Talmapimod hydrochloride(Synonyms: SCIO-469 hydrochloride)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Talmapimod hydrochloride (Synonyms: SCIO-469 hydrochloride)

Talmapimod (SCIO-469) hydrochloride 是 p38α 选择性的，具有口服活性的，ATP 竞争性的抑制剂，IC50 值是 9 nM，约为 p38β 的 10 倍，在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。

Talmapimod hydrochloride(Synonyms: SCIO-469 hydrochloride)

Talmapimod hydrochloride Chemical Structure

CAS No. : 309915-12-6

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Talmapimod hydrochloride 的其他形式现货产品:

Talmapimod

生物活性

Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs[1][2][3].

IC50 & Target

p38α

9 nM (IC50)

p38β

90 nM (IC50)

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MM.1S, U266, RPMI8226, MM.1R, and RPMI-Dox40 cell lines
Concentration: 100, 200 nM
Incubation Time: 1 hour
Result: Strongly inhibits phosphorylation of p38 MAPK.

体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)[4]
Dosage: 10, 30, 90 mg/kg
Administration: P.o.; twice daily orally for 14 days
Result: Dose-dependently reduced tumor growth.

Clinical Trial

分子量

549.46

Formula

C27H31Cl2FN4O3
CAS 号

309915-12-6
中文名称

他匹莫德盐酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

    [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.

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