S89234 |
GSK-LSD1 2HCl |
源叶(MedMol) | 98% |
- 产品描述: GSK-LSD1 2HCl is a selective inhibitor of LSD1 with IC50 value of 16 nM . Lysine (K) -specific demethylase 1A (LSD1) is a flavin-dependent histone demethylase that demethylates mono- and di-methylated lysines and plays an important role in oocyte growth, embryogenesis and tissue-specific differentiation. LSD1 plays a role in acute myeloid leukemia (AML). GSK-LSD1 2HCl irreversibly inhibited LSD1 with IC50 value of 16 nM and is > 1000 fold selective over LSD2, MAO-A and MAO-B, which were related to FAD utilizing enzymes. In cancer cell lines, GSK-LSD1 2HCl changed gene expression with average EC50 value < 5 nM and inhibited cells growth with average EC50 value < 5 nM. GSK-LSD1 2HCl (10 ?M) inhibited human recombinant dopamine transporter, 5-HT1A and 5-HT transporter by 39%, 49% and 74%, respectively. And no activity against other 55 recombinant receptors (GPCR, transporters, ion channels). GSK-LSD1 2HCl can be used as a chemical probe and a part of the SGC epigenetics
- 靶点: HistoneDemethylase
- 体外研究:
GSK-LSD1 induces gene expression changes in cancer cell lines with average EC50 of < 5 nM and inhibits cancer cell line growth with average EC50 of < 5 nM. [1]
- 参考文献:
1. Structural Genomics Consortium.http://www. thesgc.org/chemical-probes/LSD1.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.457 ml 17.287 ml 34.573 ml 5 mM 0.691 ml 3.457 ml 6.915 ml 10 mM 0.346 ml 1.729 ml 3.457 ml 50 mM 0.069 ml 0.346 ml 0.691 ml
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输入产品批号:
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)