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Chromatin/Epigenetic Histone Demethylase

Histone Demethylase

Histone demethylase proteins have a variety of domains that serve different functions. These functions include binding to the histone (or sometimes the DNA on the nucleosome), recognizing the correct methylated amino acid substrate and catalyzing the reaction, and binding cofactors. Cofactors include: alpha-keto glutarate (JmjC-domain containing demethylases), CoREST (LSD), FAD, Fe (II) or NOG (N-oxalylglycine).
Cat No. product name
T1868 JIB-04 JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
T2304 SP2509 SP2509 is a specific histone demethylase LSD1 inhibitor(IC50 =13 nM).
T2315 GSK-LSD1 dihydrochloride GSK-LSD1 2HCl is a specificity irreversible LSD1 inhibitor (IC50: 16 nM). The selectivity of GSK-LSD1 for LSD1 is >1000 fold over other closely related FAD util...
T3100 GSK J4 GSK-J4 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 ...
T3552 CPI-455 CPI-455 is a specific KDM5 inhibitor.
T3576 KDM5-inhibitor KDM5 inhibitor
T3719 Daminozide Daminozide is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
T4214 KDM4D-IN-1 KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).
T6073 OG-L002 OG-L002 is an effective and selective LSD1 inhibitor (IC50: 20 nM), showing 69- and 36-fold selectivity over MAO-A and MAO-B, respectively.
T6545 IOX1 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, res...
T6593 ML324 ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).
T6847 GSK J1 GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, ...
T6922 ORY-1001 ORY-1001 (RG-6016) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor,with high selectivity against related FAD dependent amin...
T4418 GSK2879552 2HCl (1401966-69-5(free base)) GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
T4383 GSK-J4 Hydrochloride GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a ...
T4527 Seclidemstat Seclidemstat is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.
T5825 ORY-1001(trans) ORY-1001, a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.
TQ0050 NCGC00244536 NCGC00244536 is a potent KDM4B inhibitor (IC50: 10 nM).
T1025 Tranylcypromine (2-PCPA) hydrochloride Tranylcypromine Hydrochloride, a monoamine oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It...
T7942 Tranylcypromine (hemisulfate) Tranylcypromine is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1)  with a rapid onset of activity.
T5484 GSK467 GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM). 
T13055 T-3775440 hydrochloride T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).
T12701 (rel)-Tranylcypromine D5 hydrochloride (rel)-Tranylcypromine D5 hydrochloride is a deuterium labeled (rel)-Tranylcypromine hydrochloride. (rel)-Tranylcypromine hydrochloride is an irreversible, nonse...
T13052 S 2101 S 2101 is an inhibitor of lysine-specific demethylase 1 (LSD1)(IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s).
T13056 T-448 free base T-448 free base is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).
T13057 T-448 T-448 is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).
T11475 GSK-J1 lithium salt GSK-J1 lithium salt is a potent inhibitor of me2-demethylases JMJD3/H3K27me3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. 
T11503 GSK 690 Hydrochloride GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
T15649 KDM5-IN-1 KDM5-IN-1 is an effective, selective, and orally bioavailable inhibitor of KDM5 (IC50: 15.1 nM).
T15650 KDM5A-IN-1 KDM5A-IN-1 is obviously less effective against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B). KDM5A-IN-1 is a potent and orally bioavailable inhibitor of pan-his...
T10864 Corin Corin is a dual inhibitor of histone lysine-specific demethylase (LSD1) and HDAC (Ki(inact): 110 nM for LSD1; IC50: 147 nM for HDAC1).
T13745 KF21213 KF21213 shows a high affinity for the adenosine A2A receptors (Ki=3.0 nM). KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors.
T11755 KF 13218 KF 13218 is a selective, potent and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
T11756 Kgp-IN-1 Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor.
T11757 KHK-IN-2 KHK-IN-2 is a selective and potent ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM.
T11758 KI696 isomer KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 isomer is the less active isomer of KI696 .
T16700 QC6352 QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).
T11880 LSD1-IN-5 LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-5  is a potent and reversible inhibitor of lysine-specific...
T11881 LSD1-IN-6 LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-6 is a potent and reversible inhibitor of lysine-specific d...
T17278 YUKA1 YUKA1 is a potent and cell-permeable Lysine demethylase 5A inhibitor (IC50: 2.66 μM) and less active on KDM5C (IC50, 7.12 μM). YUKA1 is inactive on KDM5B, KDM...
T22299 CPI-455 HCl CPI-455 is a specific KDM5 inhibitor with IC50 value of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H...
JIB-04
T1868CAS 199596-05-9
JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
SP2509
T2304CAS 1423715-09-6
SP2509 is a specific histone demethylase LSD1 inhibitor(IC50 =13 nM).
