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T-3775440 hydrochloride

Catalog No. T13055   CAS 1422535-52-1

T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).

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T-3775440 hydrochloride Chemical Structure
T-3775440 hydrochloride, CAS 1422535-52-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 97.00
5 mg In stock $ 263.00
10 mg In stock $ 393.00
25 mg In stock $ 658.00
50 mg In stock $ 937.00
100 mg In stock $ 1,270.00
1 mL * 10 mM (in DMSO) In stock $ 257.00
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Purity: 99.94%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).
Targets&IC50 LSD1:2.1 nM
In vitro T-3775440, a novel irreversible LSD1 inhibitor. Cell growth analysis of leukemia cell lines revealed that acute erythroid leukemia (AEL) and acute megakaryoblastic leukemia cells (AMKL) were highly sensitive to this compound. T-3775440 treatment enforced transdifferentiation of erythroid/megakaryocytic lineages into granulomonocytic-like lineage cells. Mechanistically, T-3775440 disrupted the interaction between LSD1 and growth factor-independent 1B (GFI1B), a transcription factor critical for the differentiation processes of erythroid and megakaryocytic lineage cells. Knockdown of LSD1 and GFI1B recapitulated T-3775440-induced transdifferentiation and cell growth suppression, highlighting the significance of LSD1-GFI1B axis inhibition with regard to the anti-AML effects of T-3775440[1].
In vivo T-3775440 exhibited significant antitumor efficacy in AEL and AMKL xenograft models[1].
Molecular Weight 346.85
Formula C18H23ClN4O
CAS No. 1422535-52-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30.18 mg/mL (87.01 mM)

TargetMolReferences and Literature

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. 2. Matsumoto, Satoru, Ishikawa,et al. LSD1 Inhibitor T-3775440 Inhibits SCLC Cell Proliferation by Disrupting LSD1 Interactions with SNAG Domain Proteins INSM1 and GFI1B[J]. Cancer Research the Official Organ of the American Association for Cancer Research Inc, 2017.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Chromatin Modification Compound Library Stem Cell Differentiation Compound Library Histone Modification Compound Library Epigenetics Compound Library Anti-Aging Compound Library NO PAINS Compound Library

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Keywords

T-3775440 hydrochloride 1422535-52-1 Chromatin/Epigenetic Histone Demethylase T3775440 hydrochloride T-3775440 inhibit T3775440 T 3775440 Inhibitor T 3775440 hydrochloride T 3775440 Hydrochloride T-3775440 Hydrochloride T3775440 Hydrochloride inhibitor

 

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