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Submit ReviewSGC-CBP30 is a potent CBP/p300 bromodomain (BRD) inhibitor (Kd values are 21 and 32 nM for CBP and p300 BRDs respectively). Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. Accelerates FRAP recovery in cells at a concentration of 1 μM. SGC-CBP30 can be used in protocols for the chemical reprogramming of somatic cells to iPSCs.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the SGC-CBP30 probe summary on the SGC website.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of SGC-CBP30 is reviewed on the chemical probes website.
SGC-CBP30 is also offered as part of the Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 509.04 |
公式 | C28H33ClN4O3 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1613695-14-9 |
PubChem ID | 72201027 |
InChI Key | GEPYBHCJBORHCE-SFHVURJKSA-N |
Smiles | CC1=C(C(C)=NO1)C2=CC=C3C(N=C(CCC4=CC(Cl)=C(OC)C=C4)N3C[C@@H](N5CCOCC5)C)=C2 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 100 | ||
ethanol | 100 |
以下数据基于产品分子量 509.04。 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 | 1.96 mL | 9.82 mL | 19.64 mL |
5 mM | 0.39 mL | 1.96 mL | 3.93 mL |
10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
参考文献是支持产品生物活性的出版物。
Gallenkamp et al (2014) Bromodomains and their pharmacological inhibitors. ChemMedChem 9 438 PMID: 24497428
Hay et al (2014) Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J.Am.Chem.Soc. 136 9308 PMID: 24946055
Hammitzsch et al (2015) CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proc.Natl.Acad.Sci.U.S.A. 112 10768 PMID: 26261308
Guan et al (2022) Chemical reprogramming of human somatic cells to pluripotent stem cells. Nature 605 325 PMID: 35418683
If you know of a relevant reference for SGC-CBP30, please let us know.
关键词: SGC-CBP30, SGC-CBP30 supplier, SGCCBP30, CREBBP, CBP, EP300, p300, bromodomains, inhibitors, inhibits, chemical, probes, epigenetics, SGC, potent, selective, active, in, cells, permeable, structural, genomics, consortium, induced, pluripotent, stem, reprogramming, iPSC, Bromodomains, Histone, Acetyltransferases, Stem, Cell, Reprogramming, 4889, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SGC-CBP30 的部分引用包括:
Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261
Koh et al (2018) A conserved enhancer regulates Il9 expression in multiple lineages. Nat Commun 9 4803 PMID: 30442929
Walter et al (2021) A Chemo-Genomic Approach Identifies Diverse Epigenetic Therapeutic Vulnerabilities in MYCN-Amplified Neuroblastoma. Front Cell Dev Biol 9 612518 PMID: 33968920
Laurent et al (2021) Network-Based Integration of Multi-Omics Data Identifies the Determinants of miR-491-5p Effects. Cancers (Basel) 13 PMID: 34439123
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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。
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.
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.