T-3775440 hydrochloride

SKU: orb1309043

Description

T-3775440 hydrochloride is a potent and irreversible inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 2.1 nM. This small molecule is a valuable research tool for investigating epigenetic regulation in cancer biology and other diseases, with utility in both cellular and animal model studies.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1422535-52-1
• MW: 346.85
• Purity: 99.94% (May vary between batches)
• Formula: C₁₈H₂₃ClN₄O
• SMILES: Cl.Cn1cc(cn1)C(=O)Nc1ccc(cc1)[C@@H]1C[C@H]1NCC1CC1
• Target: Histone Demethylase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.77 mM);DMSO:30.18 mg/mL (87.01 mM)

Bioactivity

• Target IC50:
  LSD1:2.1 nM
• In Vivo:
  T-3775440 exhibited significant antitumor efficacy in AEL and AMKL xenograft models.
• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

T3775440, T-3775440, T3775440 hydrochloride, T3775440 Hydrochloride, T-3775440 Hydrochloride, T 3775440, T 3775440 hydrochloride, T 3775440 Hydrochloride, HistoneDemethylase, Histone Demethylase, inhibit, Inhibitor, LSD1

Compound Identifiers

PubChem CID

86729932