| Name | ICG001 |
| 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. |
| 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. |
| 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]. |
| Storage | Powder: -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)
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| Keywords | 780757-88-2 | PRI 724 | ICG 001 | 847591-62-2 | ICG001 | PRI724 | ICG-001 |
| Inhibitors Related | ABBV-744 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | Urea | (+)-JQ-1 | Wnt pathway activator 1 | CHIR-99021 | Curcumin | XAV-939 | dBET6 | Naphthol AS-E | Nefopam hydrochloride | Bisdemethoxycurcumin |
| Related Compound Libraries | Neural Regeneration Compound Library | Histone Modification Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Stem Cell Differentiation Compound Library | Cytoskeletal Signaling Pathway Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
