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GLPG-1690 CAS: 1628260-79-6

GLPG-1690, an imidazopyridine derivative, has been found to be a ENPP2 protein inhibitor that could probably be effective as an anti-inflammatory agent and is under Phase II trial against Idiopathic pulmonary fibrosis.
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A major introduction to VER-155008!

VER-155008 is an adenosine-derived inhibitor of heat shock protein 70 (Hsp70; IC50 = 0.5 μM) tIt targets the nucleotide-binding domain (NBD) of Hsp70 and similarly binds the NBDs of Hsp70 cognates Hsc70 (Ki = 10 μM) and glucose-regulated protein 78 (Grp78; KD = 80 nM).hat is selective over Hsp90. VER-155008 inhibits the proliferation of human breast and colon cancer cell lines, inducing apoptosis or caspase-independent cell death. It induces the proteasome-dependent degradation of Hsp 90 client proteins and potentiates the apoptotic activity of Hsp90 inhibitors.

Herpes virus helicase-primase inhibitor, Amenamevir is available now!

Herpes virus helicase-primase inhibitor, Amenamevir is available now! Amenamevir, also known as ASP2151, is a herpes virus helicase-primase inhibitor. Amenamevir was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on Jul 3, 2017 and marketed as Amenalief

Verrucrin J is in stock now!

Verrucrin J is in stock now!

A major introduction to RG7388!

RG7388(cas 1229705-06-9) is an oral, selective, small molecule MDM2 antagonist that inhibits binding of MDM2 to p53. RG7388 binds to MDM2 blocking the interaction between the MDM2 protein and the transcriptional activation domain of the tumor suppressor protein p53. By preventing the MDM2-p53 interaction, p53 is not enzymatically degraded and the transcriptional activity of p53 is restored. This may lead to p53-mediated induction of tumor cell apoptosis.

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 coc…

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.