Activators & Inhibitors

2,6-Dimethoxybenzoic acid (Legacy Tebubio ref. 282T3758). 2,6-Dimethoxybenzoic acid is an o-methoxybenzoic acid and its derivatives that inhibit fungi and bacteria.

Arachidonoyl thio-PC (Legacy Tebubio ref. 282T37580). Arachidonoyl Thio-PC is a substrate for various phospholipase A2s (PLA2s), including sPLA2, cPLA2, and iPLA2. Cleavage of the sn-2 fatty acid by PLA2 produces a free thiol that reacts with chromogenic reagents like DTNB (Ellman's reagent) and DTP, facilitating PLA2 activity quantitation. Isozyme-specific cPLA2 activity can be measured by excluding or inhibiting sPLA2 and iPLA2 activities in the assay.

SCIO 469 hydrochloride (Legacy Tebubio ref. 282T37581). Selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38α in vitro). Displays approximately 10-fold selectivity for p38α over p38β and 2000-fold selectivity for p38α over 20 other kinases. Reduces p38α phosphorylation in multiple myeloma cells in vitro and in vivo; activity results in decreased tumor burden and angiogenesis in murine models of multiple myeloma. Also enhances bortezomib-induced cytotoxicity against multiple myeloma cells.

Ganglioside GM1 Mixture (ovine) (ammonium salt) (Legacy Tebubio ref. 282T37582). Ganglioside GM1is a monosialylated ganglioside and the prototypic ganglioside for those containing one sialic acid residue.1,2It is found in a large variety of cells, including immune cells and neurons, and is enriched in lipid rafts in the cell membrane.3It associates with growth factor receptors, including TrkA, TrkB, and the GDNF receptor complex containing Ret and GFRα, and is required for TrkA expression on the cell surface. Ganglioside GM1interacts with other proteins to increase calcium influx, affecting various calcium-dependent processes, including inducing neuronal outgrowth during differentiation. Ganglioside GM1acts as a receptor for cholera toxin, which binds to its oligosaccharide group, facilitating toxin cell entry into epithelial cells of the jejunum.4,5Similarly, it is bound by the heat-labile enterotoxin fromE. coliin the pathogenesis of traveler's diarrhea.6Ganglioside GM1gangliosidosis

XTT (sodium salt hydrate) (Legacy Tebubio ref. 282T37583). XTT is a cell-impermeable, negatively charged tetrazolium dye that produces a water-soluble formazan when reduced at the cell surface by cellular-derived NADH and an electron mediator [1,2]. It is frequently used in colorimetric assays to measure cell proliferation, cytotoxicity, and apoptosis [3].

Tryptoquivaline D (Legacy Tebubio ref. 282T37584). Tryptoquivaline D is a fungal metabolite found in [Neosartorya siamensis] with noted anticancer activity. It induces nuclear chromatin condensation, a marker of apoptosis, in HCT116 colon and HepG2 liver cancer cells at a concentration of 150 μM. Tryptoquivaline D (1-100 μM), alone or with doxorubicin, reduces the viability of A549 lung cancer cells.

Ensartinib (Legacy Tebubio ref. 282T37585). Ensartinib (X-396) is a potent dual ALK/MET inhibitor with IC50 values of <0.4 nM for ALK and 0.74 nM for MET.

DMHAPC-Chol (Legacy Tebubio ref. 282T37586). DMHAPC-Chol is a cationic cholesterol. Liposomes containing DMHAPC-chol have been used for DNA plasmid delivery in vitro and in vivo in a B16-F10 mouse xenograft model. Liposomes containing DMHAPC-chol are cytotoxic to B16-F10 cells when used at lipid concentrations greater than 20 μM. DMHAPC-Chol, as part of a lipoplex with DOPE , has also been used to deliver DNA into mouse lung via intratracheal injection, resulting in a heterogeneous distribution in the bronchi and bronchioles, and to deliver VEGF siRNA into A431 and MDA-MB-231 cells, which secrete VEGF.

ML 209 (Legacy Tebubio ref. 282T37587). ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.