CAS NO: | 1431368-48-7 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
25mg | 电议 |
100mg | 电议 |
Cas No. | 1431368-48-7 |
化学名 | N-((1R,2S)-2-phenylcyclopropyl)piperidin-4-amine |
Canonical SMILES | C1(N[C@@H]2C[C@H]2C3=CC=CC=C3)CCNCC1 |
分子式 | C14H22Cl2N2 |
分子量 | 289.24 |
溶解度 | ≥ 11.55mg/mL in DMSO |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | GSK-LSD1 2HCl is a selective inhibitor of LSD1 with IC50 value of 16 nM [1]. 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 [1]. Reference: |