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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
T0802 Procaine hydrochloride Procaine Hydrochloride is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds ...
T38318L Acetyl Pentapeptide-1 acetate Acetyl Pentapeptide-1 acetate is an histone deacetylase inhibitor.
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 of t...
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.
T1868 JIB-04 JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
T6593 ML324 ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).
T7942 Tranylcypromine hemisulfate Tranylcypromine is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.
T16435 PBIT 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 specif...
T15648 KDM5-C70 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 antiprol...
T0029 Procaine Procaine is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral ...
T9243 PFI-90 PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action.PFI-90 has the potential for the antitumor activity. PFI-90 induce...
T7057 Methylstat Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of...
T2304 SP2509 SP2509 is a specific histone demethylase LSD1 inhibitor(IC50 =13 nM).
T5484 GSK467 GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
T35338 CP2 CP2是一种环肽,能够抑制JmjC histone demethylases KDM4,对KDM4A和KDM4C的IC50分别为42 nM和29 nM。
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 (H3K...
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 utili...
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 ...
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).
T13052 S2101 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).
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).
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).
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, nonsel...
T11882 Pulrodemstat benzenesulfonate LSD1-IN-7 benzenesulfonate is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity.
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 dem...
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 de...
T11758 KI696 isomer KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 isomer is the less active isomer of KI696 .
T11757 KHK-IN-2 KHK-IN-2 is a selective and potent ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM.
T11756 Kgp-IN-1 Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor.
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.
T11475 GSK-J1 lithium salt GSK-J1 lithium salt is a potent inhibitor of me2-demethylases JMJD3/H3K27me3/KDM6B and UTX/KDM6A (IC50: 60 nM towards KDM6B).
T11503 GSK 690 Hydrochloride GSK 690 is a reversible inhibitor of lysine-specific demethylase 1 (LSD1) (Kd: 9 nM; biochemical IC50: 37 nM).
TQ0050 NCGC00244536 NCGC00244536 is a potent KDM4B inhibitor (IC50: 10 nM).
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 ORY1001 ORY-1001 (RG-6016) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor, with high selectivity against related FAD dependent aminox...
T4214 KDM4D-IN-1 KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).
T4100 AS8351 AS-8351 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 i...
T4527 Seclidemstat Seclidemstat is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.
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 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...
T3677 GSK2879552 GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential ant...
T3719 Daminozide Daminozide is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
T3576 KDM5-inhibitor KDM5 inhibitor
T3552 CPI-455 CPI-455 is a specific KDM5 inhibitor.
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, respec...
T5825 Iadademstat dihydrochloride ORY-1001, a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.
T16700 QC6352 QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).
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, KDM6A,...
T15650 KDM5A-IN-1 KDM5A-IN-1 is a potent and orally bioavailable inhibitor of pan-histone lysine demethylases 5 (IC50s: 45 nM, 56 nM, and 55 nM for KDM5A, KDM5B, and KDM5C) and (E...
Procaine hydrochloride
T0802
Procaine Hydrochloride is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds ...
Acetyl Pentapeptide-1 acetate
T38318L
Acetyl Pentapeptide-1 acetate is an histone deacetylase inhibitor.
GSK-J4
T3100
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 of...
OG-L002
T6073
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.
JIB-04
T1868
JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
ML324
T6593
ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).
Tranylcypromine hemisulfate
T7942
Tranylcypromine is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.
PBIT
T16435
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 spe...
KDM5-C70
T15648
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 antiprol...
Procaine
T0029
Procaine is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral ...
PFI-90
T9243
PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action.PFI-90 has the potential for the antitumor activity. PFI-90 induce...
Methylstat
T7057
Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of...
SP2509
T2304
SP2509 is a specific histone demethylase LSD1 inhibitor(IC50 =13 nM).
GSK467
T5484
GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
CP2
T35338
CP2是一种环肽,能够抑制JmjC histone demethylases KDM4,对KDM4A和KDM4C的IC50分别为42 nM和29 nM。
CPI-455 HCl
T22299
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 (H3...
GSK-LSD1 dihydrochloride
T2315
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 utili...
Tranylcypromine (2-PCPA) hydrochloride
T1025
Tranylcypromine Hydrochloride, a monoamine oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It ...
Corin
T10864
Corin is a dual inhibitor of histone lysine-specific demethylase (LSD1) and HDAC (Ki(inact): 110 nM for LSD1; IC50: 147 nM for HDAC1).
S2101
T13052
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
T13057
T-448 is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).
T-448 free base
T13056
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-3775440 hydrochloride
T13055
T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).
(rel)-Tranylcypromine D5 hydrochloride
T12701
(rel)-Tranylcypromine D5 hydrochloride is a deuterium labeled (rel)-Tranylcypromine hydrochloride. (rel)-Tranylcypromine hydrochloride is an irreversible, nonsel...
Pulrodemstat benzenesulfonate
T11882
LSD1-IN-7 benzenesulfonate is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity.
LSD1-IN-6
T11881
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 dem...
LSD1-IN-5
T11880
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 de...
KI696 isomer
T11758
KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 isomer is the less active isomer of KI696 .
KHK-IN-2
T11757
KHK-IN-2 is a selective and potent ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM.
Kgp-IN-1
T11756
Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor.
KF 13218
T11755
KF 13218 is a selective, potent and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
GSK-J1 lithium salt
T11475
GSK-J1 lithium salt is a potent inhibitor of me2-demethylases JMJD3/H3K27me3/KDM6B and UTX/KDM6A (IC50: 60 nM towards KDM6B).
GSK 690 Hydrochloride
T11503
GSK 690 is a reversible inhibitor of lysine-specific demethylase 1 (LSD1) (Kd: 9 nM; biochemical IC50: 37 nM).
NCGC00244536
TQ0050
NCGC00244536 is a potent KDM4B inhibitor (IC50: 10 nM).
GSK-J1
T6847
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, >...
ORY1001
T6922
ORY-1001 (RG-6016) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor, with high selectivity against related FAD dependent aminox...
KDM4D-IN-1
T4214
KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).
AS8351
T4100
AS-8351 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 i...
Seclidemstat
T4527
Seclidemstat is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.
GSK2879552 2HCl (1401966-69-5(free base))
T4418
GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
GSK-J4 Hydrochloride
T4383
GSK-J4 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...
GSK2879552
T3677
GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential ant...
Daminozide
T3719
Daminozide is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
KDM5-inhibitor
T3576
KDM5 inhibitor
CPI-455
T3552
CPI-455 is a specific KDM5 inhibitor.
IOX1
T6545
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, respec...
Iadademstat dihydrochloride
T5825
ORY-1001, a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.
QC6352
T16700
QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).
YUKA1
T17278
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, KDM6...
KDM5A-IN-1
T15650
KDM5A-IN-1 is a potent and orally bioavailable inhibitor of pan-histone lysine demethylases 5 (IC50s: 45 nM, 56 nM, and 55 nM for KDM5A, KDM5B, and KDM5C) and (E...
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