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抑制剂/激活剂

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凋亡与自噬

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SGI-1776 free base

SGI-1776 free base

SGI-1776 free base是一种新型的，ATP竞争性Pim1抑制剂，无细胞试验中IC50为7 nM，比作用于Pim2和Pim3选择性分别高50和10倍，也有效作用于Flt3和haspin。SGI-1776 可诱导凋亡和自噬。

货号：
TK0325
规格：

1mg

5mg
价格：
￥0.00

产品参数

CAS No.	1025065-69-3
生物活性	SGI-1776 is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.
分子式	C20H22F3N5O
分子量	405.42
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 125 mg/mL (308.32 mM; Need ultrasonic)
体内研究	SGI-1776 (75, 200 mg/kg, p.o.) shows potent and sustained antitumor activity in a dose dependent manner in MV-4-11 xenografts.
体外研究	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.
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纯度及产品资料	98%

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