Histone Demethylase Inhibitor

QC6352 (Standard) is the analytical standard of QC6352 (HY-104048). This product is intended for research and analytical applications. QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC₅₀s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC₅₀ of 750 nM (KDM5B).

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

CBB3001 is an inhibitor of LSD1/KDM1A. CBB3001 exerts its effect by inhibiting Histone Demethylase activity, with an IC₅₀ of 21.25 μM. It downregulates the expression of pluripotency-related proteins and genes such as SOX2 and OCT4, and induces cell differentiation, growth arrest, and apoptosis. CBB3001 can be used for research on testicular germ cell tumors, teratomas, and embryonal carcinomas.

RN-1 dihydrochloride (Standard) is the analytical standard of RN-1 (dihydrochloride) (HY-110130). This product is intended for research and analytical applications. RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC₅₀ values of 0.51 μM and 2.785 μM respectively.

TCP-MP-CA (compound 11a) is an inhibitor of LSD1 demethylation enzymatic via binding to LSD1/CoREST complex. TCP-MP-CA exhibits an inhibitory effect on osteoclastogenesis, with an IC₅₀ value of 0.14 µM.

LSD1-IN-44 (Compound 19) is a LSD1 inhibitor with an IC₅₀ of 0.02  μM for LSD1-CoREST enzymatic complex. LSD1-IN-44 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. LSD1-IN-44 has no significant toxicity to human cells. LSD1-IN-44 can be used for schistosomiasis research.

MC3935 is a LSD1 inhibitor with an IC₅₀ of 0.52  μM for LSD1-CoREST enzymatic complex. MC3935 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. MC3935 has no significant toxicity to human cells. MC3935 can be used for schistosomiasis research.

OG-L002 hydrochloride is a potent and highly selective LSD1 inhibitor with an IC₅₀ of 0.02 μM. OG-L002 hydrochloride is a potent monoamine oxidases (MAO) inhibitor with IC₅₀s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 hydrochloride potently inhibits the expression of HSV IE genes.

T-3775440 hydrochloride (Standard) is the analytical standard of T-3775440 hydrochloride (HY-103085). This product is intended for research and analytical applications. T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC₅₀ value of 2.1 nM.

KDM5-IN-1 (Standard) is the analytical standard of KDM5-IN-1 (HY-100422). This product is intended for research and analytical applications. KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.

GSK-LSD1 (dihydrochloride) (Standard) is the analytical standard of GSK-LSD1 (dihydrochloride) (HY-100546A). This product is intended for research and analytical applications. GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.

HDM-IN-1 (Compound A4) is an inhibitor for fungal histone demethylase (HDM), that inhibits the H3K27me3 in Cryptococcus neoformans and in Candida auris with IC₅₀s of 134 and 12 nM. HDM-IN-1 exhibits inhibitory efficacy against C. neoformans and C. auris with MIC₈₀ of 0.5-2 μg/mL, through inhibition of the biofilm and capsule formation. HDM-IN-1 exhibits antifungal activity in ICR mouse model.

KDM5A-IN-1 (Standard) is the analytical standard of KDM5A-IN-1 (HY-100014). This product is intended for research and analytical applications. KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).

N-Oxalylglycine (Standard) is the analytical standard of N-Oxalylglycine. This product is intended for research and analytical applications. N-Oxalylglycine (N-Oxaloglycine) is a Jumonji C-domain-containing histone lysine demethylase inhibitor. N-Oxalylglycine inhibits JMJD2A, JMJD2C and JMJD2D. N-Oxalylglycine also inhibits HIF prolylhydroxylase domain-1 (PHD-1) and PHD-2, with an IC50 of 2.1 μM and 5.6 μM, respectively.