| Identification | Back Directory | [Name]
T-3775440 hydrochloride | [CAS]
1422535-52-1 | [Synonyms]
T-3775440HCl
T 3775440;T3775440
T-3775440 hydrochloride | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C18H23ClN4O | [MDL Number]
MFCD31692337 | [MOL File]
1422535-52-1.mol | [Molecular Weight]
346.86 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 30.18 mg/mL (87.01 mM) | [form ]
Solid | [color ]
Light yellow to yellow | [InChI]
InChI=1/C18H22N4O.ClH/c1-22-11-14(10-20-22)18(23)21-15-6-4-13(5-7-15)16-8-17(16)19-9-12-2-3-12;/h4-7,10-12,16-17,19H,2-3,8-9H2,1H3,(H,21,23);1H/t16-,17+;/s3 | [InChIKey]
XYFPAGOQZFSLFH-NAHYZYKJNA-N | [SMILES]
N([C@@H]1C[C@H]1C1C=CC(NC(C2C=NN(C)C=2)=O)=CC=1)CC1CC1.Cl |&1:1,3,r| |
| Hazard Information | Back Directory | [Uses]
T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM. | [Biological Activity]
| Target | Value | LSD1
() | 2.1 nM |
| [Biological Activity]
T-3775440 hydrochloride is an irreversible LSD1 inhibitor. It is highly selective for LSD1 relative to other monoamine oxidases with IC50 of 2.1 nM. | [in vitro]
T-3775440 hydrochloride enhances the transdifferentiation of erythrocytes/megakaryocytes to granule-like monocytes. It disrupts the interaction of LSD1 and GFI1B. AEL (TF-1a, HEL92.1.7) cells and AMKL (CMK11-5, M07e) cells were treated with T-3775440 for 48 hours, which induced cell cycle arrest and apoptosis. In TF-1a and CMK11-5 cells, treatment with T-3775440 increased cells in G1 and sub-G1 phases. | [in vivo]
T-3775440 inhibits tumor growth in a mouse xenograft model of AML. In mice T-3775440 hydrochloride caused a transient decrease in platelets followed by a large rebound. After a single dose, it had no apparent effect on red blood cell counts. T-3775440 hydrochloride also exerted antitumor activity in AEL (HEL 92.1.7) model and AMKL (CMK11-5) model. | [IC 50]
KDM1/LSD1 | [storage]
Store at -20°C | [References]
[1] Ishikawa Y, et al. A Novel LSD1 Inhibitor T-3775440 Disrupts GFI1B-Containing Complex Leading to Transdifferentiation and Impaired Growth of AML Cells. Mol Cancer Ther. 2017 Feb;16(2):273-284. DOI:10.1158/1535-7163.MCT-16-0471 |
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| Company Name: |
BOC Sciences
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| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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