sAJM589
目录号 : GC38845sAJM589 是一种 Myc 抑制剂,能干扰 Myc- max 异二聚体的形成,其 IC50 值为 1.8 μM。
Cas No.:2089-82-9
Sample solution is provided at 25 µL, 10mM.
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sAJM589 is a Myc inhibitor which potently disrupts the Myc-Max heterodimer with an IC50 of 1.8 μM[1].
sAJM589 potently disrupts the Myc-Max heterodimer to reduce Myc protein levels in a dose dependent manner, with an IC50 of 1.8 μM[1].sAJM589 suppresses cellular proliferation in diverse Myc-dependent cancer cell lines and anchorage independent growth of Raji cells[1].
[1]. Choi SH, et al. Targeted Disruption of Myc-Max Oncoprotein Complex by a Small Molecule. ACS Chem Biol. 2017 Nov 17;12(11):2715-2719.
Cas No. | 2089-82-9 | SDF | |
Canonical SMILES | OC1=CC2=NC3=CC=CC=C3N=C2C4=CC=CC=C41 | ||
分子式 | C16H10N2O | 分子量 | 246.26 |
溶解度 | DMSO: 5 mg/mL (20.30 mM) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 4.0607 mL | 20.3037 mL | 40.6075 mL |
5 mM | 0.8121 mL | 4.0607 mL | 8.1215 mL |
10 mM | 0.4061 mL | 2.0304 mL | 4.0607 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Targeted Disruption of Myc-Max Oncoprotein Complex by a Small Molecule
ACS Chem Biol 2017 Nov 17;12(11):2715-2719.PMID:28976731DOI:10.1021/acschembio.7b00799.
Myc plays important roles in cell cycle progression, cell growth, and stem cell self-renewal. Although dysregulation of Myc expression is a hallmark of human cancers, there is no Myc targeted therapy yet. Here, we report sAJM589, a novel small molecule Myc inhibitor, identified from a PCA-based high-throughput screen. sAJM589 potently disrupts the Myc-Max heterodimer in a dose dependent manner with an IC50 of 1.8 ± 0.03 μM. sAJM589 preferentially inhibits transcription of Myc target genes in a Burkitt lymphoma cell model, P493-6. Genome-wide transcriptome analysis showed that sAJM589 treatment and Myc depletion induced similar gene expression profiles. Consistently, sAJM589 suppressed cellular proliferation in diverse Myc-dependent cancer cell lines and anchorage independent growth of Raji cells. Disruption of the Myc-Max interaction by sAJM589 reduced Myc protein levels, possibly by promoting ubiquitination and degradation of Myc. Collectively, these results suggest that sAJM589 may be a basis for the development of potential inhibitors of Myc-dependent cell growth.
Conjugate Addition of Carbon Acids to β,γ-Unsaturated α-Keto Esters: Product Tautomerism and Applications for Asymmetric Synthesis of Benzo[ a]phenazin-5-ol Derivatives
J Org Chem 2019 Nov 1;84(21):13824-13831.PMID:31566387DOI:10.1021/acs.joc.9b02021.
A correlation between the equilibrium ratio of tautomeric products generated by the asymmetric Michael reactions of cyclic carbon acids with β,γ-unsaturated α-keto esters and the chemical shift of the α-proton in starting nucleophilic substrates was revealed which makes equilibration predictable. New tetrahydropyran-fused benzo[a]phenazins were enantioselectively (up to 99% ee) synthesized from β,γ-unsaturated α-keto esters and benzo[a]phenazin-5-ol, a powerful anti-cancer agent sAJM589. Facile recyclability of catalyst Ia in the catalytic reactions was demonstrated.