ICG-001

SKU: orb1305968

特色

描述

ICG001 is a selective CBP/β-catenin antagonist that inhibits Wnt-responsive transcription with an IC50 of 3 μM. It is a valuable chemical probe for studying Wnt/β-catenin signaling in cancer research and has been utilized in both cellular and animal models of tumorigenesis.

研究领域

Cell Biology, Neuroscience, Stem Cell & Developmental Biology

图片与验证

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关键属性

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CAS 号	847591-62-2
MW	548.63
纯度	>98%
分子式	C₃₃H₃₂N₄O₄
SMILES	Oc1ccc(C[C@@H]2N3[C@H](CN(Cc4cccc5ccccc45)C2=O)N(CCC3=O)C(=O)NCc2ccccc2)cc1
靶点	Transcription factor
溶解性	Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 25 mg/ml)

生物活性

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靶点 IC50	CBP:3 μM
体内	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.
体外	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.
细胞研究	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.

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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Epigenetic Reader Domain, EpigeneticReaderDomain, ICG001, ICG-001, ICG 001, CBP, beta-catenin, betacatenin, 780757-88-2, 847591-62-2, bcatenin, PRI 724, PRI724, PRI-724, PRI-724 isomer, Wnt/β-catenin, Wnt/b-catenin, Wnt/betacatenin, Wnt, βcatenin

相似产品

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PRI-724 [orb1685665]
纯度：
99.11% (May vary between batches)
CAS 号：
1422253-38-0
MW:
658.64
分子式：
C₃₃H₃₅N₆O₇P
可选规格： 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 ml x 10 mM (in DMSO)
ICG-001 [orb1710780]
纯度：
>99.99% (May vary between batches)
CAS 号：
780757-88-2
MW:
548.63
分子式：
C₃₃H₃₂N₄O₄
可选规格： 5 mg, 10 mg, 50 mg, 100 mg, 1 mg, 500 mg, 1 ml x 10 mM (in DMSO), 25 mg
PRI-724 [orb1223869]
纯度：
>98% (HPLC)
CAS 号：
847591-62-2
MW:
548.63
分子式：
C₃₃H₃₂N₄O₄
可选规格： 5 mg, 25 mg, 100 mg, 500 mg, 1 g, 2 mg, 50 mg, 10 mg

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

11238147 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

纯度：	99.11% (May vary between batches)
CAS 号：	1422253-38-0
MW:	658.64
分子式：	C₃₃H₃₅N₆O₇P

纯度：	>99.99% (May vary between batches)
CAS 号：	780757-88-2
MW:	548.63
分子式：	C₃₃H₃₂N₄O₄

纯度：	>98% (HPLC)
CAS 号：	847591-62-2
MW:	548.63
分子式：	C₃₃H₃₂N₄O₄

ICG-001

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

PRI-724 [orb1685665]

ICG-001 [orb1710780]

PRI-724 [orb1223869]

质量保证

化合物标识

关键属性

实验方案信息

可选规格