产品说明书

ICG-001

Print
Chemical Structure| 780757-88-2 同义名 : -
CAS号 : 780757-88-2
货号 : A146696
分子式 : C33H32N4O4
纯度 : 99%+
分子量 : 548.632
MDL号 : MFCD12196918
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(91.14 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+50% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
描述 CBP has acetyltransferase activity and affects cell proliferation and differentiation. CBP and the closely related p300 are recruited Wnt-responsive promotes through interactions with the C-terminal half of β-catenin. PRI 724 is a novel inhibitor for Wnt/β-catenin/CBP pathway with IC50 value of 150nM[1]. In vitro, PRI 724 exhibited concentration dependent cytotoxicity in concentration range of 5-100μM to head and neck carcinoma lines BICR6, UM-SCC-1, and oral keratinocyte cell lines CAL27, FaDu, H314, SCC-25, OKF4/TERT-1. PRI 724 also reduced the transcript level of Wnt target genes Axin2, MMP7, and BIRC5 in these cells. Treatment with 20μM PRI 724 showed ability to inhibit the migration of BICR6, CAL27, FaDu and SCC-25 cells. In addition, PRI 724 reduced the percentage of G0/G1 cells in CAL27, SCC-25 and UM-SCC-1 cell lines, but slightly increased the percentage of G0/G1 cells in the FaDu cell linePMID: 31089983. In vivo, administration of 30mg/kg PRI 724 once daily significantly improved the overall survival of the leukemia-bearing NSG mice[2]. Subcutaneous administration of 10mg/kg PRI 724 once daily for 5 days ameliorated bleomycin-induced pulmonary fibrosis in mice[3].
作用机制 PRI 724 specifically disruption the interaction of CBP and β-catenin to inhibit Wnt/β-catenin/ CBP signaling pathway[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.82mL

0.36mL

0.18mL

9.11mL

1.82mL

0.91mL

18.23mL

3.65mL

1.82mL
参考文献

[1]Feng C. Lysophosphatidylcholine acyltransferase 3 deficiency impairs 3T3L1 cell adipogenesis through activating Wnt/β-catenin pathway. Biochim Biophys Acta Mol Cell Biol Lipids. 2018 Aug;1863(8):834-843. doi: 10.1016/j.bbalip.2018.04.008. Epub 2018 Apr 17.

[2]Zhou H. Combined inhibition of β-catenin and Bcr-Abl synergistically targets tyrosine kinase inhibitor-resistant blast crisis chronic myeloid leukemia blasts and progenitors in vitro and in vivo. Leukemia. 2017 Oct;31(10):2065-2074. doi: 10.1038/leu.2017.87. Epub 2017 Mar 21.

[3]Okazaki H. The novel inhibitor PRI-724 for Wnt/β-catenin/CBP signaling ameliorates bleomycin-induced pulmonary fibrosis in mice. Exp Lung Res. 2019 Sep;45(7):188-199. doi: 10.1080/01902148.2019.1638466.