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Histone Demethylase

Histone Demethylase

Histone methylation is carried out by methyltransferases and demethylases, two classes of enzymes. While methyltransferases are in charge of creating methylation patterns, demethylases have the ability to remove methyl groups from proteins other than histones. Histone demethylases interact with methylated sites on non-histone proteins, such as p53, in addition to targeting methylated sites on histone tails.
Due to their regulatory functions in chromatin organization and their close ties to diseases like cancer and mental disorders, histone lysine demethylases (KDMs) are of interest as drug targets.

Demethylase JMJD1A, also known as KDM3A, eliminates methyl from histone lysine H3K9. It is crucial for many cellular functions, such as spermatogenesis, energy metabolism, stem cell control, and gender expression.

A histone demethylase known as Jumonji domain-containing 3 (Jmjd3) has been discovered, and it specifically catalyzes the removal of methylation from H3K27me3.

Histone Demethylase related products

Structure Cat No. Product Name CAS No. Product Description
FY-21 V80080 FY-21 FY-21 is a selective LSD1 inhibitor (IC50=340 nM) with antiproliferation and anti-colony-forming activities.
Geranylgeranoic acid V103459 Geranylgeranoic acid 35750-48-2 Geranylgeranic acid (compound 5) inhibits lysine-specific demethylase 1 (LSD1) with an IC50 value of 46.97 µM.
GSK 690 Hydrochloride V52030 GSK 690 Hydrochloride 2436760-79-9 GSK 690 ( HCl) is a reversible inhibitor of lysine-specific demethylase 1 (LSD1) with a Kd of 9 nM and IC50 of 37 nM.
GSK J4 HCl V4761 GSK J4 HCl 1797983-09-5 GSK J4 (GSK-J4) is a novel,cell permeable, and potent prodrug of GSK J1 with anti-inflammatory effects.
GSK-690 V3540 GSK-690 2101305-84-2 GSK 690 is a novel, potent and selective reversible inhibitor of lysine specific demethylase 1(LSD1), with aKdvalue of 9 nM and a biochemicalIC50of 37 nM.
GSK-690 HCl V45816 GSK-690 HCl GSK-690 hydrochloride is a selective reversible inhibitor of lysine specific demethylase 1(LSD1) with anticancer activity.
GSK-J1 lithium salt V76952 GSK-J1 lithium salt 2309668-29-7 GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM for KDM6B.
GSK-J1 sodium V88877 GSK-J1 sodium 1797832-71-3 GSK-J1 sodium is an inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50 of 60 nM for KDM6B.
GSK-J4 V2660 GSK-J4 1373423-53-0 GSK J4 is a novel,cell permeable, and potent prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase (KDM) JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and is inactive against a panel of demethylases of the JMJ family.
GSK-LSD1 V75860 GSK-LSD1 1431368-48-7 GSK-LSD1 is an LSD1 inhibitor.
GSK-LSD1 2HCl V0376 GSK-LSD1 2HCl 1821798-25-7 GSK-LSD1 2HCl, thedihydrochloride salt of GSK-LSD1 (GSK-LSD-1), is an irreversible, potent and selectiveinhibitor ofLysine (K) -specific demethylase 1A (LSD1) with antineoplastic activity.
GSK-LSD1 dihydrochloride V52029 GSK-LSD1 dihydrochloride 2102933-95-7 GSK-LSD1 diHCl is a potent, selective, irreversible inhibitor of lysine-specific demethylase (LSD1) with IC50 of 16 nM.
GSK2807 TFA V4128 GSK2807 TFA 2245255-66-5 GSK2807 TFA (GSK-2807 TFA), the trifluoroacetic acid salt form ofGSK2807, is a selective and SAM-competitiveSMYD3inhibitorwith potential antitumor activity.
GSK2879552 dihydrochloride V52036 GSK2879552 dihydrochloride 1902123-72-1 GSK2879552 diHCl is an orally bioavailable, irreversible LSD1/KDM1A inhibitor (antagonist) with anti-tumor activity.
HDAC-IN-57 V51995 HDAC-IN-57 2716217-79-5 HDAC-IN-57 is an orally bioactive pan-inhibitor of histone deacetylase (HDAC) with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6 and HDAC8 respectively.
HDAC6-IN-3 V79995 HDAC6-IN-3 3023019-99-7 HDAC6-IN-3 (Compound 14) is an active anti-prostate cancer molecule and a potent, orally bioactive HDAC6 inhibitor (antagonist) with IC50 range of 0.02- 1.54 μM.
HSP90/LSD1-IN-1 V96827 HSP90/LSD1-IN-1 HSP90/LSD1-IN-1 (Compound 6) is a dual HSP90/LSD1 inhibitor.
INCB059872 V51948 INCB059872 1802909-49-4 INCB059872 is a potent, orally bioactive, selective and irreversible lysine-specific demethylase 1 (LSD1) inhibitor.
INCB059872 dihydrochloride V76894 INCB059872 dihydrochloride INCB059872 di-HCl is a potent, orally bioactive, selective and irreversible inhibitor of lysine-specific demethylase 1 (LSD1).
INCB059872 tosylate V94282 INCB059872 tosylate 2081940-67-0 INCB059872 mesylate is a potent, selective and orally active lysine demethylase 1 inhibitor.
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