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sAJM589 Sale

目录号 : GC38845

sAJM589 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。

sAJM589 Chemical Structure

Cas No.:2089-82-9

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1mg
¥360.00
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5mg
¥1,080.00
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10mg
¥1,710.00
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50mg
¥6,030.00
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100mg
¥9,630.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

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
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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
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Research Update

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.