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SM 16

CAS No. : 614749-78-9

MCE 站：SM 16

产品活性：SM 16 是 ALK5/ALK4 激酶抑制剂，K_i 值分别为10 和 1.5 nM。

研究领域：TGF-beta/Smad

作用靶点：TGF-β Receptor

In Vitro: SM 16 inhibits TGFβ-induced plasminogen activator inhibitor-luciferase activity (IC₅₀=64 nM) and TGFβ- or activin-induced Smad2 phosphorylation at concentrations between 100 and 620 nM. SM 16 is tested against >60 related and unrelated kinases and shows moderate off-target activity only against Raf (IC₅₀=1 μM) and p38/SAPKa (IC₅₀=0.8 μM). SM 16 exhibits no inhibitory activity against ALK family members ALK1 and ALK6.

In Vivo: SM 16 penetrates tumor cells in vivo, suppressing tumor phosphorylated Smad2/3 levels for at least 3 h following treatment of tumor-bearing mice with a single i.p. bolus of 20 mg/kg SM 16. The growth of established AB12 tumors is significantly inhibited by 5 mg/kg/d SM 16 (P<0.001) delivered via s.c. miniosmotic pumps over 28 days.

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