Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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/HDAC6/MAO-A Inhibitor
LSD1/HDAC6-IN-2 is a potent inhibitor targeting LSD1, HDAC6, and MAO-A, with IC50 values of 5 nM, 11 nM, and 5 nM, respectively. It demonstrates significant inhibitory effects on the growth of multiple myeloma cell lines, including MM.1S, MM.1R, and RPMI-8226. This compound is suitable for research applications focused on acute myeloid leukemia and lymphoma, providing insights into potential therapeutic mechanisms. -
HDAC6/MAO-A/LSD1 Inhibitor
HDAC6-IN-3 is a potent inhibitor of histone deacetylase 6 (HDAC6), with an IC50 ranging from 0.02 to 1.54 μM for various HDAC isoforms, including HDAC1, HDAC2, HDAC3, and HDAC8. Additionally, it exhibits significant inhibitory activity against monoamine oxidase A (MAO-A) with an IC50 of 0.79 μM and lysine-specific demethylase 1 (LSD1). This compound serves as a valuable tool for research applications in cancer biology and epigenetics and is equipped with an alkyne functionality, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc). -
LSD1/G9a Inhibitor
LSD1-IN-20 is a potent dual non-covalent inhibitor of lysine-specific demethylase 1 (LSD1) and G9a, exhibiting Ki values of 0.44 and 0.68 μM, respectively. This compound demonstrates significant antiproliferative effects in THP-1 leukemia and MDA-MB-231 breast cancer cell lines, with IC50 values of 0.51 and 1.60 μM over 72 hours. LSD1-IN-20 serves as a valuable tool for research focused on epigenetic regulation and its implications in cancer biology. -
EZH2/LSD1 Inhibitor
ML234 is a dual inhibitor targeting EZH2 and LSD1, exhibiting IC50 values of 0.09 μM and 0.12 μM, respectively. This compound demonstrates significant antiproliferative effects in prostate cancer cell lines, including LNCAP, PC3, and 22RV1. In vivo studies reveal that ML234 effectively suppresses tumor growth in the 22RV1 xenograft mouse model, making it a valuable tool for research focused on anticancer therapies in prostate cancer. -
JMJD1C Inhibitor
JMJD1C-IN-1 is a selective inhibitor of JMJD1C with an IC50 of 0.59 μM and a Kd of 1.96 μM. This compound effectively disrupts the binding of JMJD1C to the H3K9me2 peptide substrate as demonstrated in the HTRF assay, showing an IC50 of 1.47 μM. JMJD1C-IN-1 enhances tumor immunotherapy research by impairing intratumoral regulatory T (Treg) cell fitness through the accumulation of H3K9me2, which downregulates PD1 expression, and by reducing STAT3 demethylation, thereby promoting STAT3 activation. Furthermore, it exhibits dose-dependent antitumor efficacy across various mouse cancer models, including fibrosarcoma, melanoma, lung cancer, hepatocellular carcinoma, and colorectal cancer. -
LSD1 Inhibitor
Higenamine hydrochloride is a selective inhibitor of LSD1, with an IC50 value of 1.47 μM. This compound exhibits anti-inflammatory and antibacterial properties, and has been shown to attenuate IL-1β-induced apoptosis via the ROS-mediated PI3K/Akt signaling pathway. Additionally, Higenamine hydrochloride protects brain cells from oxygen deprivation and promotes bone formation in osteoporosis through the SMAD2/3 pathway. Its versatile applications make it suitable for research in cancer, inflammation, cardiorenal syndrome, and related diseases. -
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. -
LSD1 Inhibitor
CBB1007 trihydrochloride is a reversible and selective inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 5.27 µM for human LSD1. It effectively inhibits LSD1's demethylase activity on H3K4Me2 and H3K4Me, demonstrating notable selectivity for LSD1 over LSD2 and JARID1A. This compound has significant implications in cancer research, particularly in non-pluripotent models, as it promotes the expression of differentiation-related genes in pluripotent cells and is being explored in the context of teratocarcinoma, embryonic carcinoma, and seminoma. -
LSD1 Inhibitor
Bizine is a selective inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting a Ki value of 59 nM. This compound effectively modulates bulk histone methylation in cancer cells, contributing to alterations in gene expression. Additionally, Bizine demonstrates neuroprotective properties, making it a valuable tool for research into mechanisms of neurodegeneration and cancer biology. -
LSD1 Inhibitor
LSD1-IN-30 is a potent inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting an IC50 value of 0.291 μM. This compound effectively inhibits LSD1 activity, making it a valuable tool for studies investigating epigenetic regulation and its implications in various biological processes. Additionally, LSD1-IN-30 can be utilized in research related to cancer, neurobiology, and other disorders associated with dysregulated histone methylation. -
KDM4D Inhibitor
Zavondemstat L-lysine is a selective inhibitor of histone lysine demethylase 4D (KDM4D), a crucial enzyme involved in histone modification and epigenetic regulation. This compound exhibits notable antineoplastic activity, making it valuable in cancer research and investigations into epigenetic therapies. Its ability to modulate histone methylation contributes to the understanding of tumor biology and the development of novel therapeutic strategies targeting KDM4D-related pathways. -
KDM5 Inhibitor
KDOAM-25 is a selective inhibitor of histone lysine demethylases 5 (KDM5) with reported IC50 values of 71 nM, 19 nM, 69 nM, and 69 nM for KDM5A, KDM5B, KDM5C, and KDM5D, respectively. This compound enhances global H3K4 methylation at transcriptional start sites, thereby modulating gene expression. KDOAM-25 demonstrates potential in addressing proliferative disorders, particularly in multiple myeloma cell lines such as MM1S, making it a valuable tool for investigating epigenetic regulation and its implications in cancer research. -
