tebubio ref. 282T37246). Palonosetron N-oxide is a metabolite of the serotonin (5-HT) receptor subtype 5-HT3antagonist palonosetron .1It is also a potential impurity in palonosetron preparations.2Palonosetron N-oxide is a degradation product formed by exposure to oxidative stress.

Pantothenate Kinase Inhibitor (Legacy Tebubio ref. 282T37248). Pantothenate Kinase Inhibitor (PANKi) is a reversible inhibitor of pantothenate kinase (PanK; IC50s = 70, 92, and 25 nM for PanK1β, PanK2, and PanK3, respectively), the rate-limiting enzyme in the synthesis of coenzyme A .1It binds to the ATP-PanK3 complex with an apparent binding constant of 300 nM and exhibits mixed-type inhibition with respect to ATP and pantothenate. PANKi inhibits CoA biosynthesis in C3A cells (IC50= 0.9 μM) with no effect on cell viability when used at concentrations up to 8 μM. PANKi (5 μM) synergizes with BSO to induce ferroptosis in PANC-1 cells and sensitizes the cells to imidazole ketone erastin-induced ferroptosis.2

Methylmalonyl-Coenzyme A (sodium salt) (Legacy Tebubio ref. 282T37249). Methylmalonyl coenzyme A (methylmalonyl-CoA) is an intermediate in multiple metabolic pathways in bacteria and eukaryotes.1,2,3It is an intermediate in carbon assimilation in certain bacteria and carbon fixation in plants.1,2Methylmalonyl-CoA is converted to succinyl-CoA by methylmalonyl-CoA mutase with vitamin B12as a coenzyme.3A deficiency in vitamin B12leads to a build-up of methylmalonyl-CoA.4

K-Ras(G12C) Inhibitor 6 (Legacy Tebubio ref. 282T3725). K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C) mutant, achieving 100% protein modification at 10 μM after 24 hours in vitro.