GSK-LSD1 dihydrochloride
T2315CAS 1431368-48-7
GSK-LSD1 2HCl is a specificity irreversible LSD1 inhibitor (IC50: 16 nM). The selectivity of GSK-LSD1 for LSD1 is >1000 fold over other closely related FAD util...
GSK J4
T3100CAS 1373423-53-0
GSK-J4 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 ...
CPI-455
T3552CAS 1628208-23-0
CPI-455 is a specific KDM5 inhibitor.
KDM5-inhibitor
T3576CAS T3576
KDM5 inhibitor
Daminozide
T3719CAS 1596-84-5
Daminozide is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
KDM4D-IN-1
T4214CAS 2098902-68-0
KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).
OG-L002
T6073CAS 1357302-64-7
OG-L002 is an effective and selective LSD1 inhibitor (IC50: 20 nM), showing 69- and 36-fold selectivity over MAO-A and MAO-B, respectively.
IOX1
T6545CAS 5852-78-8
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, res...
ML324
T6593CAS 1222800-79-4
ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).
GSK J1
T6847CAS 1373422-53-7
GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, ...
ORY-1001
T6922CAS 1431326-61-2
ORY-1001 (RG-6016) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor,with high selectivity against related FAD dependent amin...
GSK2879552 2HCl (1401966-69-5(free base))
T4418CAS T4418
GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
GSK-J4 Hydrochloride
T4383CAS 1797983-09-5
GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a ...
Seclidemstat
T4527CAS 1423715-37-0
Seclidemstat is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.
ORY-1001(trans)
T5825CAS 1431303-72-8
ORY-1001, a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.
NCGC00244536
TQ0050CAS 2003260-55-5
NCGC00244536 is a potent KDM4B inhibitor (IC50: 10 nM).
Tranylcypromine (2-PCPA) hydrochloride
T1025CAS 1986-47-6
Tranylcypromine Hydrochloride, a monoamine oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It...
Tranylcypromine (hemisulfate)
T7942CAS 13492-01-8
Tranylcypromine is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1)  with a rapid onset of activity.
GSK467
T5484CAS 1628332-52-4
GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM). 
T-3775440 hydrochloride
T13055CAS 1422535-52-1
T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).
(rel)-Tranylcypromine D5 hydrochloride
T12701CAS 107077-98-5
(rel)-Tranylcypromine D5 hydrochloride is a deuterium labeled (rel)-Tranylcypromine hydrochloride. (rel)-Tranylcypromine hydrochloride is an irreversible, nonse...
S 2101
T13052CAS 1239262-36-2
S 2101 is an inhibitor of lysine-specific demethylase 1 (LSD1)(IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s).
T-448 free base
T13056CAS 1597426-52-2
T-448 free base is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).
T-448
T13057CAS 1597426-53-3
T-448 is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).
GSK-J1 lithium salt
T11475CAS
GSK-J1 lithium salt is a potent inhibitor of me2-demethylases JMJD3/H3K27me3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. 
GSK 690 Hydrochloride
T11503CAS
GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
KDM5-IN-1
T15649CAS 1628210-26-3
KDM5-IN-1 is an effective, selective, and orally bioavailable inhibitor of KDM5 (IC50: 15.1 nM).
KDM5A-IN-1
T15650CAS 1905481-36-8
KDM5A-IN-1 is obviously less effective against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B). KDM5A-IN-1 is a potent and orally bioavailable inhibitor of pan-his...
Corin
T10864CAS 1808113-09-8
Corin is a dual inhibitor of histone lysine-specific demethylase (LSD1) and HDAC (Ki(inact): 110 nM for LSD1; IC50: 147 nM for HDAC1).
KF21213
T13745CAS 155271-17-3
KF21213 shows a high affinity for the adenosine A2A receptors (Ki=3.0 nM). KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors.
KF 13218
T11755CAS 127654-03-9
KF 13218 is a selective, potent and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
Kgp-IN-1
T11756CAS 2097865-36-4
Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor.
KHK-IN-2
T11757CAS 2135304-43-5
KHK-IN-2 is a selective and potent ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM.
KI696 isomer
T11758CAS 1799974-69-8
KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 isomer is the less active isomer of KI696 .
QC6352
T16700CAS 1851373-36-8
QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).
LSD1-IN-5
T11880CAS 2035912-55-9
LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-5  is a potent and reversible inhibitor of lysine-specific...
LSD1-IN-6
T11881CAS 2035912-43-5
LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-6 is a potent and reversible inhibitor of lysine-specific d...
YUKA1
T17278CAS 708991-09-7
YUKA1 is a potent and cell-permeable Lysine demethylase 5A inhibitor (IC50: 2.66 μM) and less active on KDM5C (IC50, 7.12 μM). YUKA1 is inactive on KDM5B, KDM...
CPI-455 HCl
T22299CAS 2095432-28-1
CPI-455 is a specific KDM5 inhibitor with IC50 value of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H...