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SMI-16a

CAS No. : 587852-28-6

MCE 站：SMI-16a

产品活性：SMI-16a是选择性的 Pim 激酶抑制剂，对Pim1，Pim2 和 PC3 细胞的IC₅₀值分别为0.15，0.02 和48 μM。

研究领域：JAK/STAT Signaling

作用靶点：Pim

In Vitro: 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.

In Vivo: 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.

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  PIM-447 dihydrochloride  |  Pim1/AKK1-IN-1  |  Hispidulin  |  TCS-PIM-1-4a  |  TCS PIM-1 1  |  Quercetagetin  |  M-110  |  CK2/ERK8-IN-1  |  CK2/PIM1-IN-1  |  CX-6258 hydrochloride  |  R8-T198wt

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