Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
4 Results for "
kinase selectivity analysis
" in MedChemExpress (MCE) Product Catalog:
Products (4)
4 Results for "kinase selectivity analysis" in MCE Product Catalog:
1
1 Cited Publications
Target:
Research Areas:
Bisindolylmaleimide III is a protein kinase C (PKC) inhibitor with IC50 values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III also exhibits inhibitory activity against other off-targets, with IC50 values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its Ki for NQO2 is 16.5 μM. Bisindolylmaleimide III selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III can be used in studies of signal transduction and colorectal cancer .
Cat. No.: HY-D2415
CAS No.: 2411845-57-1
Cat. No.: HY-121708
CAS No.: 930089-25-1
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
Cat. No.: HY-112454
CAS No.: 683775-59-9
Target:
Research Areas:
Bisindolylmaleimide III hydrochloride is a protein kinase C (PKC) inhibitor with IC50 values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III hydrochloride also exhibits inhibitory activity against other off-targets, with IC50 values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its Ki for NQO2 is 16.5 μM. Bisindolylmaleimide III hydrochloride selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III hydrochloride can be used in studies of signal transduction and colorectal cancer .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
