SCIO 469 hydrochloride
Chemical Name: 6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-1H-Indole-3-acetamide hydrochloride
Biological ActivitySelective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38α in vitro). Displays approximately 10-fold selectivity for p38α over p38β and 2000-fold selectivity for p38α over 20 other kinases. Reduces p38α phosphorylation in multiple myeloma cells in vitro and in vivo; activity results in decreased tumor burden and angiogenesis in murine models of multiple myeloma. Also enhances bortezomib-induced cytotoxicity against multiple myeloma cells.
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p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells.
Hideshima et al.
Role of the p38 mitogen-activated protein kinase pathway in the generation of arsenic trioxide-dependent cellular responses.
Giafis et al.
Cancer Res., 2006;66:6763
Inhibition of p38α mitogen-activated protein kinase prevents the development of osteolytic bone disease, reduces tumor burden, and increases survival in murine models of multiple myeloma.
Vanderkerken et al.
Cancer Res., 2007;67:4572
Citations for SCIO 469 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for SCIO 469 hydrochloride include:
2 Citations: Showing 1 - 2
High-level expression of ARID1A predicts a favourable outcome in triple-negative breast cancer patients receiving paclitaxel-based chemotherapy.
Authors: Lin Et al.
J Cell Mol Med 2018;22:2458
Divergent signalling pathways regulate lipopolysaccharide-induced eRNA expression in human monocytic THP1 cells.
Authors: Heward Et al.
FEBS Lett 2015;589:396
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