Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ICG001 (PRI-724 isomer) 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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 37.00 | |
2 mg | In stock | $ 50.00 | |
5 mg | In stock | $ 72.00 | |
10 mg | In stock | $ 131.00 | |
25 mg | In stock | $ 288.00 | |
50 mg | In stock | $ 403.00 | |
100 mg | In stock | $ 588.00 | |
500 mg | In stock | $ 1,280.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 131.00 |
Description | ICG001 (PRI-724 isomer) 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. |
Targets&IC50 | CBP:3 μM |
In vitro | PRI-724 binds specifically to CBP but not the related transcriptional coactivator p300, thereby disrupting the interaction of CBP with β-catenin. Treatment with PRI-724 selectively induces apoptosis in colon carcinoma cells but not in normal colonic epithelial cells and reduces in vitro growth of colon carcinoma cells[1][2]. |
In vivo | 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[2]. |
Cell Research | 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. |
Molecular Weight | 548.63 |
Formula | C33H32N4O4 |
CAS No. | 847591-62-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 54.9 mg/mL (100 mM)
Ethanol: 27.4 mg/mL (50 mM)
You can also refer to dose conversion for different animals. More
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ICG001 847591-62-2 Chromatin/Epigenetic Cytoskeletal Signaling Stem Cells Epigenetic Reader Domain Wnt/beta-catenin 780757-88-2 PRI 724 ICG 001 PRI724 ICG-001 inhibitor inhibit