Rel-Talmapimod (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].

Product Specifications

CAS Number

[879132-01-1]

Product Name Alternative

Rel-SCIO-469 (hydrochloride)

UNSPSC

12352005

Target

Apoptosis; Interleukin Related; p38 MAPK; TNF Receptor; VEGFR

Related Pathways

Apoptosis; Immunology/Inflammation; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

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

Molecular Formula

C27H31Cl2FN4O3

Molecular Weight

549.46

References & Citations

[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]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.|[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.|[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.