Catalog No.
Product Name
Application
Product Information
Citations
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LSD1/EGFR Inhibitor
LSD1/EGFR-IN-1 is a potent inhibitor of lysine-specific demethylase 1 (LSD1) and several mutant forms of the epidermal growth factor receptor (EGFR), specifically EGFRT790M/L858R and EGFRL858R/T790M/C797S, exhibiting IC50 values of 6.24 μM, 2.06 μM, and 5.01 μM, respectively. This compound is significant for cancer research, particularly in studies focusing on targeted therapies and resistance mechanisms associated with EGFR mutations. Its application in preclinical models can aid in the understanding of tumorigenesis and the efficacy of combination therapies. -
HSP90/LSD1 Inhibitor
HSP90/LSD1-IN-1 is a dual inhibitor targeting HSP90 and LSD1, effectively disrupting their interaction and function. This compound demonstrates significant antiproliferative activity in prostate cancer cell lines, exhibiting GI50 values of 0.24 μM for PC-3 and 0.30 μM for DU145. It is a valuable tool for research into therapeutic strategies against prostate cancer and the role of chaperone proteins and histone demethylases in tumor biology. -
JARID1B Inhibitor
YU185530 is a selective inhibitor of JARID1B, a histone demethylase involved in the regulation of gene expression. It has demonstrated biological activity in modulating epigenetic landscapes associated with cancer progression. This compound is primarily utilized in cancer research to explore the therapeutic potential of targeting JARID1B in various malignancies. -
KDM1A Inhibitor
DDP-38003 is a potent inhibitor of KDM1A/LSD1, with an IC50 value measured at 84 nM. This compound demonstrates significant anticancer activity, particularly against promyelocytic leukemia cells. DDP-38003 is suitable for research applications focused on gene regulation, epigenetic modulation, and cancer therapeutics. -
LSD1 Inhibitor
LSD1-UM-109 is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting an IC50 of 3.1 nM. It demonstrates significant antiproliferative activity, with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line. This compound is valuable for research into cancer biology and the epigenetic regulation of gene expression, making it a crucial tool for studying LSD1’s role in various malignancies. -
LSD1 Inhibitor
LSD1-IN-41 is a potent and selective inhibitor of lysine-specific demethylase 1 (LSD1). It demonstrates significant biological activity in cancer research, particularly in the context of diffuse intrinsic pontine glioma (DIPG), especially when used in combination with histone deacetylase (HDAC) inhibitors. This compound serves as a valuable tool for investigating epigenetic regulation and therapeutic strategies in cancer treatment. -
KDM4C Inhibitor
KDM4C-IN-2 is a selective inhibitor of the histone lysine demethylase KDM4C, exhibiting an IC50 value of 147 μM and a Ki of 51 μM. This compound plays a crucial role in regulating histone methylation, making it valuable for cancer research, particularly in the study of prostate and breast cancer. KDM4C-IN-2 can aid in understanding the epigenetic mechanisms underlying tumorigenesis and potential therapeutic strategies. -
LSD1 Inhibitor
INCB059872 tosylate is a potent, selective inhibitor of lysine-specific demethylase 1 (LSD1). By binding to and inhibiting LSD1, this compound enhances H3K4 methylation, which increases the expression of tumor suppressor genes. Additionally, the inhibition of LSD1 promotes H3K9 methylation, leading to a decrease in the transcription of genes associated with tumor promotion. Its properties make INCB059872 tosylate valuable for research on epigenetic regulation and cancer therapy. -
LSD1 Inhibitor
S1427 is a tranylcypromine-derived inhibitor of lysine-specific demethylase 1 (LSD1) with an IC50 of 390 nM and a Ki of 80 nM. This compound demonstrates selective inhibition of the hERG channel and displays favorable microsomal stability profiles. S1427 has been shown to partially reduce the proliferation of cancer cells, making it a valuable tool for research in cancer biology and epigenetic regulation. -
LSD1 Inhibitor
LSD1-IN-23 is a mixed inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting both competitive and non-competitive inhibition patterns. With an IC50 value of 0.58 μM, it effectively inhibits LSD1 activity, making it a valuable tool for investigating the role of LSD1 in neuroblastoma (NB) research and related studies on cancer epigenetics. -
LSD Inhibitor
