Catalog No.
Product Name
Application
Product Information
Citations
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LSD Derivative
ALD-52 (1-Acetyl-LSD) serves as a prodrug for LSD, primarily targeting serotonin receptors 5-HT1A, 5-HT2A, and 5-HT2C, with binding affinities of 1054, 174, and 10.2 nM, respectively. Upon conversion to LSD, ALD-52 elicits a head-twitch response (HTR) in vivo, demonstrating its psychoactive properties. This compound is valuable in hallucinogen research, providing insights into its pharmacological effects and the underlying mechanisms of serotonergic activity. -
LSD1 Inhibitor
LSD1-IN-14 is a potent and selective inhibitor of Lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 0.89 μM. This compound effectively inhibits the proliferation of A549 lung cancer cells and THP-1 monocytic cells, while also inducing apoptosis in tumor cell lines. LSD1-IN-14 is valuable for research applications focused on understanding the role of LSD1 in cancer biology and developing potential therapeutic strategies targeting epigenetic regulation. -
LSD1/KDM1A Inhibitor
TPC-144 is an inhibitor of LSD1/KDM1A, targeting the demethylation process by reducing DNMT1 protein levels, resulting in decreased methylation of LINE-1 elements. This compound has shown promising synergistic effects with Decitabine, enhancing DNA demethylation, which promotes differentiation and apoptosis in leukemia cells. Furthermore, TPC-144 has demonstrated anti-tumor activity in acute myeloid leukemia (AML) models, making it a valuable tool for AML research and therapeutic studies. -
LSD1/HDAC Inhibitor
LSD1/HDAC-IN-2 is a potent inhibitor of lysine-specific demethylase 1 (LSD1) and several histone deacetylases (HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8), with IC50 values ranging from 1.0 to 39.0 nM. This compound demonstrates significant biological activity by inhibiting the proliferation of colorectal cancer cells, inducing apoptosis, and causing G2/M cell cycle arrest. Additionally, LSD1/HDAC-IN-2 reduces cell migration and displays antitumor efficacy in mouse models, making it a valuable tool for cancer research and therapeutic development. -
LSD1 Inhibitor
LSD1-IN-25 is a potent and selective inhibitor of lysine-specific demethylase 1 (LSD1), demonstrating an IC50 of 46 nM and a Ki of 30.3 nM. This compound effectively induces apoptosis in cancer cells, making it a valuable tool for investigating the role of LSD1 in cancer biology and therapeutic applications. Its oral bioavailability further supports its use in preclinical studies aimed at targeting epigenetic regulation in malignancies. -
PROTAC KDM4 Degrader
PROTAC KDM4 Degrader-1 is a potent proteolysis targeting chimera (PROTAC) designed to selectively degrade KDM4A-C while sparing KDM4D. This compound demonstrates significant antiproliferative effects in esophageal cancer cells, inducing apoptosis and cell cycle arrest. Additionally, PROTAC KDM4 Degrader-1 effectively inhibits histone H3 lysine demethylation, making it a valuable tool for research into cancer biology and epigenetic regulation. -
plant growth regulator
Daminozide(DMASA; DIMG; B 995), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily. -
LSD1/BHC110 & MAO inhibitor
Tranylcypromine hydrochloride is a non-selective MAO-A/B inhibitor. -
KDM1A/LSD1 inhibitor
Iadademstat dihydrochloride (ORY-1001 dihydrochloride) is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
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LSD1 inhibitor
GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM. -
Jumonji histone demethylase inihibitor
Z-JIB-04 (NSC 693627, JIB-04 Z-isomer) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively. -
epigenetic modifier
L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. -
KDM1/CDK1 Inhibitor
KDM1/CDK1-IN-1 is a potent inhibitor of both KDM1 and CDK1, exhibiting IC50 values of 0.096 μM and 0.078 μM, respectively. This compound effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in HOP-92 cancer cells. Additionally, KDM1/CDK1-IN-1 demonstrates significant cytotoxic effects against a range of cell lines, including CCRF-CEM, HOP-92, and Hep-G2, with IC50 values of 16.34 μM, 3.45 μM, and 7.79 μM, respectively. Its ability to target critical regulators of the cell cycle makes KDM1/CDK1-IN-1 valuable for cancer research applications. -
LSD1/ DCN1-UBC12 Protein-Protein Interaction Inhibitor
