产品描述: | ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. |
靶点: |
Wnt/beta-catenin;Epigenetic Reader Domain;EpigeneticReaderDomain;Wnt/beta-catenin |
体内研究: |
PRI-724 exhibits antitumor activity in the mouse xenograft models of colon cancer. The initial results of the Phase I clinic trial of PRI-724 has been disclosed publically. The drug exhibits an acceptable toxicity profile with only one dose-limiting toxicity of grade 3 reversible hyperbilirubinaemia. An Open-Label dose-escalation phase I/II study of PRI-724 for patients with advanced myeloid malignancies is still ongoing |
细胞实验: |
ICG-001 is dissolved in DMSO. To evaluate effects of ICG-001 on α-SMA and collagen type 1 expression, RLE-6TN cells are treated with TGF-β1 (0.25 ng/mL) in the presence or absence of ICG-001 (5.0 μM). After 24 h, cells are harvested and mRNA isolated for analysis by qPCR. RNA is reverse-transcribed using SuperScript reverse transcriptase. Quantitative PCR is performed with SYBR-Green PCR using Real-Time PCR System HT7900. The amplification protocol is set as follows: 95°C denaturation for 10 min followed by 40 cycles of 15-s denaturation at 95°C, 1 min of annealing/extension, and data collection at 60°C. |
参考文献: |
1.Yosuke Osawa, et al. EBioMedicine. 2015, 2(11):1751-1758. 2.Liu F, Yu F, Lu Y Z, et al. Crosstalk between pleural mesothelial cell and lung fibroblast contributes to pulmonary fibrosis[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research. 2020, 1867(11): 118806. 3.Sasaki T, et al. Transl Respir Med. 2:8. 4.Zhang X, et al. Am J Cancer Res. 2015, 5(8):2344-2360. |
溶解性: |
DMSO:54.9 mg/mL (100 mM) Ethanol:27.4 mg/mL (50 mM) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.823 ml |
9.114 ml |
18.227 ml |
5 mM |
0.365 ml |
1.823 ml |
3.645 ml |
10 mM |
0.182 ml |
0.911 ml |
1.823 ml |
50 mM |
0.036 ml |
0.182 ml |
0.365 ml |
|
注意: |
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