A32390A, an isonitrile-containing analog of mannitol, is a new class of antifungal antibiotics. In vitro antifungal activity of A32390A was found against Candida albicans, Cryptococcus neoformans and Histoplasma capsulatum. In vivo antifungal activity of A32390A was observed in mice infected with C. albicans. Accumulative doses of 37.5 approximately 600 mg/kg, administered subcutaneously over a 24-hour […]

Takeda-6d is a novel dual inhibitor of DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) with anticancer activity. It inhibits wild-type B-RAF, mutant B-RAFV600E, and C-RAF (IC50s = 12, 7, and 1.5 nM, respectively), as well as VEGFR2 (IC50 = 2.8 nM). Takeda-6d (10 mg/kg) reduces tumor volume in an A375 melanoma mouse xenograft model. […]

AMG-25 (AMG25) is a novel, oral, potent and selective inhibitor of c-Kit with anticancer activity and desirable pharmacokinetic properties. It inhibits c-Kit with IC50s of 22 nM and 16 nM in kinase assay and cell assay, respectively.

YKL-05-099 (YKL05099) is a novel, potent and selective inhibitor of salt-inducible kinase (SIK) with the potential to be used for treatment of inflammatory disorders. YKL-05-099 acts by binding to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM). SIKs are promising therapeutic targets for modulating […]

Vedolizumab (trade name Entyvio; Anti-Human lymphocyte α4β7 integrin, Humanized Antibody) is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn’s disease. Vedolizumab is a monoclonal antibody developed by Millennium Pharmaceuticals, Inc (a subsidiary of Takeda Pharmaceuticals) for the treatment of ulcerative colitis and Crohn’s disease. It binds […]

GNE-493 is a novel, potent, selective, and orally bioavailable dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR. The PI3K/AKT/mTOR pathway has been shown to play an important role in cancer. Starting with compounds 1 and 2 (GDC-0941) as templates, […]

GNE-371 is a novel, potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like with an IC50 of 10 nM for TAF1(2). The biological functions of the dual bromodomains of human transcription-initiation-factor TFIID subunit 1 (TAF1(1,2)) remain unknown, although TAF1 has been identified as a […]

BET-BAY 002 is a novel and potent BET (Bromodomain and extra-terminal ) inhibitor which exhibits high efficacy in a multiple myeloma model.

BMS 433796 is a novel and potent γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer’s disease. BMS-433796 exhibited favorable pharmacodynamic and pharmacokinetic profiles. Chronic dosing of BMS-433796 in Tg2576 mice suggested a narrow therapeutic window and Notch-mediated toxicity at higher doses. Reduction of brain beta-amyloid peptide (Abeta) synthesis by gamma-secretase […]

PF-2771 is a novel, potent and selective inhibitor of centromere protein E (CENP-E) with anticancer activity. It inhibits CENP-E motor activity with an IC50 of 16.1 nM. Mechanistic evaluation of PF-2771 in basal-a tumor cells links CENP-E-dependent molecular events (e.g., phosphorylation of histone H3 Ser-10; phospho-HH3-Ser10) to functional outcomes (e.g., chromosomal congression defects). Across a […]