| CAS NO: | 442-51-3 |
| 包装: | 500mg |
| 市场价: | 500元 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 212.25 |
| Cas No. | 442-51-3 |
| Formula | C13H12N2O |
| Solubility | insoluble in H2O; ≥33 mg/mL in DMSO with ultrasonic; ≥6.35 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 7-methoxy-1-methyl-9H-pyrido[3,4-b]indole |
| Canonical SMILES | CC1=NC=CC2=C1NC3=C2C=CC(OC)=C3 |
| 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。 |
骆驼蓬碱 (Harmine) ，分离自骆驼蓬种子，是β-carboline家族的一种生物碱，通过对Wnt信号通路的抑制可以调节PPARγ的表达。它还选择性地与MAO-A结合，可逆地抑制单胺氧化酶A (MAO-A)，但对MAO-B没有抑制作用[3]。
Harmine对肝癌细胞具有严重的细胞毒性，是一种很有前景的抗癌药物[4]。
参考文献：
[1] Smith B, Medda F, Gokhale V, et al. Recent Advances in theDesign, Synthesis, and BiologicalEvaluation of Selective DYRK1A Inhibitors: A New Avenue for a DiseaseModifying Treatment of Alzheimer’s?[J]. Acs Chemical Neuroscience, 2012, 3(11):857-72.
[2] Waki H, Park K W, Mitro N, et al. The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARgamma expression.[J]. Cell Metabolism, 2007, 5(5):357-370.
[3] Ginovart N, Meyer J H, Boovariwala A, et al. Positron emission tomography quantification of |[lsqb]|11C|[rsqb]|-harmine binding to monoamine oxidase-A in the human brain[J]. Journal of Cerebral Blood Flow & Metabolism Official Journal of the International Society of Cerebral Blood Flow & Metabolism, 2006, 26(3):330-44.
[4] Zhang L, Zhang F, Zhang W, et al. Harmine suppresses homologous recombination repair and inhibits proliferation of hepatoma cells[J]. Cancer Biology & Therapy, 2015, 16(11):1585-1592.
| 有效的、选择性抑制剂，针对靶点DYRK1A, DYRK3,DYRK2的IC50值分别是80, 800,900 nM[1]。通过对Wnt信号通路的抑制可以调节PPARγ的表达[2]。 | ||||||
| 靶点 | DYRK1A | DYRK3 | DYRK2 | PPARγ | ||
| IC50 | 80nM | 800nM | 900nM | -- | ||
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