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CAS No. : 587852-28-6
MCE 国际站: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 | Anti-Cancer Metabolism Compound Library | Anti-Obesity Compound Library | Targeted Diversity Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | GDC-0339 | Pim-1 kinase inhibitor 3 | (1S,3R,5R)-PIM447 dihydrochloride | Quercetagetin | MNK/PIM-IN-1 | HS56 | Pim-1 kinase inhibitor 1 | PIM1-IN-3 | Pim1/AKK1-IN-1 | CK2/ERK8-IN-1 | TP-3654 | Hispidulin | R8-T198wt | PIM-1/HDAC-IN-1 | PIM1-IN-6 | SMI-4a | GNE-955 | PIM1-IN-1 | AZD1208 hydrochloride | Uzansertib | Pim-1/2 kinase inhibitor 1 | PIM1-IN-7 | HTH-01-091 | SGI-1776 free base | Pim-1 kinase inhibitor 6 | CDK6/PIM1-IN-1 | M-110
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货号: HY-101947
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