Talmapimod hydrochloride
Based on 3 publication(s) in Google Scholar
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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2387505-88-4
- 分子式: C27H31Cl2FN4O3
- 分子量:549.46
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Talmapimod hydrochloride
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生物活性
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p38α 9 nM (IC50) |
p38β 90 nM (IC50) |
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.
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Cell Line:MM.1S, U266, RPMI8226, MM.1R, and RPMI-Dox40 cell lines
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Concentration:100, 200 nM
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Incubation Time:1 hour
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Result:Strongly inhibits phosphorylation of p38 MAPK.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)[4]
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Dosage:10, 30, 90 mg/kg
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Administration:P.o.; twice daily orally for 14 days
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Result:Dose-dependently reduced tumor growth.
化学情報
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CAS 番号 2387505-88-4
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分子量 549.46
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分子式 C27H31Cl2FN4O3
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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
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別名
SCIO-469 hydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Talmapimod hydrochloride 関連分類
HY-10406A 関連分類
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