SGI-1776 | CAS:1025065-69-3

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のSGI-1776(CAS:1025065-69-3)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:SGI-1776; 
Cat. No. :CS-0513
CAS No. :1025065-69-3
Formula:C20H22F3N5O
M. Wt. : 405.42
Solubility:10 mM in DMSO

SGI-1776 is an inhibitor of Pim kinases, with IC50 of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.IC50 & Target: Ki: 7 nM (Pim-1), 363 nM (Pim-2), 69 nM (Pim-3)[4]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[1]. 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[2]. 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[3]. 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[4].

Xie J, et al. SGI-1776, an imidazo pyridazine compound, inhibits the proliferation of ovarian cancer cells by inactivating Pim-1. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2014 Jul;39(7):649-57. Park YK, et al. The novel anti-adipogenic effect and mechanisms of action of SGI-1776, a Pim-specific inhibitor, in 3T3-L1 adipocytes. Int J Mol Med. 2016 Jan;37(1):157-64. Chen LS, et al. Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia. Blood, 2011, 118(3), 693-702. Hou X, et al. Biochemical changes of salivary gland adenoid cystic carcinoma cells induced by SGI-1776. Exp Cell Res. 2017 Mar 15;352(2):403-411.