KDM1/LSD1

KDM1A/LSD1 (lysine-specific demethylase 1A) is a flavin adenine dinucleotide (FAD)-dependent histone demethylase that catalyzes oxidative demethylation of histone H3K4me1/2 and H3K9me1/2, thereby regulating chromatin structure and transcriptional programs central to cell fate determination and differentiation^[1]^[2]. Mechanistically, LSD1 functions within transcriptional corepressor and chromatin-remodeling complexes, where its demethylase activity modulates epigenetic gene regulation and contributes to the dynamic control of gene expression^[2]^[3]. Through actions on both histone and non-histone substrates, LSD1 participates in multiple biological pathways involved in development, hematopoiesis, neuronal function, and cellular homeostasis^[3]^[4]. In disease settings, aberrant LSD1 activity supports cancer progression by regulating gene-expression programs associated with adaptation to the tumor microenvironment, epithelial-mesenchymal transition (EMT), stemness, and differentiation states^[4]. Experimental studies further demonstrate that pharmacological or genetic inhibition of LSD1 can suppress EMT-associated transcriptional programs and impede tumor progression in preclinical models^[4]. Compared with related isoforms, the neuronal LSD1 isoform displays distinct substrate specificity, preferentially demethylating H3K9me2 rather than H3K4me2 and promoting transcriptional programs linked to neuronal differentiation, learning, and memory^[4]. This functional divergence highlights isoform-specific biological roles that should be considered when interpreting mechanistic studies and therapeutic responses^[4]. For experimental applications, LSD1 has emerged as a major epigenetic drug target, and multiple small-molecule inhibitors, including tranylcypromine-derived compounds and clinical-stage LSD1 inhibitors, are being evaluated for hematologic malignancies and solid tumors, supporting its utility in target-validation and translational research programs^[4]^[5].

References:

[1]. Burg JM, et al. Lysine-Specific Demethylase 1A (KDM1A/LSD1): Product Recognition and Kinetic Analysis of Full-Length Histones. Biochemistry. 2016 Mar 22;55(11):1652-62. [Content Brief]

[2]. Perillo B, et al. LSD1: more than demethylation of histone lysine residues. Exp Mol Med. 2020 Dec;52(12):1936-1947. [Content Brief]

[3]. Uniprotkb.

[4]. Kim D, et al. Roles of lysine-specific demethylase 1 (LSD1) in homeostasis and diseases. J Biomed Sci. 2021 Jun 4;28(1):41. [Content Brief]

[5]. Gill H. Lysine-Specific Demethylase 1 (LSD1/KDM1A) Inhibition as a Target for Disease Modification in Myelofibrosis. Cells. 2022 Jul 3;11(13):2107. doi: 10.3390/cells11132107. Erratum in: Cells. 2022 Dec 19;11(24):4126. doi: 10.3390/cells11244126. PMID: 35805191; PMCID: PMC9265913. et al. Lysine-Specific Demethylase 1 (LSD1/KDM1A) Inhibition as a Target for Disease Modification in Myelofibrosis. Cells. 2022 Jul 3;11(13):2107. [Content Brief]

KDM1/LSD1 Related Products (92)
Antibodies (1)

KDM1/LSD1 Related Products (92):

By Type:	Pan (7) Selective (21)
By Effects:	Inhibitors (88) Antagonist (1) Ligand (1)

Cat. No.	Product Name	Effect	Purity

HY-17447A

Tranylcypromine hydrochloride	Ligand	99.91%
Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC₅₀s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression.

HY-18632

GSK2879552	Inhibitor	99.98%
GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.

HY-12782T

Iadademstat dihydrochloride	Inhibitor	99.98%
Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.

HY-100546A

GSK-LSD1 dihydrochloride	Inhibitor	99.88%
GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 16 nM.

HY-109117

Iadademstat	Inhibitor	99.82%
Iadademstat (ORY-1001) is a highly potent, orally active and selective LSD1 (KDM1A) inhibitor with antileukemic activity. Iadademstat can be used for relapsed or refractory acute myeloid leukemia research.

HY-183067A

TAS1440 benzoate	Inhibitor
TAS1440 benzoate is an orally active LSD1/KDM1A inhibitor with a human IC₅₀ of 4.8 nM. TAS1440 benzoate non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 benzoate activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 benzoate can be used for the research of small cell lung cancer, specifically the SCLC-A subtype.

HY-182892

MC4491	Inhibitor
MC4491 is a selective LSD1/PRMT5 inhibitor, with an IC₅₀ of 0.152 μM against the LSD1/CoREST complex and an IC₅₀ of 0.043 μM against the PRMT5/MEP50 complex. MC4491 induces transcriptomic changes and splicing alterations in AML cells. MC4491 is applicable for the research of acute myeloid leukemia.

HY-N18236

3β-Acetoxyl-atractylenolide I	Inhibitor
3β-Acetoxyl-atractylenolide I is a LSD1 inhibitor with an IC₅₀ of 57 μM. 3β-Acetoxyl-atractylenolide I blocks tumor growth, metastasis and invasion. 3β-Acetoxyl-atractylenolide I is used in the research of various cancers including prostate cancer, breast cancer, neuroblastoma, gastric cancer, colon cancer, bladder cancer, esophageal cancer, acute myeloid leukemia and retinoblastoma.

HY-12635

SP2509	Antagonist	99.50%
SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with an IC₅₀ of 13 nM.

HY-B1496

Tranylcypromine hemisulfate	Inhibitor	99.94%
Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects.

HY-103713

Seclidemstat	Inhibitor	99.77%
Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (K_i=31 nM, IC₅₀=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma.

HY-129388B

Pulrodemstat benzenesulfonate	Inhibitor	99.64%
Pulrodemstat (CC-90011) benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC₅₀ of 0.25 nM. Pulrodemstat benzenesulfonate is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.

HY-109169

Bomedemstat	Inhibitor	99.43%
Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.

HY-109169A

Bomedemstat ditosylate	Inhibitor	99.14%
Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.

HY-138830

TAK-418	Inhibitor	99.81%
TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC₅₀ of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models.

HY-19612A

DDP-38003 dihydrochloride	Inhibitor	99.31%
DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC₅₀ of 84 nM.

HY-109169B

Bomedemstat hydrochloride	Inhibitor	99.94%
Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.

HY-103713A

Seclidemstat mesylate	Inhibitor	99.80%
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (K_i=31 nM, IC₅₀=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma.

HY-164099

LSD1/HDAC6-IN-2	Inhibitor	99.66%
LSD1/HDAC6-IN-2 (JBI-802) is an orally active LSD1/HDAC6/MAO-A inhibitor, with IC₅₀ values of 5 nM, 11 nM, and 5 nM, respectively. LSD1/HDAC6-IN-2 can inhibit the growth of multiple myeloma cells MM.1S, MM.1R, and RPMI-8226. LSD1/HDAC6-IN-2 can be used for research on diseases such as acute myeloid leukemia and lymphoma.

HY-110277

S2101	Inhibitor	99.70%
S2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 0.99 μM, K_i of 0.61 μM and K_inact/K_i of 4560 M/s.

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KDM1/LSD1

KDM1/LSD1 Related Products (92)

Antibodies (1)

KDM1/LSD1 Related Products (92):