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.

Products for Histone Demethylases

Cat.No. 产品名称 Information
GC35621 CBB1003 CBB1003是组蛋白去甲基化酶LSD1抑制剂,IC50值为10.54uM。
GC44685 Procaine (hydrochloride)
Novocaine
Procaine (hydrochloride) is an analytical reference standard categorized as a local anesthetic that is used as an adulterant.
GC44668 Posaconazole D-Glucuronide
Posaconazole N-β-D-Glucuronide
A metabolite of posaconazole
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)
2,4-吡啶二羧酸
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 GSK690(Hydrochloride)是赖氨酸特异性去甲基化酶1(LSD1)的可逆抑制剂，Kd值为9nM，IC50值为37nM。
GC34296 DDP-38003 trihydrochloride DDP-38003trihydrochloride是新颖，有口服活性的KDM1A/LSD1抑制剂，IC50值为84nM。
GC34165 Corin Corin是组氨酸赖氨酸特异性去甲基化酶(LSD1)和组氨酸脱乙酰化酶(HDAC)的双重抑制剂，其对LSD1的Ki(inact)值为110nM，对HDAC1的IC50值为147nM。
GC33339 S 2101 S2101是一个赖氨酸特异性去甲基化酶1(LSD1)抑制剂，其IC50值为0.99μM，Ki值为0.61μM，Kinact/Ki值为4560M/s。
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 DDP-38003dihydrochloride是新颖有口服活性的KDM1A/LSD1抑制剂，IC50值为84nM。
GC32896 NCGC00247743 NCGC00247743是一种组蛋白赖氨酸脱甲基酶KDM4抑制剂。
GC32842 KDM5A-IN-1 KDM5A-IN-1是组蛋白去甲基化酶抑制剂。
GC32820 Seclidemstat (SP-2577)
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 KDM5-IN-1是高效选择，有口服活性的KDM5抑制剂，IC50值为15.1nM。
GC32764 GSK-LSD1 Dihydrochloride An LSD1 inhibitor
GC32699 QC6352
QC6352是一种有效的KDM4C抑制剂，其IC50值为35nM。
GC31887 KDM4D-IN-1 KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.
GC30766 Tranylcypromine hemisulfate (dl-Tranylcypromine hemisulfate)
反苯环丙胺半硫酸盐; SKF 385 hemisulfate
Tranylcypromine (Parnate) is an irreversible inhibitor of monoamine oxidase (MAO) with a rapid onset of activity.
GC19410 NCGC00244536
3-(8-羟基喹啉-6-基)-N-(3-苯基丙基)苯甲酰胺,KDM4B Inhibitor B3
A KDM4B/JMJD2B inhibitor
GC18623 α-Hydroxyglutaric Acid
2-Hydroxyglutarate; 2-Hydroxyglutaric acid; 2-Hydroxypentanedioic acid
An α-hydroxy acid
GC18159 BAY-598 An inhibitor of SMYD2
GC11792 OG-L002 HCl An LSD1 inhibitor
GC16114 Bizine An LSD1 inhibitor
GC18012 GSK-LSD1 (hydrochloride) An LSD1 inhibitor
GC16743 RN-1 (hydrochloride)
LSD1 Inhibitor IV
An irreversible LSD1 inhibitor
GC12458 N-Oxalylglycine
N-草酰甘氨酸,NOG
An inhibitor of JMJD2 histone demethylases
GC13534 Lysine-specific Demethylase Inhibitor (1C)
KDM1 Inhibitor I|LSD1 Inhibitor
lysine-specific demethylase Inhibitor
GC15301 PBIT
2-p-tolyl-1,2-Benzisothiazolin-3-one
An inhibitor of JARID1 family demethylases
GC10774 CPI-455
6-异丙基-7-氧代-5-苯基-4,7-二氢吡唑并[1,5-A]嘧啶-3-腈
A KDM5 inhibitor
GC17820 AS8351
NSC51355
A histone demethylase inhibitor
GC12288 GSK-J1 sodium salt A dual inhibitor of JMJD3 and UTX
GC11873 2,4-Pyridinedicarboxylic Acid
2,4-吡啶二羧酸
An inhibitor of 2-oxoglutarate-dependent enzymes
GC11578 GSK2879552 An LSD1 inhibitor
GC12997 GSK J4 free base
N-[2-(2-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-BETA-丙氨酸乙酯
GSK J4 free base 是 H3K27me3/me2-去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 的有效双重抑制剂，IC50 分别为 8.6 和 6.6 μM。 GSK J4 游离碱抑制 LPS 诱导的 TNF-α；在人原代巨噬细胞中产生，IC50 为 9 μM. GSK J4 是 GSK-J1 的细胞渗透性前药。 GSK J4 free base 诱导内质网应激相关的细胞凋亡。
GC15368 GSK-LSD1 2HCl 不可逆的、选择性的 LSD1 抑制剂
GC10319 TC-E 5002
N-(9-环丙基-1-氧代壬基)-N-羟基-Β-丙氨酸
A KDM2/7 inhibitor
GC14631 SP2509
HCI-2509, LSD1 Inhibitor VII
A reversible inhibitor of LSD1
GC12557 ML324
CID-44143209
A cell-permeable inhibitor of JMJD2 demethylases
GC10148 RN 1 dihydrochloride
LSD1 Inhibitor IV
An irreversible LSD1 inhibitor
GC17118 GSK J5
N-[2-(3-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-BETA-丙氨酸乙酯
A negative control compound for GSK-J4
GC13086 GSK J2
N-[2-(3-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-BETA-丙氨酸
A negative control compound for GSK-J1
GC17754 IOX 1
5-羰基-8-羟基喹啉
A 2-oxoglutarate oxygenase inhibitor
GC13919 Tranylcypromine hydrochloride
反苯环丙胺盐酸盐,SKF 385 hydrochloride
An irreversible, mechanism-based inhibitor of LSD1
GC14066 Procaine
普鲁卡因
An Analytical Reference Standard
GC11576 Tranylcypromine (2-PCPA) HCl
(1S,2R)-2-苯基-环丙胺盐酸盐,(1S,2R)-SKF 385 hydrochloride
(1S,2R)-Tranylcypromine ((1S,2R)-SKF 385) hydrochloride 是一种有效的抗抑郁剂。
GC17314 OG-L002 An LSD1 inhibitor