pim enzyme (Carna Inc)
Structured Review
Pim Enzyme, supplied by Carna Inc, used in various techniques. Bioz Stars score: 96/100, based on 9 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/02-054/PIM1/pm37262997-285-4-6
Average 96 stars, based on 9 article reviews
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other:Article Title: Usnic acid is a novel Pim-1 inhibitor with the abilities of inhibiting growth and inducing apoptosis in human myeloid leukemia cells Article Snippet: Usnic acid (UA) is a secondary metabolite of lichens with a unique dibenzofuran scaffold.. The growth inhibitory and apoptotic effects of UA as well as the potential mechanisms of action were determined in human acute myeloid leukemia HL-60 cells and chronic myeloid leukemia K562 cells.. UA inhibits growth and induces apoptosis in both cell lines with HL-60 cells more responsive. Article Title: Safety profiling of genetically engineered Pim-1 kinase overexpression for oncogenicity risk in human c-kit+ cardiac interstitial cells. Article Snippet: The following kinases were obtained from Incubation:Article Title: Discovery of a high potent PIM kinase inhibitor for acute myeloid leukemia based on N-pyridinyl amide scaffold by optimizing the fragments toward to Lys67 and Asp128/Glu171. Article Snippet: Despite the recent development of PIM inhibitors based on N-(pyridin-3-yl)acetamide scaffold for acute myeloid leukemia (AML), the structural-activity relationship (SAR) associated with the effects of positional isomerization of N toward to Lys67 and freedom of solvent fragment toward to Asp128/Glu171 still remains an open question.. In this work, a structurally novel compound based on N-pyridinyl amide was designed by fragment hybridization and then our SAR exploration revealed that the positional isomerization would lead to a decrease in activity, while increase of the freedom of solvent fragment by breaking the intramolecular hydrogen bond unprecedentedly leads to an increase in activity.. These studies finally resulted in the screening out of a potent PIM inhibitor FD1024 (compound 24) which exerts strong antiproliferative activity against the tested AML cell lines and achieves profound antitumor efficacy in mice at well-tolerated dose schedules. Recombinant:Article Title: Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. Article Snippet: .. Human recombinant FLT3 (Sino Biological Inc., 10445-H08H), |
