Histone Demethylase Inhibitor

LSD1-IN-51 is a selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ value of 8.7 nM. LSD1-IN-51 selectively inhibits H3K4me1/2 demethylation by binding to the FAD domain of LSD1, while disrupting the interaction between LSD1 and multiprotein complexes such as HDAC1/2 and CoREST. LSD1-IN-51 can be used for cancer research.

Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC₅₀ = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells.

DC551040 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.

LSD1-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.

LSD1-IN-45 is an LSD1 inhibitor and a ligand for the target protein for PROTAC. LSD1-IN-45 can be used to synthesize PROTAC LD-110 (HY-178825).

(2R)-Octyl-α-hydroxyglutarate (Standard) is the analytical standard of (2R)-Octyl-α-hydroxyglutarate. This product is intended for research and analytical applications. (2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a modified form of D-isomer 2-Hydroxyglutarate.

Pulrodemstat (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.

Tranylcypromine-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.

GSK-J1 sodium is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC₅₀ value of 60 nM towards KDM6B.

AW4 is a LSD1 inhibitor. AW4 inhibits LSD1 ΔTTAS activity in H3K4me2 demethylation assays. AW4 can be used for research of drug resistance.

LSD1/HDAC-IN-1 (compound 2) is a potent inhibitor of HDAC and LSD1, with IC₅₀s of 0.125 nM, 0.373 nM, 0.0118 nM, 0.103 nM, and 0.571 μM for HDAC1, HDAC2, HDAC6, HDAC8 and LSD1, respectively. LSD1/HDAC-IN-1 plays an important role in cancer research.

JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma.

LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC₅₀ of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC₅₀ of 8.79 μM.

LSD1-IN-36 is a potent LSD1 inhibitor with an IC₅₀ value of 0.8 nM. LSD1-IN-36 induces apoptosis and arrests the cell cycle. LSD1-IN-36 shows antitumor activity.

CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.

GSK-J4 (Standard) is the analytical standard of GSK-J4. This product is intended for research and analytical applications. GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

K_dM2A/7A-IN-1 (Standard) is the analytical standard of K_dM2A/7A-IN-1 (HY-108706). This product is intended for research and analytical applications. K_dM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases K_dM2A/7A, with an IC₅₀ of 0.16 μM for K_dM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.

KDM4D-IN-1 (Standard) is the analytical standard of KDM4D-IN-1 (HY-101928). This product is intended for research and analytical applications. KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC₅₀ value of 0.41±0.03 μM.

S2101 (Standard) is the analytical standard of S2101 (HY-110277). This product is intended for research and analytical applications. S2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 0.99 μM, K_i of 0.61 μM and K_inact/K_i of 4560 M/s.

Tranylcypromine (hemisulfate) (Standard) is the analytical standard of Tranylcypromine (hemisulfate). This product is intended for research and analytical applications. Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects.