Home Epigenetics Histone Demethylase

Histone Demethylase Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S6389 CPI-455

CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. This compound shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes.
Mol Cell, 2025, 85(15):2973-2987.e6
EMBO J, 2024, 44(2):437-456.
NPJ Precis Oncol, 2024, 8(1):59
S8601 CP2 CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively.
Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694
Oxid Med Cell Longev, 2022, 2022:2405943
Front Cell Dev Biol, 2021, 9:697614
S9882 PFI-90 PFI-90 is a selective inhibitor of the histone demethylase KDM3B. This compound induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo.
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Commun Biol, 2024, 7(1):1589
E4794 GSK-J4 GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A that ameliorates experimental autoimmune encephalomyelitis (EAE). It is also an inhibitor of TNF-α production, with an IC50 of 9 μM. It shows potential as a treatment for inflammatory and autoimmune disorders.
Cancer Res, 2025, 85(22):4485-4503
FASEB J, 2025, 39(1):e70306
S0201 Z-JIB-04 (NSC 693627) Z-JIB-04 (NSC 693627, JIB-04 Z-isomer) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
Mol Cell, 2025, 85(15):2973-2987.e6
Cell Death Discov, 2025, 11(1):326
S1325 L-2-Hydroxyglutaric acid disodium

L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. This compound is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively.
Cell Metab, 2024, S1550-4131(24)00415-7
Cell Rep Med, 2023, 4(5):101026
S1059 KDM4D-IN-1 KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.
Cell Rep Med, 2024, 5(2):101416
E7827 KDM5-IN-1 KDM5-IN-1 is a potent, selective and orally bioavailable inhibitor of KDM5 with an IC50 value of 15.1 nM. It displays an increased cell potency with an EC50 value of 0.34 μM, respectively.
E0132 NCGC00244536

NCGC00244536 is a novel KDM4 Inhibitor with an IC50 of ∼10 nM.
S0269 GSK467 GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. This compound shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members.
E1819 Zavondemstat Zavondemstat(QC8222, TACH 101) is a small-molecule pan-inhibitor of histone lysine demethylase 4D (KDM4D) that selectively targets KDM4A-D with no effect on other KDM families. It exhibits potent antiproliferative activity in various cancer cell lines and organoid models. It displays antineoplastic activity and acts as a potential anticancer agent.
E1793 TC-E5002(KDM2/7-IN-1) TC-E5002(KDM2/7-IN-1) is a selective inhibitor of histone demethylase KDM2/7 subfamily with IC50s of 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively. It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX with IC50s of >120, 83, 55, and 100 µM, respectively. It exhibits antiproliferative activity, indicating its potential as an anticancer agent.
S5772 AS-8351 AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.
E1733 PBIT PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. It inhibits JARID1B (KDM5B/PLU1), JARID1Aand JARID1C with an IC50 of 3 μM, 6 μM and 4.9 μM respectively. It is capable of inhibiting the multiplication of breast cancer cell lines expressing high levels of JARIDB1.
S4800New Daminozide Daminozide (Aminozide, DMASA, DIMG, B 995, Alar, Kylar, B-NINE, SADH) is a plant growth regulator that selectively inhibits human KDM2/7 histone demethylases, with IC50 of 0.55 μM for PHF8 (KDM7B), 1.5 μM for KDM2A, and 2.1 μM for KIAA1718 (KDM7A). It shows over 100-fold selectivity for the KDM2/7 subfamily compared to other histone demethylase subfamilies, with significantly weaker activity against enzymes such as KDM3A with IC50 of 127 μM.
E6667New JNJ-9350 JNJ-9350 is a chemical probe that inhibits spermine oxidase (SMOX) with an IC50 of 0.01 μM. This compound also shows inhibitory activity against polyamine oxidase (PAO), exhibiting an IC50 of 0.79 μM. JNJ-9350 has potential applications in cancer research.
S7796 GSK2879552 Dihydrochloride GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2
EMBO Rep, 2025, 10.1038/s44319-025-00385-w
Blood Adv, 2025, bloodadvances.2024015427
Verified customer review of GSK2879552 Dihydrochloride
S0356 Pulrodemstat (CC-90011) besylate Pulrodemstat (CC-90011) besylate (LSD1-IN-7 benzenesulfonate) is a potent and orally active lysine specific demethylase-1 (LSD1) inhibitor that is found to be effective in various tumors.
Nat Commun, 2024, 15(1):7366
S8438 T-3775440 HCl T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L.
Cell Death Discov, 2024, 10(1):166