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Talmapimod hydrochloride is a selective and ATP-competitive p38α inhibitor (IC50: 9 nM). It also shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
Talmapimod hydrochloride is a selective and ATP-competitive p38α inhibitor (IC50: 9 nM). It also shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 10,600 | 期货 |
产品描述 | Talmapimod hydrochloride is a selective and ATP-competitive p38α inhibitor (IC50: 9 nM). It also shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs. |
靶点活性 | p38α:9 nM, p38β:90 nM |
体外活性 | Talmapimod hydrochloride inhibits LPS-induced TNF-a production in human whole blood. Talmapimod hydrochloride decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells. Talmapimod hydrochloride (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells [1][2][3]. |
体内活性 | Talmapimod hydrochloride (10-90 mg/kg; P.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth. Talmapimod hydrochloride (10-90 mg/kg; P.o.; twice daily orally for 14 days) also dose-dependently reduced weight of the palpable tumors at termination [4]. |
别名 | SCIO-469 hydrochloride |
分子量 | 549.47 |
分子式 | C27H31Cl2FN4O3 |
CAS No. | 309915-12-6 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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