LSD1/2-IN-4 is an inhibitor of lysine-specific demethylase 1 (LSD1) and lysine-specific demethylase 2 (LSD2), exhibiting Ki values of 0.11 μM and 130 μM, respectively. This compound selectively inhibits demethylase activity, making it valuable for studying epigenetic regulation in various biological processes. LSD1/2-IN-4 has potential applications in cancer research, including investigations into T-cell acute lymphoblastic leukemia (TALL), providing insights into therapeutic strategies targeting demethylase pathways. -
LSD1 Inhibitor
NCL1 is a selective inhibitor of Lysine-specific demethylase 1 (LSD1), a pivotal enzyme in the regulation of gene expression through histone modification. With an IC50 value of 2.5 μM for LSD1 and 26 μM for LSD2, NCL1 demonstrates a preferential inhibition of LSD1 over its close homolog. This compound is primarily utilized in research applications related to epigenetics, cancer biology, and neurodegenerative disorders, facilitating investigations into the molecular mechanisms of gene regulation. -
LSD1 Inhibitor
cis-4-Br-2,5-F2-PCPA is a selective inhibitor of lysine-specific demethylase 1 (LSD1), demonstrating a Ki value of 94 nM for LSD1 compared to 8.4 μM for LSD2. This compound effectively inhibits LSD1 activity, resulting in reduced proliferation of cancer stem cells by increasing the levels of dimethylated histone H3 at lysine 4 (H3K4) in CCRF-CEM cells. Its selective action makes cis-4-Br-2,5-F2-PCPA a valuable tool for research on epigenetic regulation and cancer biology. -
KDM5 Demethylases Inhibitor
KDM5-C49 is a potent and selective inhibitor of KDM5 demethylases, exhibiting IC50 values of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C, respectively. This compound plays a critical role in epigenetic research, particularly in the study of cancer biology. It provides valuable insights into the mechanisms of gene regulation and the potential therapeutic strategies targeting KDM5 demethylases in cancer treatment. -
LSD1 Inhibitor
LSD1-IN-48 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), featuring a tranylcypromine-pyrimidine structure with a human IC50 of 7.87 nM. This compound enhances histone methylation levels of H3K4me1 and H3K4me2, promoting apoptosis in cancer cells. Additionally, LSD1-IN-48 upregulates CD86 and downregulates SOX2 and CD44, leading to reduced cell proliferation. It is particularly useful for research into acute myeloid leukemia. -
LSD1 Inhibitor
LSD1-IN-35 is a selective inhibitor of lysine-specific demethylase 1 (LSD1) with an IC50 of 108 nM. By inhibiting the demethylation of H3K4me1/2, LSD1-IN-35 acts as an immunomodulator, enhancing the response of gastric cancer cells to T-cell-mediated cytotoxicity. This compound decreases PD-L1 expression, thereby mitigating the PD-1/PD-L1 interaction, which is critical in tumor immune evasion. Its potential applications include cancer research and the study of immune regulation in tumor microenvironments. -
LSD1 Inhibitor
LSD1-IN-18 is a selective, non-covalent inhibitor of LSD1, exhibiting a Ki of 0.156 μM and a KD of 0.075 μM. It demonstrates significant antiproliferative effects in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with calculated IC50 values of 0.16 μM and 0.21 μM, respectively, after 72 hours of treatment. This compound provides a valuable tool for investigating the role of LSD1 in cancer biology and therapeutic applications. -
KDM5A/5B Histone Lysine Demethylase Inhibitor
N19-0881 is a selective inhibitor of KDM5A and KDM5B histone lysine demethylases, exhibiting potent activity with IC50 values of 0.013 μM and 0.002 μM, respectively. This compound demonstrates significant potential in the study of epigenetically dysregulated tumors, particularly in applications related to breast cancer research. Its oral bioactivity makes it an effective tool for investigating the role of histone modification in cancer biology and therapeutic development. -
LSD1 Inhibitor
Bizine di(hydrochloride) is a potent and selective inhibitor of the lysine-specific demethylase 1 (LSD1) enzyme, exhibiting a Ki value of 59 nM. This compound effectively modulates bulk histone methylation in cancer cells, making it valuable for epigenetic studies related to cancer biology. Additionally, Bizine di(hydrochloride) demonstrates neuroprotective effects, supporting its potential applications in neurological research. -
LSD1 Inhibitor
