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基本信息
PIM激酶抑制劑(SMI-16A)
SMI-16A
SMI 16A
SMI16A
PIM1/2 Kinase Inhibitor VI
SMI-16a(PIM1/2 Kinase Inhibitor VI)
2,4-Thiazolidinedione, 5-[(4-propoxyphenyl)methylene]-
物理化學(xué)性質(zhì)
常見問題列表
Target | Value |
Pim2
() | 20 nM |
Pim1
() | 150 nM |
SMI-16a has excellent potency for inhibition of both Pim-1 and Pim-2. Treatment with Pim-2 short-interference RNA as well as the Pim inhibitor SMI-16a successfully restores osteoblastogenesis suppressed by all the above inhibitory factors and MM cells. The SMI-16a treatment potentiates BMP-2-mediated anabolic signaling while suppressing TGF-β signaling.
Mice tolerate intraperitoneal dose of SMI-16a is 50 mg/kg daily for 5 days, while 100 mg/kg is overtly toxic. Treatment of the animals with SMI-16a for 5 days per week reduces the growth of tumors by approximately 50% and does not cause a loss of body weight. Subchronic dosing with SMI-16a does not affect the levels of red, white blood cells, including lymphocytes, monocytes, and granulocytes, indicating that the compound does not have myelosuppressive effects. SMI-16a does not have toxicity toward the liver as the albumin, alkaline phosphatase, and alanine aminotransferase levels are unchanged . SMI-16a effectively prevents bone destruction while suppressing MM tumor growth in MM animal models.