demethylase

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3/me2 demethylases JMJD3/KDM6B and UTX/KDM6A (IC50=8.6/6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

5-[(1S,2S)-2-[(Cyclopropylmethyl)amino]cyclopropyl]-N-(tetrahydro-2H-pyran-4-yl)thiophene-3-carboxamide hydrochloride is a cyclopropanoid enzyme compound that acts as a lysine-specific demethylase-1 inhibitor for schizophrenia, developmental disorders, and neurodegenerative diseases.

GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.

FB23-2 is a potent and selective inhibitor of the mRNA N6-methyladenosine (m6A) demethylase FTO with an IC50 of 2.6 μM.

FB23 directly binds to FTO and selectively inhibits FTO's m6A demethylase activity. (FTO, an mRNA N6-methyladenosine (m6A) demethylase, was reported to promote leukemogenesis.)

PFI-90, a selective histone demethylase (KDM3B) inhibitor, targets PAX3-FOXO1 action and demonstrates potential antitumor activity. It induces apoptosis and myogenic differentiation, leading to increased cell death.

14α-Demethylase-IN-1 (compound 2e) is an inhibitor of 14α-demethylase and serves as an antifungal agent. For Candida albicans, Candida parapsilosis, Candida krusei, and Candida glabrata, the MIC50 values recorded at 48 hours are 2.47 μM, 1.23 μM, 19.70 μM, and 19.70 μM respectively.

Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).1,2LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 μM.1It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.2LSD inhibitor (1C) also induces re-expression of the Wnt signaling pathway proteins secreted frizzle-related protein 1 (SFRP1), SFRP4, and SFRP5, as well as the transcription factor GATA5, which are aberrantly silenced in HCT116 cells.

14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase and DNA Gyrase, exhibiting significant antibacterial activity.

14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase, exhibiting antibacterial activity.

KDM4-IN-4 (compound 47) is a potent inhibitor of histone lysine demethylase 4 (KDM4), with a binding constant of approximately 80 μM for the KDM4A-Tudor domain. It inhibits H3K4Me3 binding to the Tudor domain in cellular contexts with an EC50 value of 105 μM, holding potential for anticancer research applications [1].

Zavondemstat (QC8222 free base) is a histone lysine demethylase 4 (KDM4) inhibitor with anticancer and antitumor activity for the study of triple-negative and breast cancers.

Bomedemstat (IMG-7289), an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor, shows activity in mouse myeloproliferative neoplasm (MPN) models. This compound exhibits antineoplastic effects and can be used for acute myeloid leukemia (AML) and myelofibrosis (MF) research.

Corin is an irreversible inhibitor of HDAC1(IC50 = 147 nM) and LSD1(Ki = 110 nM).

DDP-38003 dihydrochloride is an orally available histone lysine-specific demethylase 1A (KDM1A/LSD1) inhibitor (IC50: 84 nM).

KDM2A/7A-IN-1 is a cell-permeable and selective inhibitor of histone lysine demethylase KDM2A/7A, with potential antitumor activity for studying duodenal adenomas and ossifying fibromucoid tumors.

PC945 (Opelconazole) is a potent broad-spectrum antifungal compound with inhibitory effect on fumonisinol 14α-demethylase (CYP51A/CYP51B), which can be used in the study of fungal infections of the lungs.

T-448 is a specific, orally active, and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) with an IC50 of 22 nM.

QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).

Azalanstat (RS 21607) is an orally available selective mammalian lanosterol 14-alpha-demethylase inhibitor with hypocholesterolemic activity that inhibits cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes, and hamster livers through inhibition of the cytochrome P450 enzyme, lanosterol 14 alpha demethylase.

TAK-418 is a selective and orally active inhibitor of LSD1/KDM1A enzyme with an IC50 of 2.9 nM. TAK-418 unlocks abnormal epigenetic mechanisms and improves autism symptoms in models of neurodevelopmental disorders.

Pulrodemstat (CC-90011) is an orally active, selective, and highly efficient lysine-specific demethylase-1 (LSD1) inhibitor with anticancer activity. It inhibits HNSCC cell proliferation and migration by triggering apoptosis and inhibiting head and neck squamous cell carcinoma growth.

Lsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.

Bomedemstat ditosylate (IMG-7289 ditosylate) is an orally active lysine-specific demethylase 1 (LSD1) inhibitor with antitumor activity that potentiates the response to PD-1 inhibition in a homozygous model of SCLC, inhibits cancer cell proliferation, and induces apoptosis. Bomedemstat ditosylate can be used to study myeloproliferative neoplasms and myelofibrosis.