3β-Acetoxyl-atractylenolide I is a potent inhibitor of lysine-specific demethylase 1 (LSD1), demonstrating an IC50 of 57 μM. This compound has been shown to effectively block tumor growth, metastasis, and invasion across various cancer types. It is utilized in research focusing on prostate cancer, breast cancer, neuroblastoma, gastric cancer, colon cancer, bladder cancer, esophageal cancer, acute myeloid leukemia, and retinoblastoma. -
JMJD3/UTX Inhibitor
GSK-J4 hydrochloride is a potent dual inhibitor of the demethylases JMJD3 (KDM6B) and UTX (KDM6A), with IC50 values of 8.6 μM and 6.6 μM, respectively. This compound demonstrates significant inhibition of LPS-induced TNF-α production in human primary macrophages, with an IC50 of 9 μM. GSK-J4 hydrochloride serves as a cell-permeable proagent of GSK-J1 and is valuable for research into epigenetic regulation and inflammation-related pathways. -
KDM5 Inhibitor
KDM5-C70 is a potent and cell-permeable pan-KDM5 histone demethylase inhibitor, derived from KDM5-C49 as an ethyl ester. It exhibits significant antiproliferative activity in myeloma cells, effectively increasing global levels of H3K4me3. KDM5-C70 is valuable for research exploring epigenetic regulation and its implications in cancer biology. -
LSD1/KDM1A Inhibitor
GSK2879552 dihydrochloride is a selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A). This compound exhibits potential antineoplastic activity, making it valuable in cancer research. Its ability to modify epigenetic regulation through LSD1 inhibition allows for exploration of therapeutic strategies in malignancies where LSD1 is implicated. -
KDM5 Inhibitor
KDOAM-25 citrate is a selective inhibitor of histone lysine demethylases 5 (KDM5) with IC50 values of 71 nM, 19 nM, 69 nM, and 69 nM for KDM5A, KDM5B, KDM5C, and KDM5D, respectively. This compound is known to enhance global H3K4 methylation at transcriptional start sites, thereby influencing gene expression. Its activity contributes to the inhibition of proliferation in multiple myeloma MM1S cells, making it a valuable tool for research in epigenetics and cancer biology. -
KDM5B Inhibitor
TK-129 is a potent inhibitor of KDM5B, exhibiting low toxicity and high affinity with an IC50 of 44 nM. By targeting KDM5B, TK-129 disrupts the KDM5B-associated Wnt signaling pathway, resulting in cardioprotective effects. This compound effectively reduces angiotensin II-induced activation of cardiac fibroblasts in vitro and mitigates isoprenaline-induced myocardial remodeling and fibrosis in vivo. TK-129 is valuable for research in cardiovascular disease mechanisms and therapeutic strategies. -
JMJD6 Inhibitor
JMJD6-IN-1 is a selective inhibitor of JMJD6, demonstrating an inhibition rate of 82% at a concentration of 10 μM. It effectively reduces the proliferation of MCF-7 and HCC4006 cancer cell lines, with IC50 values of 19.2 μM and 25.2 μM, respectively. This compound is suitable for research applications focused on cancer biology and the exploration of JMJD6’s role in tumorigenesis. -
KDM4C Inhibitor
KDM4C-IN-1 is a potent inhibitor of the lysine demethylase KDM4C, exhibiting an IC50 of 8 nM. This compound has demonstrated significant biological activity by inhibiting the proliferation of HepG2 and A549 cancer cell lines, with IC50 values of 0.8 µM and 1.1 µM, respectively. KDM4C-IN-1 is a valuable tool for research applications related to cancer biology and epigenetic regulation. -
KDM1A/LSD1 Inhibitor
DDP-38003 dihydrochloride is a novel orally bioavailable inhibitor of the lysine-specific demethylase 1A (KDM1A/LSD1) enzyme, demonstrating an IC50 of 84 nM. This compound is valuable for research applications involving epigenetic regulation and modulation of gene expression. Its inhibitory properties make it a pertinent tool for studies in cancer biology and potential therapeutic strategies targeting KDM1A/LSD1 pathways. -
LSD1 Enzyme Inhibitor
TAK-418 is a selective inhibitor of the lysine-specific demethylase 1 (LSD1, KDM1A) enzyme, exhibiting an IC50 of 2.9 nM. This compound modulates epigenetic regulation and has demonstrated efficacy in improving symptoms associated with autism in neurodevelopmental disorder models. Its ability to target LSD1 makes it a valuable tool for research into epigenetic mechanisms and potential therapeutic strategies for related disorders. -
KDM4A/KDM4B Inhibitor
NSC636819 is a competitive and selective inhibitor of the lysine demethylases KDM4A and KDM4B. By targeting these enzymes, NSC636819 may impede the progression of prostate cancer, thereby serving as a valuable tool in cancer research. Its application is particularly relevant for studies aimed at understanding the role of KDM4A/KDM4B in oncogenesis and potential therapeutic strategies for prostate cancer. -
