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Product listing: Bortezomib #2204 to Ionomycin, Calcium Salt #9995

Molecular Weight:280.4 g/mol

Background: Brefeldin A (BFA) is a fungal metabolite demonstrated to reversibly interfere with anterograde transport from the endoplasmic reticulum to the Golgi apparatus (1,2). While initially isolated as an antibiotic (3), and does have a wide range of antibiotic activity, it is primarily used as a biological research tool for studying protein transport. Treatment leads to a rapid accumulation of proteins within the ER and collapse of the Golgi stacks. Treatment with BFA can also inhibit protein secretion (4) and prolonged exposure can induce apoptosis (5). The main target of BFA appears to be ADP-ribosylation factor (ARF), which is responsible for association of coat protein to the Golgi membrane (6,7).

Calyculin A is a more potent phosphatase inhibitor than Okadaic acid (2). As shown by Western blot, treatment of cells with 100 nM Calyculin A for 30 minutes induces threonine phosphorylation, detected by Phospho-Threonine-Polyclonal Antibody #9381. IC50 values for inhibitory activity against PP1 are approximately 2 nM. IC50 values for inhibitory activity against PP2A are approximately 0.5 -1.0 nM.

Background: Calyculin A inhibits the activity of protein phosphatases PP1 and PP2A (1,2). Unlike Okadaic acid, which reduces PP2A activity but has little effect on PP1 activity, Calyculin A inhibits both phosphatases (1). Neither Calyculin A nor Okadaic acid inhibit acid or alkaline phosphatases or phospho- tyrosine protein phosphatases (2).

Molecular Weight:1202.63 g/mol

Background: The calcium dependent protein phosphatase calcineurin is responsible for the de-phosphorylation of the transcriptional regulator nuclear factor of activated T cells (NFAT) and is essential for NFAT’s nuclear translocation and activation (1,2). Calcineurin is a target of two common immunosuppressants, cyclosporin A (CsA) (3) and FK-506 (also know as tacrolimus and fugimycin) (4), both of which can inhibit antigen and mitogen triggered T cell activation. These drugs interact with the immunophilins cyclophilin and FKBP-12, respectively, and the immunophilin-drug complex binds to calcineurin to inhibit substrate binding (5). FK-506 can be up to 100-fold more potent than CsA in various models (6-8).

Molecular Weight:807.89 g/mol

Background: Docetaxel belongs to the taxane family of antitumor and antileukemic agents (1). A microtubule-stabilizing agent, docetaxel acts as an inhibitor of cellular functions that require microtubule dynamics including cell division, and is now in use as a treatment for breast, prostate and lung cancer (2).

Molecular Weight:804.03 g/mol

Background: The calcium dependent protein phosphatase calcineurin is responsible for the de-phosphorylation of the transcriptional regulator nuclear factor of activated T cells (NFAT) and is essential for NFAT’s nuclear translocation and activation (1,2). Calcineurin is a target of two common immunosuppressants, cyclosporin A (CsA) (3) and FK-506 (also know as tacrolimus and fugimycin) (4), both of which can inhibit antigen and mitogen triggered T cell activation. These drugs interact with the immunophilins cyclophilin and FKBP-12, respectively, and the immunophilin-drug complex binds to calcineurin to inhibit substrate binding (5). FK-506 can be up to 100-fold more potent than CsA in various models (6-8).

Molecular Weight:410.5 g/mol

Background: Forskolin, a naturally occurring diterpene from the Indian plant, Coleus forskohlii, activates adenylate cyclase, and thus increases the intracellular cAMP concentration (1). The second messenger cAMP activates cAMP-dependent protein kinase (PKA or cAPK) and controls many cellular mechanisms such as gene transcription, ion transport and protein phosphorylation (2).

Molecular Weight:560.64 g/mol

Background: Geldanamycin (GA) is a naturally existing HSP90 inhibitor that belongs to the benzoquinone ansamycin family. GA binds to the amino terminal ATP-binding pocket of HSP90 and inhibits ATP binding and hydrolysis. HSP90 is a chaperone interacting with a wide variety of important target proteins for cell signaling and regulation during tumorgenesis (1,2). The binding of GA to HSP90 interferes with HSP-mediated target protein folding, leading to target aggregation and degradation (1-3). GA and its synthetic derivatives show higher affinity to HSP90 in tumor cells as compared to normal tissues and constitute a class of protential antitumor drugs (2-3).

$115
5.19 mg
Molecular Weight:519.28 g/mol
APPLICATIONS

Application Methods: Western Blotting

Background: H-89 is a potent selective inhibitor of cAMP dependent protein kinase (PKA). The in vitro IC50 of H-89 for PKA is approximately 50 nM and in vivo the inhibitiory effect on PKA substrate phosphorylation and related cellular functions range from 10 μM to 30 μM (1,2). In addition to PKA, H-89 also exhibits a moderate inhibitory effect on PKG and PKCμ, with IC50 in the 500 nM range (1,3). The inhibitory effect of H-89 is due to its competitive binding to the ATP pocket on the kinase catalytic subunit (4).

Molecular Weight:747.1 g/mol

Background: Ionomycin is a potent and selective calcium ionophore agent (1,2). The molecule acts as a motile Ca2+ carrier and enhances Ca2+ influx by direct stimulation of store-regulated cation entry across biological membranes (3). At the micromolar level, ionomycin can activate Ca2+/Calmodulin dependent kinase and phosphatase to stimulate gene expression (4). In human T cells, ionomycin induces hydrolysis of phosphoinositides and activates PKC to mediate T cell activation (5). Ionomycin treatment of human B cells induces the activation of calcium-dependent endonuclease and results in apoptosis (6). Ionomycin treatment of bovine aortic endothelial cells (BAECs) induces rapid dephosphorylation of eNOS at Thr495 and mediates eNOS activation (7).