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T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $88 | In Stock | |
5 mg | $213 | In Stock | |
10 mg | $322 | In Stock | |
25 mg | $579 | In Stock | |
50 mg | $813 | In Stock | |
100 mg | $1,130 | In Stock | |
1 mL x 10 mM (in DMSO) | $235 | In Stock |
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 | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30.18 mg/mL (87.01 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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