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LSD1 Products

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  • LSD1 Inhibitors (11)
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Catalog No. Product Name Information Product Use Citations Product Validations
S7680 SP2509 SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.
MedComm (2020), 2023, 4(3):e269
JCI Insight, 2023, 8(15)e167440
JCI Insight, 2023, 8(15)e167440
S7796 GSK2879552 2HCl GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
MedComm (2020), 2023, 4(3):e269
Cell Rep, 2023, 10.1016/j.celrep.2023.113477
Int J Mol Sci, 2023, 24(4)3605
S7795 Iadademstat (ORY-1001) 2HCl ORY-1001 (RG-6016) 2HCl is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1.
Cell Death Discov, 2024, 10(1):166
Nat Cell Biol, 2023, 10.1038/s41556-023-01281-y
MedComm (2020), 2023, 4(3):e269
S7574 GSK-LSD1 2HCl 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).
Cell Death Dis, 2023, 10.1038/s41419-023-06238-5
Front Immunol, 2023,
Cell Death Differ, 2022, 10.1038/s41418-022-00983-4
S7237 OG-L002 OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM in a cell-free assay, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.
Cell Death Discov, 2024, 10(1):166
Viruses, 2023, 15(1)163
Sci Rep, 2021, 11(1):10285
S6722 Seclidemstat (SP-2577) Seclidemstat (SP-2577) is a potent and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A) with IC50 of 13 nM. Seclidemstat (SP-2577) has potential antineoplastic activity.
Nat Commun, 2023, 10.1038/s41467-023-42850-x
S9894New Vafidemstat Vafidemstat(ORY-2001) is a potent, selective, brain-penetrant dual inhibitor of lysine-specific histone demethylase (LSD1, KDM1A) and MAO-B, with IC50 values of 105 nM and 58 nM, respectively. It shows potential for treating memory deficits and behavioral alterations in neurodegenerative and psychiatric diseases.
E4596New GSK-2879552 GSK-2879552 is a selective and potent inhibitor of Lysine-specific demethylase 1 (LSD1, KDM1A), with the potential to treat Small cell lung cancer (SCLC). It induces the expression of putative KDM1A target genes and demonstrates potent, predominantly cytostatic, antiproliferative activity in SCLC cell lines and tumor xenograft models.
S9734New Bomedemstat Bomedemstat(IMG-7289) is an orally active and irreversible inhibitor of LSD1(lysine-specific demethylase 1). Bomedemstat exhibits the ability to enhance methylation levels of H3K4 and H3K9, subsequently leading to modifications in gene expression. Bomedemstat demonstrates anti-cancer properties by restraining cancer cell proliferation and prompting apoptosis.
S0356 Pulrodemstat (CC-90011) besylate Pulrodemstat (CC-90011) besylate (LSD1-IN-7 benzenesulfonate) is a potent and orally active lysine specific demethylase-1 (LSD1) inhibitor that is found to be effective in various tumors.
S8438 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.
Cell Death Discov, 2024, 10(1):166
S7680 SP2509 SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.
MedComm (2020), 2023, 4(3):e269
JCI Insight, 2023, 8(15)e167440
JCI Insight, 2023, 8(15)e167440
S7796 GSK2879552 2HCl GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
MedComm (2020), 2023, 4(3):e269
Cell Rep, 2023, 10.1016/j.celrep.2023.113477
Int J Mol Sci, 2023, 24(4)3605
S7795 Iadademstat (ORY-1001) 2HCl ORY-1001 (RG-6016) 2HCl is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1.
Cell Death Discov, 2024, 10(1):166
Nat Cell Biol, 2023, 10.1038/s41556-023-01281-y
MedComm (2020), 2023, 4(3):e269
S7574 GSK-LSD1 2HCl 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).
Cell Death Dis, 2023, 10.1038/s41419-023-06238-5
Front Immunol, 2023,
Cell Death Differ, 2022, 10.1038/s41418-022-00983-4
S7237 OG-L002 OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM in a cell-free assay, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.
Cell Death Discov, 2024, 10(1):166
Viruses, 2023, 15(1)163
Sci Rep, 2021, 11(1):10285
S6722 Seclidemstat (SP-2577) Seclidemstat (SP-2577) is a potent and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A) with IC50 of 13 nM. Seclidemstat (SP-2577) has potential antineoplastic activity.
Nat Commun, 2023, 10.1038/s41467-023-42850-x
S9894New Vafidemstat Vafidemstat(ORY-2001) is a potent, selective, brain-penetrant dual inhibitor of lysine-specific histone demethylase (LSD1, KDM1A) and MAO-B, with IC50 values of 105 nM and 58 nM, respectively. It shows potential for treating memory deficits and behavioral alterations in neurodegenerative and psychiatric diseases.
E4596New GSK-2879552 GSK-2879552 is a selective and potent inhibitor of Lysine-specific demethylase 1 (LSD1, KDM1A), with the potential to treat Small cell lung cancer (SCLC). It induces the expression of putative KDM1A target genes and demonstrates potent, predominantly cytostatic, antiproliferative activity in SCLC cell lines and tumor xenograft models.
S9734New Bomedemstat Bomedemstat(IMG-7289) is an orally active and irreversible inhibitor of LSD1(lysine-specific demethylase 1). Bomedemstat exhibits the ability to enhance methylation levels of H3K4 and H3K9, subsequently leading to modifications in gene expression. Bomedemstat demonstrates anti-cancer properties by restraining cancer cell proliferation and prompting apoptosis.
S0356 Pulrodemstat (CC-90011) besylate Pulrodemstat (CC-90011) besylate (LSD1-IN-7 benzenesulfonate) is a potent and orally active lysine specific demethylase-1 (LSD1) inhibitor that is found to be effective in various tumors.
S8438 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.
Cell Death Discov, 2024, 10(1):166
S9894New Vafidemstat Vafidemstat(ORY-2001) is a potent, selective, brain-penetrant dual inhibitor of lysine-specific histone demethylase (LSD1, KDM1A) and MAO-B, with IC50 values of 105 nM and 58 nM, respectively. It shows potential for treating memory deficits and behavioral alterations in neurodegenerative and psychiatric diseases.
E4596New GSK-2879552 GSK-2879552 is a selective and potent inhibitor of Lysine-specific demethylase 1 (LSD1, KDM1A), with the potential to treat Small cell lung cancer (SCLC). It induces the expression of putative KDM1A target genes and demonstrates potent, predominantly cytostatic, antiproliferative activity in SCLC cell lines and tumor xenograft models.
S9734New Bomedemstat Bomedemstat(IMG-7289) is an orally active and irreversible inhibitor of LSD1(lysine-specific demethylase 1). Bomedemstat exhibits the ability to enhance methylation levels of H3K4 and H3K9, subsequently leading to modifications in gene expression. Bomedemstat demonstrates anti-cancer properties by restraining cancer cell proliferation and prompting apoptosis.

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