Home Methylation LSD1 inhibitor - Histone Demethylase inhibitor T-3775440 HCl For research use only.

T-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.

T-3775440 HCl Chemical Structure

T-3775440 HCl Chemical Structure

CAS: 1422535-52-1

Purity & Quality Control

Batch: S843801 DMSO] 69 mg/mL] false] Water] 22 mg/mL] false] Ethanol] Insoluble] false Purity: 99.80%
99.80

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Biological Activity

Description 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.
Targets
LSD1 [1]
2.1 nM
In vitro
In vitro

T-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[1].
Cell Research 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
Method

TF-1a and CMK11-5 cells are treated with the indicated concentration of T-3775440 for 24 or 48 hours. Treated cells are subsequently harvested and lysed to prepare total lysates. Immunoblotting analyses are performed to determine the expression levels of p27, cleaved PARP, and β-actin in the cell lysates.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p27 / cPARP 27903753
Growth inhibition assay IC50 27903753
In Vivo
In vivo

T-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[1].
Animal Research Animal Models Female C.B17/Icr-scid/scid Jcl mice subcutaneously (s.c.) inoculated in the flank with AML cells
Dosages 15-20 mg/kg
Administration oral

Chemical Information & Solubility

Molecular Weight 346.85 Formula

C18H23ClN4O
CAS No. 1422535-52-1 SDF --
Smiles CN1C=C(C=N1)C(=O)NC2=CC=C(C=C2)C3CC3NCC4CC4.Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 69 mg/mL ( (198.93 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 22 mg/mL

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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