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SLx-2119 CAS: 911417-87-3

SLx-2119(KD-025, cas 911417-87-3) is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM). In humans, oral KD 025 diminishes STAT3 phosphorylation and pro-inflammatory cytokine production in CD4+ T cells while up-regulating phosphorylation of STAT5 in regulatory T cells, altering the immune response.

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A major introduction to T-705!

Favipiravir (cas 259793-96-9 ), also known as T-705 or Avigan, is an antiviral drug that selectively inhibits the RNA-dependent RNA polymerase of influenza virus. It is phosphoribosylated by cellular enzymes to its active form, favipiravir-ribofuranosyl-5'-triphosphate (RTP). Favipiravir is active against a broad range of influenza viruses, including A(H1N1)pdm09, A(H5N1) and the recently emerged A(H7N9) avian virus. It also inhibits influenza strains resistant to current antiviral drugs, and shows a synergistic effect in combination with oseltamivir, thereby expanding influenza treatment options.
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A major introduction to K03861!

Kinases can switch between active and inactive conformations of the ATP/Mg(2+) binding motif DFG, which has been explored for the development of type I or type II inhibitors. However, factors modulating DFG conformations remain poorly understood. We chose CDK2 as a model system to study the DFG in-out transition on a target that was thought to have an inaccessible DFG-out conformation. We used site-directed mutagenesis of key residues identified in structural comparisons in conjunction with biochemical and biophysical characterization of the generated mutants. As a result, we identified key residues that facilitate the DFG-out movement, facilitating binding of type II inhibitors. However, surprisingly, we also found that wild type CDK2 is able to bind type II inhibitors. Using protein crystallography structural analysis of the CDK2 complex with an aminopyrimidine-phenyl urea inhibitor ( K03861 ) revealed a canonical type II binding mode and the first available type II inhibitor CDK2 co
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Itacitinib is in stock now!

Itacitinib(cas# 1334298-90-6) , also known as INCB39110 or INCB039110, is a potent JAK1 tyrosine kinase inhibitor, which is currently in Phase II trials for the treatment of rheumatoid arthritis, myelofibrosis, rheumatoid arthritis and plaque psoriasis. INCB039110 produced significant improvements in sPGA, demonstrating proof of concept in chronic plaque psoriasis.
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