Histone Demethylases
Histone demethylases are a diverse group of enzymes catalyzing a process to reverse histone methylation, in which methyl (CH3-) groups are removed from instead of being transferred to histone. So far, two evolutionarily conserved histone demethylase families have been identified, including LSD demethylases and JMJC demethylases. LSD1 and LSD2 are two well-established members of LSD demethylase family, which catalyze demethylation through a flavin adenine dinucleotide (FAD)-dependent amine oxidation reaction. LSD1 has been found to demethylate H3K4mel, H3K4me2, H3K9me1, H3K9me2 and a few non-histone targets; while LSD2 has been found to demethylate only H3K4me1 and H3K4me2. Members of JMJC demethylase family is characterized by containing the catalytic JMJC domain, which demethylate substrates, including H3K4, H3K9, H3K27, H3K36 and H4K20, through a Fe(II)- and α-ketogutarate-dependent dioxygenase reaction.
Products for Histone Demethylases
- Cat.No. Product Name Information
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GC72837
α-Hydroxyglutaric acid-d4 disodium
2-Hydroxyglutarate-d4 disodium; 2-Hydroxyglutaric acid-d4 disodium; 2-Hydroxypentanedioic acid-d4 disodium
α-droxyglutaric acid-d4 (disodium) is the deuterium labeled α-droxyglutaric acid disodium. -
GC60004
(rel)-Tranylcypromine D5 hydrochloride
Tranylcypromine-d5 (SKF 385-d5) hydrochloride is a deuterium labeled (rel)-Tranylcypromine hydrochloride.
-
GC11873
2,4-Pyridinedicarboxylic Acid
2,4-Pyridinedicarboxylic Acid (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-Pyridinedicarboxylic Acid is a target chemical in the field of bio-based plastics.
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GC42075
2,4-Pyridinedicarboxylic Acid (hydrate)
2,4-Dicarboxylpyridine, 2,4-PDCA
2,4-Pyridinedicarboxylic Acid (2,4-PDCA) is a compound that structurally mimics 2-oxoglutarate (2-OG, also known as α-ketoglutarate) and chelates zinc, thus affecting a range of enzymes. -
GC12961
Apicidin
OSI 2040
A cell-permeable HDAC inhibitor
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GC17820
AS8351
NCI 51355, NSC 51355
histone demethylase inhibitor -
GC18159
BAY-598
A potent and selective SMYD2 inhibitor
-
GC16114
Bizine
LSD1 inhibitor
-
GC64865
Bomedemstat
IMG-7289
Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis. -
GC68795
Bomedemstat dihydrochloride
IMG-7289 dihydrochloride
Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1). Bomedemstat dihydrochloride can increase the methylation of H3K4 and H3K9, which then alters gene expression. Bomedemstat dihydrochloride has anti-cancer activity, inhibiting cancer cell proliferation and inducing apoptosis.
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GC67921
Bomedemstat ditosylate
IMG-7289 ditosylate
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GC65879
Bomedemstat hydrochloride
IMG-7289 hydrochloride
Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis. -
GC35621
CBB1003
CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
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GC35622
CBB1003 hydrochloride
CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
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GC14151
CBB1007
LSD1 inhibitor,potent and selective
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GC35623
CBB1007 hydrochloride
CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
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GC35624
CBB1007 trihydrochloride
CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
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GC34165
Corin
Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
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GC25304
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.
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GC10774
CPI-455
KDM5 inhibitor
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GC25305
CPI-455 HCl
CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
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GC15830
Daminozide
Alar, Aminozide, B 995, DIMG, DMASA, Kylar, SADH, Succinic Acid
Selective inhibitor of KDM2/7 histone demethylases -
GC33013
DDP-38003 dihydrochloride
DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
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GC34296
DDP-38003 trihydrochloride
DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
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GC60833
FB23
FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity.
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GC34314
GSK 690 Hydrochloride
GSK 690 (Hydrochloride) is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
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GC10617
GSK J1
A dual inhibitor of JMJD3 and UTX
-
GC13086
GSK J2
inactive control of GSK J1, JMJD3 (KDM6B) and UTX (KDM6A) inhibitor
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GC12997
GSK J4 free base
GSK J4 free base is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK J4 free base inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1. GSK J4 free base induces endoplasmic reticulum stress-related apoptosis.
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GC15497
GSK J4 HCl
GSK-J4 HCl is a small-molecule inhibitor with highly efficient cell permeability and a pharmacologically selective inhibitor that preserves H3K27 methylation by inhibiting KDM6B.
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GC17118
GSK J5
inactive isomer of GSK J4, KDM inhibitor
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GC39491
GSK-3484862
GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.
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GC36195
GSK-J1 lithium salt
GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
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GC12288
GSK-J1 sodium salt
A neuropeptide with diverse biological activities
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GC43792
GSK-J2 (sodium salt)
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.
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GC43794
GSK-J5 (hydrochloride)
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.
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GC15368
GSK-LSD1 2HCl
irreversible, and selective LSD1 inhibitor
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GC32764
GSK-LSD1 Dihydrochloride
An LSD1 inhibitor
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GC11578
GSK2879552
Novel and irreversible LSD1 inhibitor
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GC62719
GSK2879552 dihydrochloride
GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
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GC34604
GSK467
GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM and an IC50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.
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GC72852
Helenalin acetate
Helenalin acetate, a natural NF-κB inhibitor, is a potent C/EBPβ inhibitor.
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GC69273
INCB059872 dihydrochloride
INCB059872 dihydrochloride is an effective, orally active, selective and irreversible inhibitor of lysine-specific demethylase 1 (LSD1). It can be used for research on myeloid leukemia.
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GC17754
IOX 1
histone demethylase JMJD inhibitor
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GC73462
JHDM-IN-1
JHDM-IN-1 (Compound 1) is a Jumonji C domain-containing HDMs (JHDM) inhibitor with IC50s of 3.4, 4.3, 5.9, 10 and 43 μM against JMJD2C, JMJD2A, JMJD2E, PHF8 and JMJD3, respectively.
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GC15603
JIB-04
JHDM Inhibitor VII, NSC 693627
Jumonji histone demethylase inihibitor -
GC64841
JQKD82 trihydrochloride
JADA82 trihydrochloride; PCK82 trihydrochloride
JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma. -
GC36388
KDM2A/7A-IN-1
KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16?μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
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GC70823
KDM2B-IN-1
KDM2B-IN-1 is a histone demethylase (kdm2b) inhibitor and can be used for hyperproliferative diseases research.
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GC69327
KDM2B-IN-4
KDM2B-IN-4 is a histone demethylase KDM2B inhibitor. It can be used for cancer research. For more information, please refer to compound 182b in patent document WO2016112284A1.
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GC36389
KDM4-IN-2
KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7?nM for KDM4A and KDM5B, respectively.
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GC69328
KDM4C-IN-1
KDM4C-IN-1 (Compound 4d) is an effective inhibitor of KDM4C with an IC50 of 8 nM. It inhibits the growth of HepG2 and A549 cells with IC50 values of 0.8 μM and 1.1 μM, respectively.
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GC31887
KDM4D-IN-1
KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
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GC69329
KDM5-C49 hydrochloride
KDOAM-20 hydrochloride
KDM5-C49 (KDOAM-20) hydrochloride is an effective and selective inhibitor of KDM5 demethylases, with IC50 values of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C respectively. It can be used in cancer research.
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GC39394
KDM5-C70
KDOAM-21
KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels. -
GC32790
KDM5-IN-1
KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
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GC32842
KDM5A-IN-1
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).
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GC38709
KDOAM-25 citrate
KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
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GC73220
LSD1-IN-24
LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor with IC50 = 0.247 μM.
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GC73549
LSD1-IN-27
LSD1-IN-27 (Compound 5ac) is a LSD1 inhibitor (IC50: 13 nM).
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GC73859
LSD1-IN-30
LSD1-IN-30 (compound 3) is a potent inhibitor of lysine-specific demetlase 1 (LSD1), with the IC50 value of 0.291 μM.
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GC36484
LSD1-IN-5
LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
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GC36485
LSD1-IN-6
LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
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GC62434
LSD1/HDAC6-IN-1
LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM).
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GC13534
Lysine-specific Demethylase Inhibitor (1C)
KDM1 Inhibitor I|LSD1 Inhibitor
lysine-specific demethylase Inhibitor -
GC47586
Lysine-specific Demethylase Inhibitor (1C) (hydrochloride)
An LSD1 inhibitor
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GC65254
MC4355
MC4355 is a dual inhibitor of EZH2 and histone deacetylase (HDAC).
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GC44184
Methylstat (hydrate)
Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability.
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GC12557
ML324
CID-44143209
JMJD2 demethylase inhibitor, potent and cell-permeable -
GC12458
N-Oxalylglycine
NOG
cell permeable inhibitor of α-ketoglutarate-dependent enzymes, including JMJD2A, JMJD2C, and JMJD2E.
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GC65138
NCDM-32B
NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer.
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GC19410
NCGC00244536
NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM
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GC32896
NCGC00247743
NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
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GC50136
NSC 636819
KDM4A/KDM4B inhibitor
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GC17314
OG-L002
LSD1 inhibitor,potent and specific
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GC11792
OG-L002 HCl
LSD1 inhibitor,potent and specific
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GC36818
ORY-1001(trans)
ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride
Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor. -
GC73981
P3FI-63
P3FI-63 is a KDM3B inhibitor with a IC50 value of 7 μM.
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GC15301
PBIT
2-p-tolyl-1,2-Benzisothiazolin-3-one
JARID1 family demethylases inhibitor -
GC62678
PFI-90
PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. PFI-90 induces apoptosis and myogenic differentiation, resulting in the cell death increased. PFI-90 has the potential for the antitumor activity. (patent WO2021101929A1).
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GC44668
Posaconazole D-Glucuronide
Posaconazole N-β-D-Glucuronide
Posaconazole D-glucuronide is a metabolite of the antifungal agent posaconazole. -
GC90195
Posaconazole-d5
An internal standard for the quantification of posaconazole
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GC14066
Procaine
Sodium channel inhibitor
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GC44685
Procaine (hydrochloride)
Novocaine
Procaine (hydrochloride) is an analytical reference standard categorized as a local anesthetic that is used as an adulterant. -
GC49116
Prohexadione
BX-112
A plant growth regulator -
GC32699
QC6352
QC6352 is an orally available, selective and potent KDM4C inhibitor with an IC50 of 35 nM.
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GC10148
RN 1 dihydrochloride
LSD1 Inhibitor IV
LSD1 inhibitor, potent and selective -
GC33339
S 2101
S 2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
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GC64303
S2116
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
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GC64902
S2157
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
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GC32820
Seclidemstat (SP-2577)
SP-2577
Seclidemstat (SP-2577) is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat (SP-2577) promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat (SP-2577) can be used for the research of Ewing Sarcoma. -
GC63456
Seclidemstat mesylate
SP-2577 mesylate
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma. -
GC14631
SP2509
HCI-2509, LSD1 Inhibitor VII
Demethylase 1 (LSD1) antagonist, novel Lysine-specific -
GC33038
T-3775440 hydrochloride
T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
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GC65456
T-448
T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM.
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GC63437
TAK-418
TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM.
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GC10319
TC-E 5002
TC-E 5002 (TC-E 5002) is a selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). TC-E 5002 inhibits growth of HeLa and KYSE-150 cancer cells in vitro.
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GC45029
TFMB-R-2-HG
TFMB-R-2-HG is a cell-permeable form of (R)-2-hydroxyglutarate ((R)-2-HG).
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GC70033
TK-129
TK-129 is an orally effective, low-toxicity and potent KDM5B inhibitor (with high affinity; IC50=44 nM).
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GC11576
Tranylcypromine (2-PCPA) HCl
(1S,2R)-Tranylcypromine ((1S,2R)-SKF 385) hydrochloride is a potent antidepressant agent.