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Submit ReviewI-BET 151 dihydrochloride
说明： BET bromodomain inhibitor; also promotes differentiation of hiPSCs into megakaryocytes
化学名： 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydroxy-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one dihydrochloride
纯度： ≥98% (HPLC)
生物活性 for I-BET 151 dihydrochloride
I-BET 151 dihydrochloride is a BET bromodomain inhibitor; blocks recruitment of BET to chromatin. Induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively); reduces BCL2 expression in NOMO1 cells. Improves survival in two rodent models of MLL-fusion leukemia in vivo. Enhances differentiation of human iPSC into megakaryocytes. Also enhances fibroblast reprogramming to hiPSCs at low concentration.
For more information about how I-BET 151 dihydrochloride may be used, see our protocol: Transdifferentiating Fibroblasts into Neurons.
许可信息
Sold for research purposes under agreement from GlaxoSmithKline
External Portal Information for I-BET 151 dihydrochloride
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of I-BET 151 is reviewed on the chemical probes website.
化合物库 for I-BET 151 dihydrochloride
I-BET 151 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
技术数据 for I-BET 151 dihydrochloride
| 分子量 | 488.37 |
| 公式 | C23H21N5O3.2HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1883545-47-8 |
| PubChem ID | 170320 |
| InChI Key | IQOJZZHRYSSFJM-UHFFFAOYSA-N |
| Smiles | O=C(N3[C@H](C)C4=NC=CC=C4)NC2=C3C1=CC(OC)=C(C5=C(C)ON=C5C)C=C1N=C2.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for I-BET 151 dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 41.54 | 100 | |
| ethanol | 41.54 | 100 | |
| water | 48.84 | 100 |
制备储备液 for I-BET 151 dihydrochloride
以下数据基于产品分子量 488.37。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.05 mL | 10.24 mL | 20.48 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.1 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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产品说明书 for I-BET 151 dihydrochloride
参考文献 for I-BET 151 dihydrochloride
参考文献是支持产品生物活性的出版物。
Dawson et al (2011) Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 478 529 PMID: 21964340
Feng et al (2014) Scalable generation of universal platelets from human induced pluripotent stem cells. Stem Cell Reports 3 817 PMID: 25418726
Shao et al (2016) Reprogramming by de-bookmarking the somatic transcriptional program through targeting of BET bromodomains. Cell Rep. 16 3138 PMID: 27653680
If you know of a relevant reference for I-BET 151 dihydrochloride, please let us know.
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关键词: I-BET 151 dihydrochloride, I-BET 151 dihydrochloride supplier, I-BET151, epigenetics, bet, bromodomains, inhibits, inhibitors, chromatin, recruitment, readers, antileukemia, MLL, fusion, induces, apoptosis, Bromodomains, ESCs, and, iPSC, 4650, Tocris Bioscience
7 篇 I-BET 151 dihydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 I-BET 151 dihydrochloride 的部分引用包括：
Scott W et al (2017) Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and Lysosomal Function. Mol Cell 66 517-532.e9 PMID: 28525743
Bowry et al (2018) BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication. Cell Rep 25 2061 PMID: 30463005
Pengfei et al (2020) CRISPR-based gene knockout screens reveal deubiquitinases involved in HIV-1 latency in two Jurkat cell models. Sci Rep 10 5350 PMID: 32210344
Shao et al (2016) Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains. Cell Rep 16 3138 PMID: 27653680
Fernando et al (2023) Epigenetic inactivation of the 5-methylcytosine RNA methyltransferase NSUN7 is associated with clinical outcome and therapeutic vulnerability in liver cancer. Mol Cancer 22 83 PMID: 37173708
Xie et al (2018) β-actin regulates a heterochromatin landscape essential for optimal induction of neuronal programs during direct reprograming. PLoS Genet 14 e1007846 PMID: 30557298
Kumar et al (2015) GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1. Genes Dev 5 9489 PMID: 25807524
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I-BET 151 dihydrochloride 的评论
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By
Anonymous on 06/22/2020
分析类型： In Vitro
种属： Human
细胞系/组织： U2OS
I-BET151 (1 μM)
I used short treatments with I-BET151 in the presence of JQ1.
Reprogramming media with i-BET.
By
Anonymous on 02/23/2020
分析类型： In Vitro
种属： Mouse
细胞系/组织： ipsc
100 nM
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
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