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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
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 (H3...
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 ...
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.
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...
T4214 KDM4D-IN-1 KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).
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...
T3576 KDM5-inhibitor 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...
T1868 JIB04 JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
T3552 CPI455 CPI-455 is a specific KDM5 inhibitor.
TQ0050 NCGC00244536 NCGC00244536 is a potent KDM4B inhibitor (IC50: 10 nM).
T3719 Daminozide Daminozide is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
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...
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...
T2304 SP2509 SP2509 is a specific histone demethylase LSD1 inhibitor(IC50 =13 nM).
T3677 GSK2879552 GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential ant...
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...
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, >...
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.
T5825 ORY-1001(trans) ORY-1001, a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.
T7942 Tranylcypromine (hemisulfate) Tranylcypromine is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1)  with a rapid onset of activity.
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, KDM6...
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).
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 de...
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 ...
T16700 QC6352 QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).
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.
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.
T13748 L-2-Hydroxyglutaric acid disodium L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine...
T5484 GSK467 GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
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...
T15649 KDM5-IN-1 KDM5-IN-1 is an effective, selective, and orally bioavailable inhibitor of KDM5 (IC50: 15.1 nM).
T11503 GSK 690 Hydrochloride GSK 690 is a reversible inhibitor of lysine-specific demethylase 1 (LSD1) (Kd: 9 nM; biochemical IC50: 37 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).
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).
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).
T12701 (rel)-Tranylcypromine D5 hydrochloride (rel)-Tranylcypromine D5 hydrochloride is a deuterium labeled (rel)-Tranylcypromine hydrochloride. (rel)-Tranylcypromine hydrochloride is an irreversible, nonsel...
T13055 T-3775440 hydrochloride T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).
T6593 ML324 ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).
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 (H3...
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 ...
Seclidemstat
T4527CAS 1423715-37-0
Seclidemstat is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.
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.
AS8351
T4100CAS 796-42-9
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...
KDM4D-IN-1
T4214CAS 2098902-68-0
KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).
GSK-J4 Hydrochloride
T4383CAS 1797983-09-5
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...
KDM5-inhibitor
T3576CAS T3576
KDM5 inhibitor
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, respec...
JIB04
T1868CAS 199596-05-9
JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
CPI455
T3552CAS 1628208-23-0
CPI-455 is a specific KDM5 inhibitor.
NCGC00244536
TQ0050CAS 2003260-55-5
NCGC00244536 is a potent KDM4B inhibitor (IC50: 10 nM).
Daminozide
T3719CAS 1596-84-5
Daminozide is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
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 utili...
ORY1001
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 aminox...
SP2509
T2304CAS 1423715-09-6
SP2509 is a specific histone demethylase LSD1 inhibitor(IC50 =13 nM).
GSK2879552
T3677CAS 1401966-69-5
GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential ant...
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 of...
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, >...
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.
ORY-1001(trans)
T5825CAS 1431303-72-8
ORY-1001, a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.
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.
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, KDM6...
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).
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 de...
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 ...
QC6352
T16700CAS 1851373-36-8
QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).
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 .
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.
Kgp-IN-1
T11756CAS 2097865-36-4
Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor.
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.
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.
L-2-Hydroxyglutaric acid disodium
T13748CAS 63512-50-5
L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine...
GSK467
T5484CAS 1628332-52-4
GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
KDM5A-IN-1
T15650CAS 1905481-36-8
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...
KDM5-IN-1
T15649CAS 1628210-26-3
KDM5-IN-1 is an effective, selective, and orally bioavailable inhibitor of KDM5 (IC50: 15.1 nM).
GSK 690 Hydrochloride
T11503CAS T11503
GSK 690 is a reversible inhibitor of lysine-specific demethylase 1 (LSD1) (Kd: 9 nM; biochemical IC50: 37 nM).
GSK-J1 lithium salt
T11475CAS T11475
GSK-J1 lithium salt is a potent inhibitor of me2-demethylases JMJD3/H3K27me3/KDM6B and UTX/KDM6A (IC50: 60 nM towards KDM6B).
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).
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).
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).
(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, nonsel...
T-3775440 hydrochloride
T13055CAS 1422535-52-1
T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).
ML324
T6593CAS 1222800-79-4
ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).