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T-3775440 hydrochloride is a potent, selecitve, irreversible LSD1 inhibitor with IC50 value of 2.1 nM. T-3775440 is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with IC50 value of 2.1 nM. In CMK11-5 cells, CD86 mRNA expression is also clearly upregulated by T-3775440 in a concentration-dependent manner, although only a modest increase in cell surface CD86 expression is observed. T-3775440 treatment disrupts the LSD1-GFI1B association in a concentration-dependent manner. T-3775440 decreases LSD1 binding but not GFI1B binding and increases the level of dimethylated H3K4 at the PI16 locus.
In a TF-1a (AEL) tumor xenograft model, T-3775440 exhibits significant antitumor effects, with 15-day T/C values of 15.6% and <0% at doses of 20 and 40 mg/kg, respectively. T-3775440 also exhibits potent antitumor effects in an additional AEL model of HEL 92.1.7 and an AMKL model of CMK11-5, leading to nearly complete tumor growth suppression during the dosing period.
| Molecular Weight | 346.85 |
| Formula | C18H23ClN4O |
| CAS Number | 1422535-52-1 |
| Solubility (25°C) | DMSO ≥ 25 mg/mL Water ≥ 10 mg/mL |
| Storage | -20°C, dry, protect from light, sealed |
| Related Histone demethylase Products |
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| JIB-04
JIB-04 is a selective inhibitor of Jumonji histone demethylase with IC50 values of 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively. |
| GSK-J1
GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. GSK J1 is selective for the H3K27 demethylases JMJD3 and UTX. |
| GSK-J4 hydrochloride
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 hydrochloride is a cell permeable procompound of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family. |
| OG-L002
OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively. |
| GSK-LSD1 dihydrochloride
GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). |
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