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Submit ReviewA 485
说明： Potent and selective p300/CBP inhibitor; orally bioavailable
化学名： (1R)-N-[(4-Fluorophenyl)methyl]-2,3-dihydro-5-[[(methylamino)carbonyl]amino]-2',4'-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]spiro[1H-indene-1,5'-oxazolidine]-3'-acetamide
纯度： ≥98% (HPLC)
生物活性 for A 485
A 485 is a potent and selective p300/CREB-binding protein (CBP) HAT domain inhibitor (IC50 values are 2.6 and 9.8 nM for the CBP-bromodomain HAT-C/H3 (BHC) and p300-BHC domains, respectively), which displays > 1000-fold selectivity over closely related HATs. A 485 suppresses proliferation in several hematological malignancies and AR+ prostate cancer cell lines in vitro, and also inhibits tumor growth in a castration-resistant prostate cancer xenograft model. A 485 is orally bioavailable.
To request the negative control for A 485, please fill out the A 486 request form on the SGC website.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the A-485 probe summary on the SGC website.
External Portal Information for A 485
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A 485 is reviewed on the chemical probes website.
化合物库 for A 485
A 485 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for A 485
| 分子量 | 536.48 |
| 公式 | C25H24F4N4O5 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1889279-16-6 |
| PubChem ID | 118958122 |
| InChI Key | VRVJKILQRBSEAG-LFPIHBKWSA-N |
| Smiles | CNC(NC1=CC=C2C(CC[C@@]23OC(N(C3=O)CC(N([C@H](C(F)(F)F)C)CC4=CC=C(C=C4)F)=O)=O)=C1)=O |
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 A 485
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 53.65 | 100 | |
| ethanol | 53.65 | 100 |
制备储备液 for A 485
以下数据基于产品分子量 536.48。 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 | 1.86 mL | 9.32 mL | 18.64 mL |
| 5 mM | 0.37 mL | 1.86 mL | 3.73 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.86 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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产品说明书 for A 485
参考文献 for A 485
参考文献是支持产品生物活性的出版物。
Lasko et al (2017) Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature 550 128 PMID: 28953875
Kodadek et al (2018) Another one (of the "undruggable" targets) bites the dust: discovery of a potent and selective inhibitor of the histone acetyl transferase p300/CBP. Biochemistry 57 899 PMID: 29244478
Weinert et al (2018) Time-Resolved Analysis Reveals Rapid Dynamics and Broad Scope of the CBP/p300 Acetylome. Cell. PMID: 29804834
If you know of a relevant reference for A 485, please let us know.
按产品操作查看相关产品
关键词: A 485, A 485 supplier, A485, inhibitors, inhibits, histone, acetyltransferase, HAT, PCAF, p300, HSCs, potent, selective, androgen, receptor-positive, prostate, CBP, Histone, Acetyltransferases, 6387, Tocris Bioscience
13 篇 A 485 的引用文献
引用文献是使用了 Tocris 产品的出版物。 A 485 的部分引用包括：
Jing et al (2019) The Acetylation of Lysine-376 of G3BP1 Regulates RNA Binding and Stress Granule Dynamics. Mol Cell Biol 39 PMID: 31481451
Stephen J et al (2019) Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. J Pharmacol Exp Ther 370 219-230 PMID: 31189728
Lynda K et al (2022) A mitotic chromatin phase transition prevents perforation by microtubules. Nature 609 183-190 PMID: 35922507
Adriana et al (2022) 3D chromatin remodeling potentiates transcriptional programs driving cell invasion. Proc Natl Acad Sci U S A 119 e2203452119 PMID: 36037342
Anusha et al (2022) Oncohistone Mutations Occur at Functional Sites of Regulatory ADP-Ribosylation. Cancer Res 82 2361-2377 PMID: 35472077
Asgerally T et al (2020) ARID1A Mutations Promote P300-Dependent Endometrial Invasion through Super-Enhancer Hyperacetylation. Cell Rep 33 108366 PMID: 33176148
Masaya et al (2020) Acetylation-dependent regulation of PD-L1 nuclear translocation dictates the efficacy of anti-PD-1 immunotherapy. Nat Cell Biol 22 1064-1075 PMID: 32839551
Peggie et al (2021) The single-cell epigenomic and transcriptional landscape of immunity to influenza vaccination. Cell 184 3915-3935.e21 PMID: 34174187
Johan et al (2021) The transcriptional coactivator CBP/p300 is an evolutionarily conserved node that promotes longevity in response to mitochondrial stress. Nat Aging 1 165-178 PMID: 33718883
Rebecca et al (2021) Nuclear ADP-ribosylation drives IFNγ-dependent STAT1α enhancer formation in macrophages. Nat Commun 12 3931 PMID: 34168143
Marc et al (2021) Extracellular signal-regulated kinase mediates chromatin rewiring and lineage transformation in lung cancer. Elife 10 PMID: 34121659
Hubertus et al (2021) A unique bipartite Polycomb signature regulates stimulus-response transcription during development. Nat Genet 53 379-391 PMID: 33603234
Aristotelis et al (2021) H3K27ac bookmarking promotes rapid post-mitotic activation of the pluripotent stem cell program without impacting 3D chromatin reorganization. Mol Cell 81 1732-1748.e8 PMID: 33730542
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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。
Epigenetics Scientific Review
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.