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You are here:Home-Inhibitors & Agonists-Epigenetics-Histone Demethylase

Request The Product List ofHistone Demethylase Histone Demethylase

There are two classes of enzymes involved in histone methylation: methyltransferases and demethylases. While methyltransferases are responsible for establishing methylation patterns, demethylases are capable of removing methyl groups not only from histones but other proteins as well. Histone demethylases not only target methylated sites on histone tails but also interact with methylated sites on non-histone proteins, such as p53.

Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders.

JMJD1A (also named KDM3A) is a demethylasethat removes methyl from histone lysine H3K9. It plays important roles in various cellular processes, including spermatogenesis, energy metabolism, regulation of stem cell and gender display.

Jumonji domain-containing 3 (Jmjd3) has been identified as a histone demethylase, which specifically catalyzes the removal of methylation from H3K27me3.

Cat. No. Product Name CAS No. Information
GY04394

OG-L002

1357302-64-7

OG-L002 is a novel selective LSD1 inhibitor with IC50 of 20 nM; demonstrates significant potency both in inhibition of HSV IE gene expression and in suppression of viral reactivation from latency in a mouse ganglion explant model; also suppresses the expression of the initial class of hCMV and adenovirus genes in vitro; reduces the induction of TNF-α mRNA in splenocytes from mice.

GY02914

KDM5A-IN-1

1905481-36-8

An inhibitor of histone demethylase.

GY02882

QC6352

1851373-36-8

QC-6352 is a potent and selective KDM4 family inhibitor with IC50 of 104, 56, 35, and 104 nM for KDM4A, KDM4B, KDM4C, and KDM4D, respectively; displays high selectivity over other KDM family members, with the exception of KDM5B (IC50=750 nM); shows a promising cellular potency (KYSE-150 EC50=3.5 nM, H3K36 MOA=1.5 nM); has excellent physical properties and drug-like characteristics, exhibits favorable in vivo efficacy in a breast cancer PDX model and reduces the tumor initiating cell populations which are associated with resistance to chemotherapy treatments.

GY02727

KDM5-IN-1

1628210-26-3

A potent, selective and orally bioavailable KDM5 inhibitor with biochemical IC50 of 15.1, 4.7 and 65.5 nM for KDM5A, KDM5B and KDM5C, respectively; displays significantly less potent against other KDM enzymes (KDM4C IC50=1.9 uM); increases H3K4Me3 level in PC9 cells with EC50 of 0.34 uM; possesses suitable physiochemical properties and displays excellent PK profile in mice.

GY02726

CPI-455

1628208-23-0

A potent, specific histone demethylase pan-KDM5 inhibitor with biochemical IC50 of 10, 3 and 14 nM for KDM5A, KDM5B and KDM5C, respectively; shows substantially weaker potency toward KDM4C and KDM7B (200- and 770-fold, respectively) and no inhibition of KDM2B, KDM3B or KDM6A; dose-dependently increases in H3K4 methylation in multiple cell lines, decreases the number of drug-tolerant persister cancer cells (DTPs) in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

GY02496

GSK-2879552

1401966-69-5

A potent, selective irreversible inhibitor of LSD1 with Ki app of 1.7 uM; shows good selectivity against LSD2, MAO-A, MAO-B, D-amino acid oxidase and LoxL2; exhibits growth inhibition (EC50=2-240 nM) in sensitive cell lines; orally bioavailable.

GY06977

T-3775440 hydrochloride

1422535-52-1

T-3775440 hydrochloride is a novel potent, selecitve, irreversible LSD1 inhibitor with IC50 of 2.1 nM; displays high selectivity for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B); disrupts the interaction between LSD1 and growth factor-independent 1B (GFI1B) in leukemia cell lines, exhibites significant antitumor efficacy in AEL and AMKL xenograft models.

GY10210

LSD1 inhibitor 24

1853269-07-4

LSD1 inhibitor 24 is a novel potent, selective lysine-specific demethylase 1 (LSD1) inhibitor with IC50 of 1 nM, induces CD11b expression in THP-1 cells with EC50 of 8 nM; demonstrates attenuating the hERG inhibition and improving oral bioavailability.

GY10216

KDM5A covalent inhibitor N71

KDM5A covalent inhibitor N71 is an irreversible KDM5A inhibitor (IC50=0.22 uM) that covalently interacts with Cys481, >20-fold selectivity over KDM4A.

GY10217

KDM5A covalent inhibitor N73

KDM5A covalent inhibitor N73 is the the isopropyl ester derivative of N71, an irreversible KDM5A inhibitor (IC50=0.22 uM) that covalently interacts with Cys481, >20-fold selectivity over KDM4A.

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