Activators & Inhibitors

TPCA-1 (TPCA1) is an effective and specific IKK-2 inhibitor (IC50: 17.9 nM); shows >22-fold selectivity over IKK-1 and >550-fold selectivity over others kinases and enzymes.

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

H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.

 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

Ricolinostat (Rocilinostat) is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.