Talmapimod (SCIO-469) 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 (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC 50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.

Solid

p38α 9 nM (IC50) p38β 90 nM (IC50u

Talmapimod (SCIO-469) (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells.
Talmapimod inhibits LPS-induced TNF-a production in human whole blood.
Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease.
Talmapimod inhibits multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models.
Talmapimod (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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
ClinicalTrial
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.