KDM4 inhibitor
NCDM-32B is a selective inhibitor of KDM4, demonstrating IC50 values of 3.0 μM for KDM4A and 1.0 μM for KDM4C in in vitro enzyme assays. This compound significantly enhances global levels of H3K9me3/me2 in basal breast cancer cells, contributing to impaired cell viability in KDM4C-amplified breast cancer cell lines such as HCC1954 and Colo824. NCDM-32B serves as a valuable tool for investigating the role of KDM4 in breast cancer research and therapeutic development. -
LSD1 Inhibitor
CBB1007 hydrochloride is a reversible and selective inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 5.27 µM for human LSD1. It effectively inhibits the demethylase activity of LSD1 on histone substrates H3K4Me2 and H3K4Me, demonstrating selectivity over LSD2 and JARID1A. This compound is involved in promoting the expression of differentiation-related genes in pluripotent cells and finds applications in cancer research, particularly in the study of teratocarcinoma, embryonic carcinoma, and seminoma. -
LSD1 Inhititor
Pulrodemstat Methylbenzenesulfonate is a selective, reversible inhibitor of lysine-specific demethylase-1 (LSD1), exhibiting an IC50 of 0.25 nM. This compound demonstrates minimal inhibition of LSD2, monoamine oxidase A, and monoamine oxidase B. Pulrodemstat Methylbenzenesulfonate effectively induces differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells, showcasing significant anticancer activity. Its targeted action positions it as a valuable reagent in cancer research and therapeutic studies. -
EGFR/LSD1 Inhibitor
ZJY-54 is a potent dual-target inhibitor of EGFR and LSD1, exhibiting IC50 values of 3.8 nM and 0.6 μM, respectively. This compound effectively inhibits the proliferation of non-small cell lung cancer cells and promotes the accumulation of H3K4me2 and H3K9me2 modifications. Additionally, ZJY-54 disrupts the phosphorylation of the EGFR signaling pathway, demonstrating significant anti-tumor activity suitable for cancer research applications. -
LSD1 Inhibitor
T-448 free base is a selective, orally active, and irreversible inhibitor of lysine-specific demethylase 1 (LSD1), targeting H3K4 demethylation with an IC50 of 22 nM. This compound promotes H3K4 methylation in primary cultured rat neurons, making it a valuable tool for investigating epigenetic regulation in neurobiology and related research applications. -
LSD1 Inhibitor
LSD1-IN-13 hydrochloride is a potent inhibitor of the lysine-specific demethylase 1 (LSD1) enzyme, exhibiting an IC50 of 24.43 nM. This compound enhances CD86 expression with an EC50 of 470 nM and promotes the differentiation of acute myeloid leukemia (AML) cell lines. It serves as a valuable tool for research focused on epigenetic regulation and the therapeutic modulation of leukemia. -
LSD1 Inhibitor
Namoline is a selective and reversible inhibitor of Lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 51 μM in HRP-coupled enzymatic assays. This compound effectively impairs the demethylase activity of LSD1, resulting in the inhibition of cell proliferation. Namoline shows promise for applications in research related to androgen-dependent prostate cancer. -
LSD1 Inhibitor
MC2652 is a potent inhibitor of the lysine-specific demethylase 1 (LSD1). It exhibits significant inhibitory effects in MV4-11 and NB4 leukemia cells, indicating strong potential for hematological research. Additionally, MC2652 demonstrates antiproliferative activity against prostate cancer LNCaP cells, making it a valuable tool for exploring therapeutic strategies in oncology. -
LSD1 Inhibitor
FY-21 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 340 nM. This compound demonstrates significant anti-proliferative effects and inhibits colony formation in cancer cells. Additionally, FY-21 enhances p53 expression while down-regulating HOXA9 and MEIS1, contributing to its potential in inducing differentiation in leukemia cells, thereby providing a promising avenue for antitumor research applications. -
KDM4 Inhibitor
KDM4-IN-4 is a potent inhibitor of histone lysine demethylase 4 (KDM4), specifically targeting the Tudor domain of KDM4A with a binding affinity of approximately 80 µM. This compound demonstrates the ability to inhibit the interaction of H3K4Me3 with the Tudor domain in cellular contexts, exhibiting an EC50 value of 105 µM. KDM4-IN-4 is utilized in anticancer research to explore its role in epigenetic regulation and potential therapeutic applications. -
LSD1 Inhibitor
LSD1-IN-34 is a potent inhibitor of Lysine-specific demethylase 1 (LSD1) and monoamine oxidase A (MAO). It demonstrates IC50 values of 4.51 nM for LSD1 and 18.46 nM for MAO A, effectively blocking the activation of neonatal rat myocardial fibroblasts (NRCFs) induced by Ang II, with minimal toxicity at 20 μM. Furthermore, LSD1-IN-34 disrupts the TGFβ/Smad signaling pathway, providing therapeutic potential in ameliorating heart failure in mouse models. The compound also shows favorable pharmacokinetic properties in rats, supporting its use in cardiovascular research. -
LSD1 Inhibitor
LSD1-IN-27 is a potent inhibitor of the lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 13 nM. This compound effectively inhibits the stemness and migratory capacity of gastric cancer cells while decreasing PD-L1 expression in BGC-823 and MFC cell lines. Additionally, LSD1-IN-27 has been shown to enhance T cell immune responses in the context of gastric cancer, making it a valuable tool for research in cancer immunotherapy and cellular differentiation studies.
