InformationT-3775440 HCl T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L.TargetsLSD1 2.1 nMIn vitroT-3775440 treatment enforces transdifferentiation of erythroid/megakaryocytic lineages into granulomonocytic-like lineage cells. T-3775440 disrupts the interaction between LSD1 and growth factor-independent 1B (GFI1B), a transcription factor critical for the differentiation processes of erythroid and megakaryocytic lineage cells. 48-hour T-3775440 treatment induces cell-cycle arrest and apoptosis in AEL (TF-1a, HEL92.1.7) and AMKL cell lines (CMK11-5, M07e). T-3775440 treatment increases the G1 and sub-G1 phase populations in TF-1a and CMK11-5 cells.In vivoT-3775440 exerts tumor growth suppression in in vivo mouse xenograft models of AML. In mice, T-3775440 treatment results in a transient reduction in platelets, followed by a significant rebound. There is no obvious effect on red blood cell counts following a single administration. T-3775440 also exhibits potent antitumor effects in an additional AEL model of HEL 92.1.7 and an AMKL model of CMK11-5, possessing profound anti-AEL and anti-AMKL activity.Cell Research(from reference)Cell lines:TF-1a and CMK11-5 cells Concentrations:0, 10, 50 nM (TF-1a cells); 0, 20, 100 nM (CMK11-5 cells) Incubation Time:24 and 48 h.
Specifications and Purity: ≥99%
Molecular Formula: C18H23ClN4O
Molecular Weight: 346.85
PubChem CID: 86729932
Isomeric SMILES: CN1C=C(C=N1)C(=O)NC2=CC=C(C=C2)[C@@H]3C[C@H]3NCC4CC4.Cl
- UPC:
- 41105600
- Condition:
- New
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- T414009-10mg
- CAS:
- 1422535-52-1
- Product Size:
- 10mg
akash.verma@cenmed.com
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