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Submit ReviewL Moses dihydrochloride
说明： High affinity and selective PCAF bromodomain inhibitor
化学名： (1S, 2S)-N1,N1-Dimethyl-N2-(3-methyl-1,2,4-triazolo[3,4-a]phthalazin-6-yl)-1-phenylpropane-1,2-diamine dihydrochloride
纯度： ≥98% (HPLC)
生物活性 for L Moses dihydrochloride
L Moses dihydrochloride is a high affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM), which exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). L Moses exhibits >4500-fold selectivity for PCAF over BRD4. The compound inhibits Tunicamycin (Cat. No. 3516) -induced neuronal cell death by reversing the transcriptional changes associated with Tunicamycin treatment. L Moses exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC).
许可信息
This compound is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the L-Moses probe summary on the SGC website.
External Portal Information for L Moses dihydrochloride
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of L-Moses is reviewed on the chemical probes website.
化合物库 for L Moses dihydrochloride
L Moses dihydrochloride 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 L Moses dihydrochloride
| 分子量 | 433.38 |
| 公式 | C21H24N6.2HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2922480-38-2 |
| PubChem ID | 131698638 |
| InChI Key | MSFPLTWUFWOKBX-IFXJQAMLSA-N |
| Smiles | C[C@@H]([C@H](C1=CC=CC=C1)N(C)C)NC2=NN3C(C)=NN=C3C4=CC=CC=C24 |
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 L Moses dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 100 | ||
| DMSO | 100 |
制备储备液 for L Moses dihydrochloride
以下数据基于产品分子量 433.38。 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 | 2.31 mL | 11.54 mL | 23.07 mL |
| 5 mM | 0.46 mL | 2.31 mL | 4.61 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.31 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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产品说明书 for L Moses dihydrochloride
参考文献 for L Moses dihydrochloride
参考文献是支持产品生物活性的出版物。
Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 PMID: 27966810
Pavlou et al (2023) CRISPR-Cas9 genetic screen leads to the discovery of L-Moses, a KAT2B inhibitor that attenuates Tunicamycin-mediated neuronal cell death. Sci Rep 13 3934 PMID: 36894612
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关键词: L Moses dihydrochloride, L Moses dihydrochloride supplier, PCAF, p300/CBP-associated, factor, GCN5, general, control, non-derepressible, 5, inhibitors, inhibits, high, affinity, selective, cell-permeable, 2079885-05-3, KAT2B, lysine, acetyltransferase, 2B, neuroprotectant, neuroprotection, Bromodomains, 6251, Tocris Bioscience
1 篇 L Moses dihydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 L Moses dihydrochloride 的部分引用包括：
Pavlou et al (2023) CRISPR-Cas9 genetic screen leads to the discovery of L-Moses, a KAT2B inhibitor that attenuates Tunicamycin-mediated neuronal cell death. Sci.Rep. 13 3934 PMID: 36894612
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