KDM2B Inhibitor
KDM2B-IN-2 is a potent inhibitor of the histone demethylase KDM2B, demonstrating an IC50 of 0.021 μM in a KDM2B TR-FRET assay. This compound is utilized in research focused on hyperproliferative diseases, providing insights into epigenetic regulation and potential therapeutic applications. Its high specificity and efficacy make it a valuable tool for studying the role of KDM2B in various biological contexts. -
KDM5 Demethylases Inhibitor
KDM5-C49 hydrochloride is a potent and selective inhibitor of KDM5 demethylases, demonstrating IC50 values of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C, respectively. This compound is instrumental for research investigating the role of KDM5 demethylases in cancer biology. Its specificity and inhibitory potency make KDM5-C49 hydrochloride a valuable tool for elucidating the mechanisms of cancer progression and potential therapeutic targets. -
LSD1 Inhibitor
Seclidemstat mesylate is a potent noncompetitive and reversible inhibitor of the lysine-specific demethylase 1A (LSD1/KDM1A), with a Ki of 31 nM and an IC50 of 13 nM. This compound enhances antitumor immunity in ovarian cancer associated with SWI/SNF complex mutations and demonstrates efficacy in inhibiting viral production, DNA replication, and late gene expression. Seclidemstat mesylate is suitable for research applications in Ewing Sarcoma and other malignancies involving LSD1 modulation. -
KDM5 Inhibitor
CPI-455 hydrochloride is a potent pan-KDM5 inhibitor, exhibiting an IC50 of 10 nM for KDM5A. This compound effectively inhibits KDM5 activity, leading to an increase in global levels of H3K4me3. It has demonstrated the ability to reduce the population of drug-tolerant persister cancer cells across various cancer cell line models subjected to standard chemotherapy or targeted treatments, making it a valuable tool for cancer research and therapeutic development. -
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
S2116 is a potent inhibitor of lysine-specific demethylase 1 (LSD1), derived from N-alkylated tranylcypromine (TCP). This compound enhances H3K9 methylation while concurrently promoting H3K27 deacetylation at super-enhancer regions. S2116 effectively induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by downregulating the transcription of NOTCH3 and TAL1 genes, and it has demonstrated significant growth inhibition of T-ALL cells in xenotransplanted mouse models. This reagent holds potential for research applications in cancer biology and epigenetic regulation. -
LSD1 Inhibitor
S2157 is a potent inhibitor of lysine-specific demethylase 1 (LSD1), derived from N-alkylated tranylcypromine (TCP). It enhances H3K9 methylation while concurrently promoting H3K27 deacetylation at super-enhancer regions, contributing to its apoptotic effects in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells through the repression of NOTCH3 and TAL1 gene transcription. Additionally, S2157 demonstrates efficient penetration of the blood-brain barrier, effectively eliminating CNS leukemia in mouse models transplanted with T-ALL cells, making it a valuable tool for cancer research. -
LSD1 Inhibitor
Geranylgeranoic acid is a Lysine-specific demethylase 1 (LSD1) inhibitor, exhibiting an IC50 value of 46.97 µM. This isoprenoid compound has demonstrated significant apoptosis-inducing properties through the disruption of mitochondrial membrane potential and the activation of caspase pathways, specifically interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32). Geranylgeranoic acid is applicable in cancer research and is derived from S. chinensis, highlighting its potential as an anticancer agent in studies involving human hepatoma cells and mouse hepatocytes. -
JMJD3/HDAC1/HDAC6 Inhibitor
JMJD3/HDAC-IN-1 is a dual inhibitor targeting both Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylases HDAC1 and HDAC6. With an IC50 value of 16 nM for HDAC1, this compound induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, promoting apoptosis through cleavage of caspase-7 and PARP. JMJD3/HDAC-IN-1 demonstrates significant anti-cancer activity by inhibiting cell cloning, migration, and invasion, making it valuable in cancer research and therapeutic studies. -
KDM1A Inhibitor
Iadademstat is a selective inhibitor of KDM1A (LSD1) that demonstrates potent antileukemic activity. This orally active compound is particularly relevant for research involving relapsed or refractory acute myeloid leukemia. Its mechanism of action and specificity make it a valuable tool for exploring the therapeutic potential of KDM1A inhibition in hematological malignancies. -
