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.

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.

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.

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).

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.

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.

FY-21 is a selective LSD1 inhibitor (IC50= 340 nM) that inhibits proliferation and colony formation of leukemia cells, decreases mRNA levels of the transcription factors HOXA9 and MEIS1, and can be used in the study of leukemia.

Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.

Voriconazole (UK-109496) is a triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 [CYP3A].

Tioconazole (Vagistat) is a synthetic imidazole derivative, inhibits cell wall synthesis by inhibiting the biosynthesis of ergosterol or other sterols, damaging the fungal cell membrane, altering its permeability, and promoting loss of essential intracellular elements.

Miconazole (R18134) is an imidazole antifungal agent used both topically and via intravenous infusion.

Econazole ((±)-Econazol) is an imidazole derivative that is commonly used as a topical antifungal agent.

Econazole nitrate (NSC-243115) (Spectazole) is an imidazole class antifungal medicine.

Clotrimazole (FB 5097), an imidazole derivative with a broad spectrum of antimycotic activity, inhibits biosynthesis of the sterol ergostol.