Activators & Inhibitors

Potent and selective inhibitor of phosphatidyl-inositol 3-kinase. Active in purified preparations and cytosolic fractions(IC50 = 5nM) and is highly cell permeable. Covalently binds to PI 3-kinase and is selective, inhibiting other kinases such as PI 4-kinase and myosin light chain kinase at concentrations 100-fold higher than that required for inhibition of PI 3-kinase.

Gefitinib is a tyrosine kinase inhibitor. It is a potent inhibitor of EGFR kinase (Ki = 0.40 nM), but much weaker against ErbB-2 kinase (Ki = 870 nM) and ErbB-4 kinase (Ki = 1.1 µM).

K252a is a general kinase inhibitor that inhibits PKA (Ki = 18 nM), PKC (Ki = 25 nM), PKG (Ki = 20 nM), CaMK (Ki = 1.8 nM), and phosphorylase kinase (IC50 = 1.7 nM). It functions by acting competitively with ATP and noncompetitively with the substrate.

Cediranib, also known as AZD2171, is a highly potent inhibitor of recombinant KDR tyrosine kinase activity in vitro (IC50 < 1 nM). Inhibitory activity was also observed against the kinase associated with Flt-1 (IC50 = 5 nM), the VEGF-C and VEGF-D receptor Flt-4 (IC50 ≤ 3 nM), recombinant PDGFR-related kinase c-Kit (IC50 = 2 nM), and PDGFRβ tyrosine kinase (IC50 = 5 nM). In HUVEC, it inhibited VEGF-stimulated phosphorylation of KDR, c-Kit, PDGFR-α, PDGFR-β in a dose-dependent manner with IC50 values of 0.5, 1, 5, and 8 nM, respectively. Cediranib exhibits antitumor and antiangiogenic activity, and is a potential treatment for hypertension.

Tofacitinib, also known as Tasocitinib, is a novel inhibitor of Janus kinase 3 (JAK3), a critical cytoplasmic tyrosine kinase in the signaling pathways of multiple cytokines. Research suggests Tofacitinib acts as an immunosuppressant, preventing organ transplant rejection, and that it has potential to alleviate symptoms of autoimmune diseases, such as rheumatoid arthritis and psoriasis.

Specific inhibitor (IC50 = 1.40 µM) of phosphatidylinositol 3-kinase (PI3K).

Roscovitine is a potent inhibitor of p34cdc2 (IC50 = 0.2 µM). Also inhibits p33cdk2 and p33cdk5.

A cell-permeable, water-soluble, potent inhibitor of poly(ADP-ribose) polymerase (PARP; EC50 = 20 nM). Shown to be about 10,000 times more potent than the prototypical PARP inhibitor, 3-Aminobenzamide (Cat. No. 165350; EC50 = 200 µM). Does not act as an antioxidant at higher concentrations (1 µM to 10 mM). Exhibits neuroprotection in in vivo and in vitro models of stroke.

Specifically and reversibly blocks translocation of proteins from the endoplasmic reticulum to the Golgi apparatus and induces apoptosis in human tumor cells via caspase activation. Brefeldin A has been identified as an activator of the sphingomyelin signal transduction cycle.