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ICG001

ICG001
ICG001 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.
Catalog No. T2237Cas No. 847591-62-2
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Purity:99.95%
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ICG001

Catalog No. T2237Cas No. 847591-62-2
ICG001 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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Pack SizePriceAvailabilityQuantity
1 mg$30In Stock
5 mg$64In Stock
10 mg$108In Stock
25 mg$218In Stock
50 mg$379In Stock
100 mg$588In Stock
500 mg$1,260In Stock
1 mL x 10 mM (in DMSO)$78In Stock
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Product Introduction

Bioactivity
Description
ICG001 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
ICG001 binds specifically to CBP but not the related transcriptional coactivator p300, thereby disrupting the interaction of CBP with β-catenin. Treatment with ICG001 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
ICG001 exhibits antitumor activity in the mouse xenograft models of colon cancer. The initial results of the Phase I clinic trial of ICG001 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 ICG001 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.
Chemical Properties
Molecular Weight548.63
FormulaC33H32N4O4
Cas No.847591-62-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 40 mg/mL (72.91 mM), Sonication is recommended.
Ethanol: 27.4 mg/mL (50 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.8227 mL9.1136 mL18.2272 mL91.1361 mL
5 mM0.3645 mL1.8227 mL3.6454 mL18.2272 mL
10 mM0.1823 mL0.9114 mL1.8227 mL9.1136 mL
20 mM0.0911 mL0.4557 mL0.9114 mL4.5568 mL
50 mM0.0365 mL0.1823 mL0.3645 mL1.8227 mL

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