Talmapimod (hydrochloride)

• Description:

  Talmapimod (SCIO-469) hydrochloride is an orally active and selective inhibitor of p38α MAPK with an IC50 of 9 nM. 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. Talmapimod hydrochloride inhibits the growth of multiple myeloma cells and induces apoptosis. Talmapimod hydrochloride can be used to study various hematological malignancies (such as multiple myeloma, myelodysplastic syndrome) [1][2][3][4].

• Product Name Alternative:

  SCIO-469 (hydrochloride)

• UNSPSC:

  12352005

• Target:

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

• Type:

  Reference compound

• Related Pathways:

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

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/talmapimod-hydrochloride.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C(N(C)C)C(C1=CN(C)C2=C1C=C(C(N3[C@H](C)CN(CC4=CC=C(F)C=C4)[C@@H](C)C3)=O)C(Cl)=C2)=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.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• Isoform:

  P38α; p38β

• CAS Number:

  [2387505-88-4]