GSK-LSD1 2HCl
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:
[1]. Structural Genomics Consortium.
http://www. thesgc.org/chemical-probes/LSD1.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 289.24 |
| Cas No. | 2102933-95-7 |
| Formula | C14H22Cl2N2 |
| Solubility | ≥11.55 mg/mL in DMSO |
| Chemical Name | N-((1R,2S)-2-phenylcyclopropyl)piperidin-4-amine |
| SDF | Download SDF |
| Canonical SMILES | C1(N[C@@H]2C[C@H]2C3=CC=CC=C3)CCNCC1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
- View current batch:
Chemical structure
