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

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/DNA Gyrase with antibacterial activity.

Clausine E is an inhibitor of fat mass and obesity-associated protein (FTO) demethylase activity. The binding of Clausine E to FTO was driven by positive entropy and negative enthalpy changes.

GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

KDM5-C49 HCl (KDOAM-20 hydrochloride) is a potent and selective inhibitor of KDM5 demethylase. KDM5-C49 HCL(1596348-16-1 Free base) is a candidate compound for the treatment of cancer.

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 (GSK J4 HCl) is a potent H3K27me3 demethylase inhibitor, with IC50s of 8.6 μM and 6.6 μM towards KDM6B and KDM6A respectively. It is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.

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.

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

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.

KDM4-IN-4 is a selective histone lysyl demethylase 4 (KDM4) inhibitor with anticancer activity, inhibits the KDM4A-Tudor structural domain, and inhibits intracellular binding of H3K4Me3 to the Tudor structural domain.KDM4-IN-4 is used in the study of cancer, obesity, and cardiovascular disease.

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

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.

T-448 is an orally available and potent lysine-specific demethylase 1 inhibitor (IC50: 22 nM) that improves learning function in mice.T-448 can be used to study memory deficits.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.

KDM5-C70 is an ethyl ester derivative of KDM5-C49. KDM5-C70 is an effective, cell-permeable, and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, inducing a genome-wide elevation of H3K4me3 levels.

IOX1 is the most effective broad-spectrum 2OG oxygenases(including the JmjC demethylases) inhibitor. The IC50 of IOX1 for KDM4A, KDM3A, is 0.6 and 0.1 uM, respectively.

AS8351 (NSC51355) is a histone demethylase inhibitor. It has been used in combination with CHIR99021, A 83-01, BIX01294, SC-1, Y-27632, OAC2, SU 16f, and JNJ-10198409 to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.

ORY1001 (ORY 1001) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor, with high selectivity against related FAD dependent aminoxidases with IC50 of <20 nM.

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

CPI-455 is a specific KDM5 inhibitor.

INCB059872 is a highly potent, orally active, selective, and irreversible inhibitor of Lysine-Specific Demethylase 1 (LSD1). Its chemical properties make it suitable for use in researching myeloid leukemia.

Pulrodemstat (CC-90011) is a highly potent and selective inhibitor of lysine specific demethylase-1 (LSD1). It exhibits a reversible mode of action and can be administered orally. With an impressive IC50 of 0.25 nM, Pulrodemstat effectively suppresses the enzymatic activity of LSD1. Notably, it demonstrates minimal inhibition against LSD2, MOA-A, and MAO-B enzymes. Moreover, Pulrodemstat possesses remarkable anticancer properties, promoting differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells.

GSK-690 is a selective and potent inhibitor of lysine demethylase 1 (LSD 1), which induces differentiation of leukemic stem cells in acute myeloid leukemia (AML), and can be used in the study of leukemias.

E67-2, a derivative of E67, is a low-toxicity, selective inhibitor of the KIAA1718 Jumonji domain. It has an IC 50 value of 3.4 μM. E67-2 specifically inhibits the Jumonji demethylase for histone H3 lysine 9 (H3K9) and histone H3 lysine 4 (H3K4) demethylase.

FTO-IN-10 (compound 7), a potent inhibitor of the human demethylase FTO (fat mass and obesity-associated protein), exhibits an IC50 of 4.5 μM. It interacts with the binding pocket of FTO's structural domain II via hydrophobic and hydrogen bonding interactions, and promotes DNA damage and autophagic cell death in A549 cells [1].

LSD1-IN-30 is a lysine-specific demethylase 1 (LSD1) inhibitor with anticancer activity for the study of small cell lung cancer and acute myeloid leukemia.

Bifonazole (Bay H-4502) acts to destabilize the fungal cytochrome p450 51 enzyme (also known as Lanosterol 14-alpha-demethylase). It works by inhibiting the production of a substance called ergosterol, which is an essential component of fungal cell membranes. This is vital in the cell membrane structure of the fungus. Its inhibition leads to cell lysis. The disruption in production of ergosterol disrupts the cell membrane and causes holes to appear. The cell membranes of fungi are vital for their survival. They keep unwanted substances from entering the cells and stop the contents of the cells from leaking out.

lutidinic acid (2,4-Dicarboxypyridine) is an in vitro and in cell inhibitor, as well as a known inhibitor of the histone lysine demethylases.

SD49-7 is an inhibitor of histone lysine demethylase 4 (KDM4) with an IC50 of 0.19 µM.

Antifungal agent 68 (compound 10) effectively combats fungal infections caused by Candida and Cryptococcus gattii through the inhibition of ergosterol biosynthesis, likely via interaction with lanosterol 14α-demethylase (CYP51). It is proposed that the imidazole ring of antifungal agent 68 interacts with the heme group of CYP51 [1].

Compound A5b, also known as JMJD3/HDAC-IN-1, is a dual inhibitor that targets both JMJD3 (Jumonji domain-containing protein demethylase 3) and HADC1 (histone deacetylase, IC50 = 16 nM). It induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, while also promoting apoptosis through the cleavage of caspase-7 and PARP. This compound has demonstrated the ability to effectively inhibit cancer cell cloning, migration, and invasion [1].

KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).

FTO-IN-7d is the first inhibitor of the RNA demethylase FTO with anticonvulsant activity.

KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.

SK&F 104976 is a 32-carboxylic acid derivative of lanosterol. It was found to be a potent lanosterol 14 alpha-demethylase (14 alpha DM) inhibitor.

A 60586, a non-azole inhibitor of ergosterol biosynthesis, inhibits lanosterol 14alpha-demethylase and displays in-vitro antifungal activity.

Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and HIF-2α in Hep3B hepatocellular carcinoma cells. It increases levels of secreted erythropoietin in Hep3B cells in a concentration-dependent manner and increases erythropoiesis in rats when administered at doses of 25 and 50 mg/kg. Roxadustat reverses anemia in a rat model of chronic inflammation induced by peptidoglycan-polysaccharide, as well as a rat model of chronic kidney disease induced by 5/6 nephrectomy. It reduces tumor growth and increases survival in a murine Lewis lung carcin......

Tranylcypromine hemisulfate (Tranylcypromine Sulfate) is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.

Tebuconazole-d9 is intended for use as an internal standard for the quantification of tebuconazole by GC- or LC-MS. Tebuconazole is a triazole fungicide that is active against both seed and foliar fungi. It inhibits 14α-demethylase isolated from U. maydis and S. bicolor with IC50 values of 0.05 and 0.16 nM, respectively. It inhibits the androgenic effect of the androgen receptor agonist DHT (IC20 = 2.89 µM) and is cytotoxic (EC20 = 38.9 µM) in an MDA-kb2 assay. Tebuconazole (50 and 100 mg/kg per day) administered during gestation reduces testosterone levels and increases testicular levels of progesterone and 17α-hydroxyprogesterone in male rat fetuses. It has a feminizing effect on male pups and a virializing effect on female pups. When administered to rats gestationally through postnatal day 42, tebuconazole (20 and 60 mg/kg per day) leads to cell death of pyramidal cells in the CA3-4 region of the hippocampus and layer V of the cortex concomitant with impairment in learning......

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.

RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).

L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium) is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity(Km and Ki of 2.52 mM and 11.13 mM, respectively).

Namoline is a γ-pyrone compound that functions as a selective and reversible inhibitor of Lysine-specific demethylase 1 (LSD1) with an IC50 of 51 μM in an HRP-coupled enzymatic assay. By impairing LSD1 demethylase activity, Namoline effectively inhibits cell proliferation. Due to its characteristics, Namoline holds promise for research pertaining to androgen-dependent prostate cancer.

Seclidemstat (SP-2577) is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.

Daminozide (Succinic Acid) is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.

Quilseconazole besylate, also known as VT-1129 besylate, is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor.

GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).

Antifungal agent 40 is an antifungal agent that extends into the narrow hydrophobic pocket II of C. alb. CYP51 and inhibits the activity of lanosterol 14α-demethylase (CYP51), which has an inhibitory effect on biofilm formation.