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MW 434.5 Da. Potent, selective, substrate competitive neutrophil elastase inhibitor (IC₅₀ values are 19-49 nM and 5.6 μM for leukocyte and pancreas elastase respectively). Suppresses neutrophil-induced capillary permeability and leukocyte kinetics. Active in vivo. .
MW 411.33 g/mol, Purity >99%. Potent and selective protein kinase D inhibitor (IC₅₀ values are 1, 2 and 2.5 nM at PKD1, PKD3 and PKD2, respectively). Reduces proliferation of pancreatic cancer cells. Orally active. Antitumor agent. Active in vivo and in vitro.
MW 294.4 Da, Purity >98%. Potent, cell-permeable inhibitor of X-linked inhibitor of apoptosis (XIAP) (IC₅₀ = 4.1 μM). Binds to the XIAP BIR3 protein and interacts with residues crucial for Smac and caspsase-9 binding. Inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells (IC₅₀ = 3.7 - 5.7 μM); minimal effects on normal prostate cells (IC₅₀ = 19.3 - 20.1 μM). Antitumor and anti-inflammatory effects in vivo.
MW 452.7 Da, Purity >99%. Potent and selective myosin light chain kinase inhibitor (MLCK) (Ki = 300 nM). Also inhibits PKA and PKC (Ki values are 21 and 42 μM, respectively). Cell-permeable. Inhibits tumor cell growth.