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ICG001

Catalog No. T2237   CAS 847591-62-2

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.

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ICG001 Chemical Structure
ICG001, CAS 847591-62-2
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
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Purity: 99.95%
Purity: 98.63%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 54.9 mg/mL (100 mM)

Ethanol: 27.4 mg/mL (50 mM)

TargetMolReferences and Literature

1. Sasaki T, et al. Transl Respir Med. 2:8. 2. Zhang X, et al. Am J Cancer Res. 2015, 5(8):2344-2360. 3. Yosuke Osawa, et al. EBioMedicine. 2015, 2(11):1751-1758. 4. 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.

TargetMolCitations

1. Liu F, Yu F, Lu Y Z, et al. Crosstalk between pleural mesothelial cell and lung fibroblast contributes to pulmonary fibrosis. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research. 2020, 1867(11): 118806. 2. Xiao K, Liu C, Wang H, et al.Umbilical cord mesenchymal stem cells overexpressing CXCR7 facilitate treatment of ARDS-associated pulmonary fibrosis via inhibition of Notch/Jag1 mediated by the Wnt/β-catenin pathway.Biomedicine & Pharmacotherapy.2023, 165: 115124. 3. Wang J, Sheng N, Li Y, et al.Ly6D facilitates chemoresistance in laryngeal squamous cell carcinoma through miR-509/β-catenin signaling pathway.American Journal of Cancer Research.2023, 13(5): 2155.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Colorectal Cancer Compound Library Drug Repurposing Compound Library NO PAINS Compound Library Stem Cell Differentiation Compound Library Anti-Obesity Compound Library Anti-COVID-19 Compound Library ReFRAME Related Library

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Keywords

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

 

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