Histone Demethylase

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.

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.

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

Tranylcypromine (2-PCPA) hydrochloride (SKF-385 HCl), a Monoamine Oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression.

Eicosapentaenoic Acid (EPA) is a ω-3 fatty acid abundantly available in marine organisms.

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.

GSK-LSD1 is a selective LSD1 inhibitor with potential anticancer activity that attenuates the expression of CTGF CCN2, MMP13, LOXL4, and waveform proteins in cancer cells.GSK-LSD1 regulates the cell cycle, induces apoptosis, and can be used to study breast cancer.

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

PBIT inhibits JARID1B histone demethylase (IC50 of about 3 μM). PBIT also inhibits JARID1A and JARID1C (IC50s of 6 μM and 4.9 μM, respectively). PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes .

Vafidemstat (ORY-2001) is a selective, orally active lysyl-histone demethylase (LSD1) MAO-B inhibitor that crosses the blood-brain barrier for the study of neurological diseases.

YUKA1, a cell-permeable KDM5A inhibitor (IC50=2.66 μM) with a weak effect on KDM5C (IC50=7.12 μM) and no effect on other KDM isoforms, was able to increase the level of H3K4me3 in human cells and inhibit the proliferation of cancer cells, and also prevented the emergence of drug-resistant cells.

GSK J5 is an inhibitor of schistosomes and helminths and is often used as a trematode insecticide.GSK J5 promotes schistosome mortality in a dose- and time-dependent manner.GSK J5 increases the mortality rate of schistosomes and decreases the viability of adult worms.GSK J5 is an inhibitor of schistosomes and helminths and is often used as a trematode insecticide.

HDAC3-IN-T247 (HDAC3 inhibitor T247) is a selective and potent histone deacetylase 3 (HDAC3) inhibitor with anticancer and antiviral activities.HDAC3-IN-T247 induces NF-κB acetylation in human colon cancer HCT116 cells in a dose-dependent manner.HDAC3-IN-T247 inhibits cancer cell proliferation. HDAC3-IN-T247 inhibits cancer cell proliferation.

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.

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

KDM4C-IN-1 is a selective and potent KDM4C inhibitor (IC50: 8 nM) with potential anticancer activity.KDM4C-IN-1 inhibits the growth of HepG2 and A549 cells, and can be used for the study of leukaemia.

LSD1-IN-25 (Compound 9j) is a potent, selective, and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM) that induces apoptosis in cancer cells [1].

NCD38 TFA serves as a selective inhibitor of LSD1 [1] [2].

LSD1-UM-109 is a highly potent and reversible inhibitor of LSD1, demonstrating an IC50 of 3.1 nM. This compound exhibits strong antiproliferative activity, inhibiting cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line [1].

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.

3-pyridine toxoflavin is a potent KDM4C inhibitor, IC50=19nM.

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

LSD1-IN-24 is a selective and potent LSD1 inhibitor with an IC50 value of 0.247 μM.LSD1-IN-24 induces PD-L1 expression and enhances the T cell killing response, and can be used in cancer-related diseases.