JMJD6 Inhibitor
SKLB325 is a selective inhibitor of Jumonji domain-containing 6 (JMJD6) with a binding affinity (KD) of 0.755 μM and an IC50 value of 0.7797 μM. This compound demonstrates significant antitumor activity against ovarian cancer in both in vivo and in vitro models, effectively inducing apoptosis. Additionally, SKLB325 has shown impressive efficacy in renal cell carcinoma (RCC), making it a valuable tool for cancer research and therapeutic exploration. -
KDM3B Inhibitor
PFI-90 is a selective inhibitor of the histone demethylase KDM3B, effectively inhibiting the action of PAX3-FOXO1. This compound induces apoptosis and promotes myogenic differentiation, leading to increased cell death. PFI-90 exhibits potential antitumor activity, making it a valuable tool for cellular and cancer research studies. -
LSD1 Inhibitor
Bomedemstat ditosylate is a potent and irreversible inhibitor of lysine-specific demethylase 1 (LSD1). By inhibiting LSD1, Bomedemstat ditosylate increases methylation levels of H3K4 and H3K9, leading to significant alterations in gene expression. This compound demonstrates notable anti-cancer properties, effectively inhibiting cancer cell proliferation and inducing apoptosis, making it a valuable tool for cancer research and therapeutic development. -
Histone Demethylases Inhibitor
Methylstat is a potent inhibitor of histone demethylases, effectively suppressing the activity of these enzymes. It demonstrates notable anti-proliferative effects with minimal cytotoxicity, inducing apoptosis and causing cell cycle arrest at the G0/G1 phase. Methylstat enhances the expression of key regulatory proteins such as p53 and p21, and it also inhibits cytokine-induced angiogenesis. This compound serves as a valuable chemical probe for investigating the role of histone demethylation in cancer biology and angiogenesis-related research. -
KDM2B Inhibitor
KDM2B-IN-4 is a potent inhibitor of the histone demethylase KDM2B, exhibiting an IC50 of 1.12 nM. This compound plays a crucial role in the modulation of histone methylation, making it valuable for research on hyperproliferative conditions, including various types of cancer. Its ability to inhibit KDM2B provides insights into epigenetic regulation and potential therapeutic strategies for tumorigenesis. -
KDM5A Inhibitor
JQKD82 trihydrochloride is a selective inhibitor of the lysine-specific demethylase KDM5A. By inhibiting KDM5A, JQKD82 trihydrochloride effectively increases levels of trimethylated histone H3 at lysine 4 (H3K4me3), making it a valuable tool for studying epigenetic regulation. This compound is particularly relevant for research applications focused on multiple myeloma and other cancers driven by alterations in histone methylation patterns. -
KDM4 Inhibitor
KDM4-IN-3 is a selective inhibitor of the KDM4 family of lysine demethylases, with an IC50 of 871 nM. This compound demonstrates enhanced potency in biochemical assays and is cell-permeable, effectively inducing cytotoxicity in prostate cancer cell lines at low micromolar concentrations. KDM4-IN-3 inhibits cell growth while increasing the levels of trimethylated histone H3 at lysine 9 (H3K9me3), making it a valuable tool for research focused on prostate cancer biology and epigenetic regulation. -
KDM2B Inhibitor
KDM2B-IN-1 is a potent inhibitor of the histone demethylase KDM2B, exhibiting an IC50 of 0.016 nM. This compound is valuable for investigating hyperproliferative diseases, as it modulates epigenetic regulation and gene expression. Its ability to inhibit KDM2B provides essential insights into potential therapeutic strategies targeting cellular growth and transformation. -
LSD1 Inhibitor
Arborinine is a potent inhibitor of lysine-specific demethylase 1 (LSD1), known for its capacity to modulate histone methylation marks, specifically increasing H3K4me1/2 and H3K9me1/2 levels while decreasing UBE2O protein expression. This compound effectively induces cell cycle arrest at the S phase and demonstrates significant antitumor activity. Arborinine serves as a valuable tool for research in cancer biology and epigenetic regulation. -
KDM3B Inhibitor
P3FI-63 is a selective inhibitor of the lysine demethylase KDM3B, with an IC50 value of 7 μM. This compound demonstrates notable antitumor activity, making it a valuable tool for cancer research. Its specificity for KDM3B allows for the exploration of its role in histone methylation dynamics and potential therapeutic applications in oncology.
