Talmapimod (SCIO-469) (Synonyms: Talmapimod) |
Katalog-Nr.GC34072 |
Talmapimod (SCIO-469) (SCIO-469) ist ein oral aktives, selektives und ATP-kompetitives p38α Inhibitor mit einem IC50 von 9 nM. Talmapimod (SCIO-469) zeigt eine etwa 10-fache SelektivitÄt gegenÜber p38β und eine mindestens 2000-fache SelektivitÄt gegenÜber einer Reihe von 20 anderen Kinasen, einschließlich anderer MAPKs.
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Cas No.: 309913-83-5
Sample solution is provided at 25 µL, 10mM.
Talmapimod (SCIO-469) is a selective ATP-competitive p38 inhibitor with IC50 of 9 nM for p38α.
Talmapimod (SCIO-469)decreased constitutive p38α MAPK phosphorylation of both 5T2MM and 5T33MM cells. Talmapimod (SCIO-469) also inhibits secretion and expression of the osteoclast-activating factors IL-11, receptor activator of NF-κB ligand, and macrophage inflammatory protein 1α, and prevents human osteoclast activationIn. It can also inhibit multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models.
Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease.
[1]. Hideshima T et al. p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells. Oncogene. 2004 Nov 18, 23(54), 8766-76. [2]. Vanderkerken K et al. Inhibition of p38alpha mitogen-activated protein kinase prevents the development of osteolytic bone disease,reduces tumor burden, and increases survival in murine models of multiple myeloma. Vanderkerken K et al.
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