Results for Chemicals & Small Molecules ( 96685 )
Our potent and selective hOT receptor fluorescent antagonist shows high affinity for hOT receptor (Kd =1,59 nMin TR-FRET saturation binding assay). It allows to perform cell visualization in fluorescence microscopy, confocal microscopy, high content system experiments and TR-FRET experiments. It is potentially suitable for other fluorescence-based assays.
NVP-AUY922 potently inhibits HSP90 with IC50 values of 7.8 nM and 21 nM, and Ki values of 9 nM and 8.2 nM for HSP90α and HSP90β, respectively. NVP-AUY922 shows a very high binding affinity to HSP90β with a Kd of 1.7 nM. NVP-AUY922 inhibits the proliferation of human tumor cells in vitro with GI50 values of approximately 2 to 40 nM, inducing G1-G2 arrest and apoptosis. Human endothelial cells are very sensitive to NVP-AUY922 with GI50s of 2.5-3.9 nM. NVP-AUY922 also exhibits potent antitumor efficacy in human tumor xenografts including BT474 breast, A2780 ovarian, U87MG glioblastoma, PC3 prostate, and WM266.4 melanoma.
NVP-AUY922 potently inhibits HSP90 with IC50 values of 7.8 nM and 21 nM, and Ki values of 9 nM and 8.2 nM for HSP90α and HSP90β, respectively. NVP-AUY922 shows a very high binding affinity to HSP90β with a Kd of 1.7 nM. NVP-AUY922 inhibits the proliferation of human tumor cells in vitro with GI50 values of approximately 2 to 40 nM, inducing G1-G2 arrest and apoptosis. Human endothelial cells are very sensitive to NVP-AUY922 with GI50s of 2.5-3.9 nM. NVP-AUY922 also exhibits potent antitumor efficacy in human tumor xenografts including BT474 breast, A2780 ovarian, U87MG glioblastoma, PC3 prostate, and WM266.4 melanoma.
Potent (Ki, 0.6 nM), specific and reversible proteasome inhibitor; no significant inhibitory activity against other enzymes or receptors. Bortezomib inhibits cell proliferation of H460 cells (human non-small cell lung cancer cell lines) with an IC50 of 0.1 µM and has been associated with suppresion of prostate cancer cell lines with an IC90 of 10 nM.
Potent (Ki, 0.6 nM), specific and reversible proteasome inhibitor; no significant inhibitory activity against other enzymes or receptors. Bortezomib inhibits cell proliferation of H460 cells (human non-small cell lung cancer cell lines) with an IC50 of 0.1 µM and has been associated with suppresion of prostate cancer cell lines with an IC90 of 10 nM.
Doramapimod is a protein kinase inhibitor with a >330-fold selectivity for p38 MAPK compared with 12 other protein kinases. Doramapimod prevents both the kinetic activity and phosphorylation of p38 MAPK by binding to the ATP pocket as well as to a novel allosteric binding site on p38 MAPK. Doramapimod also blocks proliferation of cells expressing BCR-ABL(T315I), with an IC50 of 2-3 µM.
Doramapimod is a protein kinase inhibitor with a >330-fold selectivity for p38 MAPK compared with 12 other protein kinases. Doramapimod prevents both the kinetic activity and phosphorylation of p38 MAPK by binding to the ATP pocket as well as to a novel allosteric binding site on p38 MAPK. Doramapimod also blocks proliferation of cells expressing BCR-ABL(T315I), with an IC50 of 2-3 µM.