WS-384 is a dual inhibitor targeting LSD1 and the DCN1-UBC12 protein-protein interaction, demonstrating IC50 values of 338.79 nM and 14.81 nM, respectively. This compound exhibits significant anticancer activity, facilitating cell cycle arrest, DNA damage, and apoptosis in cancer cells. WS-384 serves as a valuable tool for research into non-small cell lung cancer (NSCLC) and other related malignancies. -
KDM4D Inhibitor
Zavondemstat (QC8222; TACH 101) is an inhibitor of histone lysine demethylase 4D (KDM4D) with demonstrated antineoplastic activity. It is under investigation for its potential use in cancer therapy by targeting epigenetic regulation mechanisms. -
LSD1 inhibitor
Bomedemstat (IMG-7289) is an orally active, irreversible inhibitor of lysine-specific demethylase 1 (LSD1). By inhibiting LSD1, it increases methylation of histone marks H3K4 and H3K9, leading to altered gene expression. Bomedemstat exhibits potent anti-cancer activity by inhibiting cancer cell proliferation and inducing apoptosis, and is being explored as a therapeutic agent in hematologic malignancies and other cancers. -
LSD1 inhibitor
Pulrodemstat benzenesulfonate (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. It exhibits significantly lower inhibitory activity against related enzymes such as LSD2, MAO-A, and MAO-B. CC-90011 induces differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells and demonstrates strong anticancer activity, making it a promising candidate for epigenetic cancer therapy. -
PRMT5 inhibitor
AMG 193 is an orally bioavailable, MTA-cooperative inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting potent antitumor activity. By leveraging the accumulation of methylthioadenosine (MTA) in MTAP-deficient cells, AMG 193 selectively inhibits PRMT5 with an IC₅₀ of 0.107 μM, leading to preferential suppression of tumor cell growth while sparing normal cells with intact MTAP function. -
MAO/LSD1 Inhibitor
Tranylcypromine hemisulfate is an irreversible, nonselective inhibitor of monoamine oxidase (MAO) and also acts as a lysine-specific demethylase 1 (LSD1) inhibitor. This compound demonstrates notable antidepressant effects and is utilized in the treatment of depression. Additionally, tranylcypromine hemisulfate has been shown to suppress lesion growth and alleviate generalized hyperalgesia in mouse models of induced endometriosis, making it a valuable tool for research in both psychiatric and pain-related studies. -
LSD1/HDAC Inhibitor
LSD1/HDAC-IN-1 is a potent inhibitor of histone deacetylases (HDACs) and lysine-specific demethylase 1 (LSD1), demonstrating impressive inhibitory activity with IC50 values of 0.125 nM for HDAC1, 0.373 nM for HDAC2, 0.0118 nM for HDAC6, 0.103 nM for HDAC8, and 0.571 μM for LSD1. This compound is significant in cancer research, as it influences gene expression and histone modification, making it a valuable tool for studies addressing epigenetic regulation and potential therapeutic interventions. -
LSD1/HDAC6 Inhibitor
LSD1/HDAC6-IN-1 is a dual inhibitor targeting lysine-specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6), demonstrating significant anti-tumor activity. This compound is particularly relevant for research into multiple myeloma (MM), providing insights into epigenetic regulation and potential therapeutic strategies. Its oral bioavailability makes it suitable for in vivo studies in cancer research. -
LSD1 Inhibitor
GSK-LSD1 is a selective inhibitor of lysine-specific demethylase 1 (LSD1). This compound demonstrates significant biological activity by reducing food intake and body weight, while also enhancing insulin sensitivity and glycemic control in mouse models of obesity. Additionally, GSK-LSD1 shows promise in alleviating non-alcoholic fatty liver disease (NAFLD) and inhibiting cytokine release triggered by SARS-CoV-2 in peripheral blood mononuclear cells from COVID-19 patients. Furthermore, GSK-LSD1 has been identified as a potential therapeutic agent for suppressing cancer growth and metastasis. -
KDM2B Inhibitor
KDM2B-IN-3 is a selective inhibitor of the histone demethylase KDM2B, designed to modulate epigenetic regulation. By inhibiting KDM2B, this compound can alter histone methylation patterns, making it a valuable tool for cancer research and investigations into epigenetic modifications. Its potential applications include studying the role of KDM2B in tumorigenesis and evaluating therapeutic strategies targeting epigenetic regulators. -
LSD1 Inhibitor
