Talmapimod hydrochloride   (Synonyms: SCIO-469 hydrochloride )

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].

Talmapimod (SCIO-469) hydrochloride (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells^[1].
Talmapimod hydrochloride inhibits LPS-induced TNF-a production in human whole blood^[2].
Talmapimod hydrochloride decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Talmapimod hydrochloride (10-90 mg/kg; P.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

549.46

C₂₇H₃₁Cl₂FN₄O₃

2387505-88-4

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

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]