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SGI-1776

CAS No. : 1025065-69-3

MCE 站：SGI-1776

产品活性：SGI-1776 是一种 Pim 抑制剂，抑制 Pim-1，Pim-2 和 Pim-3 的活性，IC₅₀ 值分别为 7 nM，363 nM 和 69 nM。

研究领域：JAK/STAT Signaling  |  Autophagy  |  Apoptosis

作用靶点：Pim  |  Autophagy  |  Apoptosis

In Vitro: SGI-1776 (2.5, 5 μM) inhibits Pim-1 protein expression ａnd Pim-1 kinase activity in SACC cells. SGI-1776 (2.5, 5 μM) causes cell cycle arrest ａnd reduces cell proliferation in SACC-83 ａnd SACC-LM cells. SGI-1776 (5 μM) inhibits cell migration ａnd invasiveness in both SACC-83 ａnd SACC-LM cells. SGI-1776 (0, 2.5, or 5 μM) induces apoptosis via Caspase-3 activation. SGI-1776 (5 µM) exerts inhibitory effects on both lipid accumulation ａnd TG synthesis without affecting the number of adipocytes. SGI-1776 (5 µM) inhibits adipogenesis particularly at an early phase of differentiation. SGI-1776 (5 µM) decreases the expression of C/EBP-α ａnd PPAR-γ ａnd the phosphorylation levels of STAT-3 during adipocyte differentiation, ａnd downregulates the protein and/or mRNA expression of FAS, leptin ａnd RANTES during adipocyte differentiation. SGI-1776 shows the significant activity against HO-8910 cells in a dose-dependent manner, with IC₅₀ of (5.2±0.6) µM, ａnd the inhibiting effect of SGI-1776 is sharply increased from 1.25 µM to 20 µM in vitro. SGI-1776 inhibits the migration ａnd invasion of HO-8910 cells in a dose-dependent manner, ａnd the inhibiting migration ａnd invasion rate of 5 µM. SGI-1776 (2.5, 5 ａnd 10 µM) decreases Pim-1 kinase activity of HO-8910 cells in a dose-dependent manner. Furthermore, the down-regulation of Pim-1 expression by SGI-1776 significantly inhibits cell viability, arrests cell in G1 phase, ａnd inhibits the migration ａnd invasion.

In Vivo: SGI-1776 (75, 200 mg/kg, p.o.) shows potent ａnd sustained antitumor activity in a dose dependent manner in MV-4-11 xenografts.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  Angiotensin II human  |  Acetylcysteine  |  SP600125  |  5-Fluorouracil  |  Staurosporine  |  Bortezomib  |  Tamoxifen  |  2-Deoxy-D-glucose  |  Gemcitabine  |  Verteporfin  |  Temozolomide  |  Decitabine  |  BAY 11-7082  |  Etoposide  |  CCCP  |  DAPT  |  Rote  |  Etomoxir  |  Stattic  |  Docetaxel  |  Fulvestrant  |  Everolimus  |  Resveratrol

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