Pulrodemstat (hydrochloride) is a potent and selective reversible inhibitor of lysine-specific demethylase-1 (LSD1), exhibiting an IC50 value of 0.25 nM. This compound demonstrates minimal enzymatic inhibition of LSD2, MAO-A, and MAO-B, making it a highly specific agent. Pulrodemstat (hydrochloride) promotes differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells, showcasing significant anticancer activity. It serves as a valuable tool for research in cancer biology and therapeutic development. -
JMJD3/KDM6B Inhibitor
GSK-J1 sodium is a selective inhibitor of the histone demethylases JMJD3 (KDM6B) and UTX (KDM6A), exhibiting an IC50 value of 60 nM for KDM6B. This compound modulates H3K27me3/me2 levels, thereby influencing gene expression and cellular differentiation. GSK-J1 sodium is useful in research applications focused on epigenetic regulation, cancer biology, and developmental processes. -
LSD1 Inhibitor
AW4 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), effectively targeting the ΔTTAS activity during H3K4me2 demethylation assays. This compound demonstrates significant potential in studying the biological implications of LSD1 modulation and can be utilized in research related to drug resistance mechanisms. AW4's ability to interfere with LSD1 activity positions it as a valuable tool in epigenetic research and therapeutic development. -
KDM5A Inhibitor
JQKD82 is a selective inhibitor of the lysine demethylase KDM5A. It effectively increases levels of trimethylated histone H3 at lysine 4 (H3K4me3), facilitating research into epigenetic regulation and its implications in various cancers, including multiple myeloma. This compound is suitable for studies investigating KDM5A's role in oncogenic processes and potential therapeutic strategies. -
KDM5A Inhibitor
JQKD82 dihydrochloride is a selective inhibitor of the lysine demethylase KDM5A. This compound enhances levels of trimethylation at histone H3 lysine 4 (H3K4me3), making it a valuable tool for studying epigenetic regulation in various cellular contexts. Its application in research includes investigations into the mechanisms underlying multiple myeloma and other hematological malignancies. -
LSD1 Inhibitor
LSD1-IN-29 is a potent inhibitor of Lysine-specific demethylase 1 (LSD1), demonstrating an IC50 value of 19 nM. This compound effectively modulates LSD1 activity, making it a valuable tool for investigating epigenetic regulation and gene expression mechanisms. It is applicable in research focusing on cancer biology, neurodegenerative diseases, and other conditions influenced by methylation status. -
LSD1 Inhibitor
NCD-25 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 0.48 μM. This compound is effective in modulating epigenetic regulation through its inhibition of LSD1, which plays a key role in the demethylation of histone proteins. NCD-25 is valuable for research applications focused on cancer biology, developmental processes, and drug discovery involving epigenetic mechanisms. -
LSD1 Inhibitor
rel-OG-L002 (hydrochloride) is a selective inhibitor of lysine-specific demethylase 1 (LSD1). It demonstrates potent inhibition of LSD1 activity, leading to increased levels of methylated histones, which can influence gene expression regulation. This compound is valuable for research in cancer biology, epigenetics, and the study of histone methylation pathways. -
LSD1 Inhibitor
OG-L002 hydrochloride is a selective inhibitor of lysine-specific demethylase 1 (LSD1) with an IC50 value of 0.02 μM, demonstrating robust inhibition of this target. Additionally, it acts as a potent monoamine oxidase (MAO) inhibitor, with IC50 values of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. This compound has potential applications in research related to gene expression regulation and the modulation of herpes simplex virus immediate early genes. -
LSD1 Inhibitor
LSD1-IN-46 is a potent and orally bioavailable inhibitor of Lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 0.082 μM. By disrupting the β-catenin-mediated transcriptional program, LSD1-IN-46 effectively diminishes the stemness characteristics of gastric cancer cells. This compound demonstrates significant anti-tumor activity, making it a valuable reagent for research into gastric cancer therapeutics. -
LSD1 Inhibitor
