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]
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KDM1/LSD1 Related Products (98)
Related Products (98)
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Antibodies (1)
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LSD1-IN-42
0 ImagesCat. No.: HY-172809LSD1-IN-42 (Compound 7ae) is an orally active LSD1 inhibitor that potently inhibits LSD1 activity (IC50 = 0.08 μM). LSD1-IN-42 downregulates PD-L1 expression and enhances T cell-mediated tumor killing effects. LSD1-IN-42 demonstrates significant anti-gastric cancer activity by inhibiting tumor cell invasion and migration.
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LSD1-IN-10
0 ImagesCat. No.: HY-136878CAS No.: 1235864-15-9LSD1-IN-10 is a LSD1/MAO inhibitor with LSD1 IC50 of 5 nM, MAO-A IC50 of 16 μM, and MAO-B IC50 of 7.4 μM. LSD1-IN-10 suppresses enzymatic activity of LSD1, MAO-A, and MAO-B. LSD1-IN-10 can be used for the research of cancer, alzheimer's disease, parkinson's disease, huntington's disease.
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LSD1/2-IN-3
0 ImagesCat. No.: HY-151192CAS No.: 2821068-07-7LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 11 nM instead of 7 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, LSD1/2-IN-1 inhibits LSD1 cell proliferation.
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LSD1-IN-49 hydrochloride
0 ImagesCat. No.: HY-186116ACAS No.: 1422534-06-2LSD1-IN-49 hydrochloride (Compound (±) 1) is an irreversible LSD1/KDM1A inhibitor with an IC50 of 29 nM against hLSD1. LSD1-IN-49 hydrochloride irreversibly inhibits the enzymatic activity of LSD1 by forming an adduct with flavin adenine dinucleotide (FAD) in the binding pocket of LSD1. LSD1-IN-49 hydrochloride is applicable to research related to schizophrenia, autism spectrum disorder and Huntington's disease.
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DC551040
0 ImagesCat. No.: HY-183105CAS No.: 2133291-32-2DC551040 is an orally active and selective lysine demethylase 1 (LSD1) inhibitor with a human IC50 of 2.14 nM. DC551040 binds to LSD1 via π-π stacking with Trp552, polar interactions with Phe538, and covalent adduct formation with FAD, and disrupts the LSD1-GFI1B-CoREST complex. DC551040 induces H3K4me2 accumulation, apoptosis, and cell differentiation, activates STAT5, NF-κB, AKT, and IL6-STAT3 pathways, and upregulates IL6 expression. DC551040 can be used for the research of acute myeloid leukemia.
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LSD1-IN-16
0 ImagesCat. No.: HY-144757CAS No.: 3033060-68-0LSD1-IN-16 (compound 4b) is a potent LSD1 inhibitor. LSD1-IN-16 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 15.2 μM.
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Pulrodemstat hydrochloride
0 ImagesCat. No.: HY-129388CCAS No.: 1821307-11-2Synonyms: CC-90011 hydrochloride; LSD1-IN-7 hydrochloridePulrodemstat (CC-90011) hydrochloride is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 value of 0.25 nM. Pulrodemstat hydrochloride is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat hydrochloride induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
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Tranylcypromine-d5 hydrochloride
0 ImagesCat. No.: HY-17447SACAS No.: 107077-98-5Synonyms: SKF 385-d5 hydrochlorideTranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis.
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AW4
0 ImagesCat. No.: HY-173590CAS No.: 2455469-18-6AW4 is a LSD1 inhibitor. AW4 inhibits LSD1 ΔTTAS activity in H3K4me2 demethylation assays. AW4 can be used for research of drug resistance.
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CBB1003 hydrochloride
0 ImagesCat. No.: HY-15774ACAS No.: 2070015-02-8CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
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CBB3001
0 ImagesCat. No.: HY-124616CAS No.: 1639358-50-1CBB3001 is an inhibitor of LSD1/KDM1A. CBB3001 exerts its effect by inhibiting Histone Demethylase activity, with an IC50 of 21.25 μM. It downregulates the expression of pluripotency-related proteins and genes such as SOX2 and OCT4, and induces cell differentiation, growth arrest, and apoptosis. CBB3001 can be used for research on testicular germ cell tumors, teratomas, and embryonal carcinomas.
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LSD1-IN-44
0 ImagesCat. No.: HY-175184LSD1-IN-44 (Compound 19) is a LSD1 inhibitor with an IC50 of 0.02 μM for LSD1-CoREST enzymatic complex. LSD1-IN-44 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. LSD1-IN-44 has no significant toxicity to human cells. LSD1-IN-44 can be used for schistosomiasis research.
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MC3935
0 ImagesCat. No.: HY-175185MC3935 is a LSD1 inhibitor with an IC50 of 0.52 μM for LSD1-CoREST enzymatic complex. MC3935 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. MC3935 has no significant toxicity to human cells. MC3935 can be used for schistosomiasis research.
