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SGI-1776 free base

CAS No. : 1025065-69-3

MCE 站：SGI-1776 free base

产品活性：SGI-1776 free base 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 free base (2.5, 5 μM) inhibits Pim-1 protein expression ａnd Pim-1 kinase activity in SACC cells. SGI-1776 free base (2.5, 5 μM) causes cell cycle arrest ａnd reduces cell proliferation in SACC-83 ａnd SACC-LM cells.
SGI-1776 free base (5 μM) inhibits cell migration ａnd invasiveness in both SACC-83 ａnd SACC-LM cells. SGI-1776 free base (0, 2.5, or 5 μM) induces apoptosis via Caspase-3 activation.
SGI-1776 free base (5 M) exerts inhibitory effects on both lipid accumulation ａnd TG synthesis without affecting the number of adipocytes.
SGI-1776 free base (5 M) inhibits adipogenesis particularly at an early phase of differentiation.
SGI-1776 free base (5 M) 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 free base shows the significant activity against HO-8910 cells in a dose-dependent manner, with IC₅₀ of (5.2±0.6) M, ａnd the inhibiting effect of SGI-1776 free base is sharply increased from 1.25 M to 20 M in vitro.
SGI-1776 free base inhibits the migration ａnd invasion of HO-8910 cells in a dose-dependent manner, ａnd the inhibiting migration ａnd invasion rate of 5 M.
SGI-1776 free base (2.5, 5 ａnd 10 M) 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 free base significantly inhibits cell viability, arrests cell in G1 phase, ａnd inhibits the migration ａnd invasion.

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

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