LSD1-IN-22 is a potent inhibitor of Lysine-specific demethylase 1 (LSD1) with an inhibitory constant (Ki) of 98 nM. This compound exhibits anti-proliferative activity in various cancer cell lines, making it a valuable tool for studying the role of LSD1 in cancer biology. Its inhibition of LSD1 can aid in exploring therapeutic strategies targeting epigenetic modifications in cancer treatment. -
LSD1 Inhibitor
LSD1-IN-39 is a reversible inhibitor of lysine-specific demethylase 1 (LSD1) with an IC50 of 0.18 μM. This compound demonstrates significant anti-proliferative effects across various cancer cell lines, effectively inhibits HepG2 cell migration, and prevents epithelial-mesenchymal transition. Furthermore, LSD1-IN-39 exhibits notable antitumor activity in murine models, making it a valuable tool for cancer research. -
KDM5B Inhibitor
KDM5B-IN-3 is a selective inhibitor of histone lysine-specific demethylase 5B (KDM5B/JARID1B), displaying an IC50 of 9.32 μM. This compound is instrumental in studying the epigenetic regulation associated with gastric cancer. It provides a valuable tool for researchers investigating KDM5B's role in tumorigenesis and therapeutic strategies targeting histone modifications. -
LSD1 Inhibitor
LSD1-IN-19 is a potent and selective inhibitor of the lysine-specific demethylase 1 (LSD1), exhibiting a Ki value of 0.108 μM and a KD of 0.068 μM. This compound demonstrates significant antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 values of 0.17 μM and 0.40 μM, respectively, over a 72-hour treatment period. LSD1-IN-19 is valuable for investigating the role of LSD1 in cancer biology and may serve as a potential therapeutic candidate in the treatment of cancers driven by epigenetic regulation. -
LSD1 Inhibitor
LSD1-IN-12 is a potent inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting a Ki value of 1.1 μM for LSD1. Additionally, it demonstrates moderate inhibition of LSD2, MAO-A, and MAO-B with Ki values of 61 μM, 2.3 μM, and 3.5 μM, respectively. This compound is valuable for studying the role of LSD1 in epigenetic regulation and its implications in various diseases, including cancer and neurodegenerative disorders. -
LSD1 Inhibitor
LSD1-IN-13 is a potent inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 24.43 nM. This orally active compound has been shown to enhance CD86 expression with an EC50 of 470 nM. Additionally, LSD1-IN-13 promotes differentiation in acute myeloid leukemia (AML) cell lines, making it a valuable tool for investigating epigenetic regulation in cancer research. -
LSD1 Inhibitor
LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1) with a Ki value of 11 nM, demonstrating significantly lower affinity for LSD2 (7 μM). This compound effectively inhibits LSD1-mediated cell proliferation, particularly in cancer stem cells, highlighting its potential for oncological research. It is valuable for investigations into epigenetic regulation and therapeutic strategies targeting LSD1 in cancer. -
JMJD7 Inhibitor
JMJD7-IN-1 is a selective inhibitor of the JMJD7 enzyme, exhibiting an IC50 value of 6.62 μM. This compound effectively inhibits JMJD7 activity in cells with elevated JMJD7 expression levels. It serves as a valuable tool for investigating the biological functions of JMJD7 and its role in various cellular processes. This compound is suitable for research applications in epigenetics and cancer biology. -
LSD1 Inhibitor
LSD1-IN-24 is a selective inhibitor of lysine-specific demethylase 1 (LSD1) with an IC50 of 0.247 μM. This compound has been shown to modulate the expression of PD-L1, thereby enhancing T cell-mediated cytotoxicity. It is primarily utilized in cancer research to explore the effects of LSD1 inhibition on immune response and tumor progression. -
LSD1 Inhibitor
Pulrodemstat is a potent and reversible inhibitor of lysine specific demethylase-1 (LSD1), exhibiting an IC50 of 0.25 nM, while demonstrating minimal inhibition of LSD2, MAO-A, and MAO-B. This compound effectively promotes differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells, showcasing its significant anticancer properties. Due to its selective action, Pulrodemstat serves as a valuable tool for exploring the therapeutic potential of LSD1 inhibition in cancer research. -
LSD1 Inhibitor
INCB059872 dihydrochloride is a selective and irreversible inhibitor of Lysine-Specific Demethylase 1 (LSD1). This compound demonstrates potent biological activity and is primarily utilized in research focused on myeloid leukemia. Its ability to modulate LSD1 activity makes it a valuable tool for exploring demethylation processes in cancer biology.
