rel-Talmapimod hydrochloride
Based on 3 publication(s) in Google Scholar
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).
For research use only. We do not sell to patients.
- CAS No.: 879132-01-1
- Formula: C27H31Cl2FN4O3
- Molecular Weight:549.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) rel-Talmapimod hydrochloride
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Biological Activity
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p38α MAPK 9 nM (IC50) |
p38β MAPK 90 nM (IC50) |
IL-6 |
IL-1β |
Chemical Information
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CAS No. 879132-01-1
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Molecular Weight 549.46
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Formula C27H31Cl2FN4O3
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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
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Synonyms
rel-SCIO-469 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell
2020 Aug 6;182(3):685-712.e19. PMID: 32645325 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Cell Biol Toxicol
The 14-3-3η/GSK-3β/β-catenin complex regulates EndMT induced by 27-hydroxycholesterol in HUVECs and promotes the migration of breast cancer cells. [Abstract]2021 Aug;37(4):515-529. PMID: 33131013
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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