rel-Talmapimod hydrochloride  (Synonyms: rel-SCIO-469 hydrochloride)

rel-Talmapimod (rel-SCIO-469) hydrochloride is an orally active and selective inhibitor of p38α MAPK with an IC₅₀ of 9 nM. rel-Talmapimod hydrochloride inhibits the secretion of inflammatory factors (such as TNFα, IL-1β, IL-6, and VEGF) by suppressing the p38α MAPK pathway, and it also inhibits angiogenesis and osteoclast activation. rel-Talmapimod hydrochloride inhibits the growth of multiple myeloma cells and induces apoptosis. rel-Talmapimod hydrochloride can be used to study various hematological malignancies (such as multiple myeloma, myelodysplastic syndrome)^[1][2][3][4].

549.46

C₂₇H₃₁Cl₂FN₄O₃

879132-01-1

CN(C)C(C(C(C1=C2)=CN(C)C1=CC(Cl)=C2C(N3[C@@H](CN([C@H](C3)C)CC4=CC=C(C=C4)F)C)=O)=O)=O.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [2]. Navas T, et al. Inhibition of p38alpha MAPK disrupts the pathological loop of proinflammatory factor production in the myelodysplastic syndrome bone marrow microenvironment. Leuk Lymphoma. 2008 Oct;49(10):1963-75.  [Content Brief]

  [3]. 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. Cancer Res. 2007 May 15;67(10):4572-7.  [Content Brief]

  [4]. Medicherla S, et al. p38alpha-selective MAP kinase inhibitor reduces tumor growth in mouse xenograft models of multiple myeloma. Anticancer Res. 2008 Nov-Dec;28(6A):3827-33.  [Content Brief]