Activators & Inhibitors

Activity: ALK4,5 and 7 inhibitor . Function/Pharmacology: Potent and selective ALK4, ALK5 and ALK7 inhibitor (TGFβ superfamily Type I activin receptor-like kinase). (ALK5 IC50 = 94 nM)1,2. Inhibits TGFβ-induced proliferation of human osteosarcoma cells3. Ehances growth and integrity of embryonic stem cell-derived endothelial cells4. A frequently used agent employed in numerous stem cell differentiation protocols5. Cell permeable. Chemical Name: 4-[4-(1,3-Benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide

Activity: Autophagosome inhibitor . Function/Pharmacology: Inhibits autophagy by blocking autophagosome formation via inhibition of type III phosphatidylinositol 3-kinases (PI-3K)1,2. Protects 1321N1 astrocytoma cells against pyocyanin and hydroxyphenazine-induced toxicity3. Enhances celastrol-induced apoptosis in human pancreatic cancer cells4. Chemical Name: 3-Methyl-3H-purin-6-amine

Activity: Mitochondrial import inhibitor . Function/Pharmacology: Inhibits redox-regulated protein translocation into mitochondria. It attenuates the import of Erv1 substrates by inhibition of Erv1 oxidase activity (the import of Tim23 and AAC was decreased by ~50% at 20 μM). MitoBloCK-6 elucidated an unexpected role for Erv1 in the carrier import pathway, namely transferring substrates from the translocase of the outer membrane complex into the small Tim complexes. It impaired cardiac development in zebrafish embryos and induced apoptosis via the release of cytochrome c in human embryonic stem cells but not differentiated cells1. Chemical Name: 2-[[(4-Anilinophenyl)imino]methyl]-4,6-dichlorophenol

Activity: Disrupts actin filaments . Function/Pharmacology: Potent inhibitor of actin polymerization which also causes the disruption of actin filaments. More potent that cytochalasin B (10-fold) and does not inhibit monosaccharide transport across cell membranes. Disruption of actin microfilaments leads to activation of p53. Cell permeable Chemical Name: (7S,13E,16S,18R,19E,21R)-21-(Acetyloxy)-7,18-dihydroxy-16,18-dimethyl-10-phenyl[11]cytochalasa-6(12),13,19-triene-1,17-dione

Activity: Microtubule stabilizing agent . Function/Pharmacology: Taxol is a clinically useful cancer chemotherapeutic agent for the treatment of breast, non-small cell lung and ovarian cancer.1 It acts as a promoter of tubulin polymerization and stabilizes microtubules in vitro and in vivo resulting in arrest of cells in the G2 and M phase of the cell cycle.2

 for Western Blotting and ELISA (Kit contents: solution A, solution B, 250ml each)

Activity: GSK3β inhibitor . Function/Pharmacology: Potent and selective inhibitor of glycogen synthase kinase-3β (GSK3β, IC50 = 5 nM) and GSK3α (IC50 = 10 nM)1. Induces osteoblastogenesis, increases mineralization and inhibits adipogenesis in ST2 cells2. Promotes replication and survival of pancreatic beta cells3. Enhances differentiation and reduces proliferation of adult human olfactory epithelium neural precursors4. Cell permeable and active in vivo. Chemical Name: 6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile

Activity: SOD mimetic . Function/Pharmacology: Superoxide dismutase (SOD) mimetic. Displays protective effects in CNS1 kidney2 and radiation damage3. Inhibits superoxide anion-induced inflammatory pain in mice.4 Blunts diabetes-induced upregulation of NADPH oxidase and ER stress in a rat model of diabetic nephropathy.5 Cell permeable Chemical Name: 4-Hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl