Histone Demethylases(组蛋白去甲基化酶)
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.
- Cat.No. 产品名称 Information
-
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!
-
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.
-
GC67921
Bomedemstat ditosylate
-
GC65879
Bomedemstat hydrochloride
-
GC65456
T-448
-
GC65254
MC4355
-
GC65138
NCDM-32B
-
GC64902
S2157
-
GC64865
Bomedemstat
-
GC64841
JQKD82 trihydrochloride
-
GC64303
S2116
-
GC63456
Seclidemstat mesylate
-
GC63437
TAK-418
-
GC49116
Prohexadione
A plant growth regulator
-
GC62719
GSK2879552 dihydrochloride
An LSD1 inhibitor
-
GC62678
PFI-90
PFI-90 is a selective inhibitor of the histone demethylase KDM3B. PFI-90 induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo.
-
GC62434
LSD1/HDAC6-IN-1
-
GC47586
Lysine-specific Demethylase Inhibitor (1C) (hydrochloride)
An LSD1 inhibitor
-
GC60004
(rel)-Tranylcypromine D5 hydrochloride
-
GC50136
NSC 636819
NSC 636819 是 KDM4A/KDM4B 的竞争性和选择性抑制剂。 KDM4A/KDM4B 是前列腺癌的潜在进展因素。 NSC 636819 具有研究癌症疾病,尤其是前列腺癌的潜力。
-
GC38709
KDOAM-25 citrate
-
GC37956
YUKA1
-
GC36818
ORY-1001(trans)
-
GC36485
LSD1-IN-6
-
GC36484
LSD1-IN-5
-
GC36389
KDM4-IN-2
-
GC36388
KDM2A/7A-IN-1
-
GC36195
GSK-J1 lithium salt
GSK-J1 is a highly potent inhibitor of H3K27 histone demethylase JMJD3 (KDM6B) and UTX (KDM6A) with IC50 of 60 nM in cell-free assays for JMJD3 (KDM6B) , respectively, >10-fold selectivity over other tested demethylases, with IC50 of 0.95μM and 1.76μM towards JARID1B/C.
-
GC35624
CBB1007 trihydrochloride
-
GC35623
CBB1007 hydrochloride
-
GC35622
CBB1003 hydrochloride
-
GC35621
CBB1003
-
GC44184
Methylstat (hydrate)
A cell-permeable demethylase inhibitor
-
GC43794
GSK-J5 (hydrochloride)
A negative control compound for GSK-J4
-
GC43792
GSK-J2 (sodium salt)
A negative control compound for GSK-J1
-
GC42075
2,4-Pyridinedicarboxylic Acid (hydrate)
An inhibitor of 2-oxoglutarate-dependent enzymes
-
GC34604
GSK467
GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members.
-
GC34314
GSK 690 Hydrochloride
-
GC34296
DDP-38003 trihydrochloride
-
GC34165
Corin
-
GC33339
S 2101
-
GC33038
T-3775440 hydrochloride
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.
-
GC33013
DDP-38003 dihydrochloride
-
GC32896
NCGC00247743
-
GC32842
KDM5A-IN-1
-
GC32820
Seclidemstat (SP-2577)
Seclidemstat (SP-2577) is a potent and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A) with IC50 of 13 nM. Seclidemstat (SP-2577) has potential antineoplastic activity.
-
GC32790
KDM5-IN-1
-
GC32764
GSK-LSD1 Dihydrochloride
An LSD1 inhibitor
-
GC32699
QC6352
-
GC31887
KDM4D-IN-1
KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.