| CAS NO: | 581073-80-5 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 385.4 |
| Cas No. | 581073-80-5 |
| Formula | C22H15N3O4 |
| Solubility | ≤20mg/ml in DMSO;25mg/ml in dimethyl formamide |
| Chemical Name | 4-[2-(2-furanyl)-6-(4-nitrophenyl)-4-pyridinyl]-benzamide |
| Canonical SMILES | NC(C(C=C1)=CC=C1C2=CC(C3=CC=CO3)=NC(C4=CC=C([N+]([O-])=O)C=C4)=C2)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Target: MYC
Kd value: 6.5 ± 1.0 nM
KJ Pyr 9 is a novel small molecule inhibitor of MYC, with the Kd value of 6.5 ± 1.0 nM. Besides, KJ Pyr 9 also suppresses the formation of MYC-MAX and oncogenic transformation induced by MYC in cell culture [1].
In Vitro: In chicken embryo fibroblasts, KJ Pyr 9 was found to have the ability to interfere with the oncogenic activity of MYC, with the best aqueous solubility. Besides, in human B-cell line P493-6, 20 μM KJ Pyr 9 could significantly inhibit cell proliferation, and KJ Pyr 9 could also inhibit the proliferation of NCI-H460, MDA-MB-231, and SUM-159PT cell lines, with the IC50 values between 5-10 μM. Furthermore, treatment of P493-6 cells with KJ Pyr 9 could significantly suppress the transcription ability of MYC [1].
In Vivo: KJ Pyr 9 was found to have no acute toxicity in mouse and rat at a dose of 10 mg/kg, with an impressive ability to cross the blood-brain barrier. Besides, in a MDA-MB-231 cells xenograft tumor nude mice model, intraperitoneal injection with 10 mg/kg KJ Pyr 9 for 31 days could significantly inhibit tumor growth, while having no effect on the body weight [1].
Clinical trial: No data available recently.
Reference:
[1] Hart J R, Garner A L, Yu J, et al. Inhibitor of MYC identified in a Krohnke pyridine library[J]. Proceedings of the National Academy of Sciences, 2014, 111(34): 12556-12561.
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