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Catalog No.
Product Name
Application
Product Information
Citations
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Demethylase Inhibitor
GSK J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor; attenuates lipopolysaccharide (LPS)-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 uM for the inhibition of TNF?? release).- Guang Bai, .et al. , Epigenetics of Chronic Pain, 2019, Pages 1-48
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LSD1 inhibitor
GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.- Nicolas A Fraunhoffer, .et al. , EBioMedicine, 2023, Jun;92:104602 PMID: 37148583
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Histone demethylase inhibitor
GSK J1 is a potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX- Nicolas A Fraunhoffer, .et al. , EBioMedicine, 2023, Jun;92:104602 PMID: 37148583
- Guang Bai, .et al. , Epigenetics of Chronic Pain, 2019, Pages 1-48
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Histone Demethylase inhibitor
JIB-04 is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.- Thibaud Reyser, .et al. , Pharmaceutics, 2023, Oct 10;15(10):2440 PMID: 37896200
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LSD1 inhibitor
SP2509 is a novel histone demethylase LSD1 (KDM1A) antagonist with IC50 of 13 nM; no inhibition on MAO-A and MAO-B.- Ziliang Yu, .et al. , Immunol Res, 2024, May 9 PMID: 38722530
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KDM4A inhibitor
Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity. -
LSD1 inhibitor
T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM. -
LSD1 Inhibitor
ORY-1001 is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1. -
KDM inhibitor
2,4-Pyridinedicarboxylic Acid (2,4-PDCA) is an inhibitor of histone lysine-specific demethylases that targets on JMJD2A (KDM4A), KDM4C, KDM4E (IC50, 1.4 μM), KDM5B (IC50, 3 μM), KDM6A and other 2-oxogynases. -
KDM2/7 inhibitor
TC-E 5002, selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 uM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). Inhibits growth of HeLa and KYSE-150 cancer cells in vitro. -
KDM4D inhibitor
KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM. -
KDM2A/7A inhibitor
KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16?μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases. -
LSD1 inhibitor
Seclidemstat (SP-2577) is a potent and orally bioavailable LSD1 inhibitor, with a mean IC50 of 127 nM. -
LSD1/MAO-B inhibitor
Vafidemstat (ORY-2001) is a dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor. -
KDM5 inhibitor
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. -
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. -
LSD Inhibitor
N-Benzylideneaniline is a selective inhibitor of xylinostilbene-α,β-dioxygenase (LSD), a key enzyme involved in the oxidative degradation of lignin. This compound exhibits significant biological activity in influencing lignin metabolism, making it valuable for studies on lignocellulosic biomass conversion. Its applications extend to research focusing on environmental biochemistry and the enzymatic processes governing plant biomass degradation. -
LSD1 Inhibitor
INCB059872 is a potent and selective irreversible inhibitor of Lysine-Specific Demethylase 1 (LSD1). This compound demonstrates strong biological activity in the modulation of histone methylation, making it a valuable tool for investigating epigenetic regulation. INCB059872 is particularly relevant for research applications focused on myeloid leukemia and other hematological malignancies, providing insights into therapeutic strategies targeting LSD1-dependent pathways. -
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. -
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.
