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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V51918 | JNJ-9350 | 326923-09-5 | JNJ-9350 is an inhibitor (blocker/antagonist) of spermine oxidase (SMOX) with IC50 of 0.01 μM. |
|
V51916 | JQKD82 trihydrochloride (JADA82 trihydrochloride; PCK82 trihydrochloride) | 2863676-87-1 | JQKD82 (JADA82) tri HCl is a cell-permeable (penetrable) and selective KDM5 inhibitor. |
|
V56070 | KDM2B-IN-1 | 1965248-33-2 | KDM2B-IN-1 is a histone demethylase (KDM2B) inhibitor that may be utilized in the research/study of proliferative diseases. |
|
V53270 | KDM2B-IN-2 | 1965248-01-4 | KDM2B-IN-1 is a potent inhibitor of histone demethylase (KDM2B) with IC50 of 0.021 μM in the KDM2B TR-FRET assay. |
|
V56075 | KDM2B-IN-3 | 1966933-87-8 | KDM2B-IN-3 is an inhibitor (blocker/antagonist) of the histone demethylase KDM2B. |
|
V53146 | KDM2B-IN-4 | 1966933-85-6 | KDM2B-IN-4 is an inhibitor (blocker/antagonist) of the histone demethylase KDM2B. |
|
V53316 | KDM4-IN-3 | 1068515-53-6 | KDM4-IN-3 is a KDM4 inhibitor that showed better potency in biochemical assays, was cell permeable (penetrable), and killed prostate cancer cells at low micromolar concentrations. |
|
V75853 | KDM4C-IN-1 | 52348-60-4 | KDM4C-IN-1 (Compound 4d) is a potent inhibitor of KDM4C with IC50 of 8 nM. |
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V76854 | KDM5-C49 hydrochloride (KDOAM-20 hydrochloride) | KDM5-C49 (KDOAM-20) HCl is a potent and specific KDM5 demethylase inhibitor (antagonist) with IC50s of 40 nM, 160 nM and 100 nM for KDM5A, KDM5B and KDM5C respectively. | |
|
V23032 | KDM5-C70 | 1596348-32-1 | KDM5-C70 is a novel and potent JARID1 (Jumonji AT-Rich Interactive Domain 1) Histone Demethylases Inhibitor with anticancer activity. |
|
V21991 | KDM5-IN-48 | 1628210-26-3 | KDM5-IN-48 is a novel, potent, selective and orally bioavailable KDM5 inhibitor (IC50o=15.1 nM). |
|
V51904 | KDOAM-25citrate | 2448475-08-7 | KDOAM-25 citrate is a potent and selective inhibitor of histone lysine demethylase 5 (KDM5), with IC50s of 71 nM, 19 nM, 69 nM, and 69 nM for KDM5A, KDM5B, KDM5C, and KDM5D respectively. |
|
V80481 | KDOAM-25 trihydrochloride | KDOAM-25 tri HCl is a potent and selective inhibitor of histone lysine demethylase 5 (KDM5), with IC50s of 71 nM, 19 nM, 69 nM, and 69 nM for KDM5A, KDM5B, KDM5C, and KDM5D respectively. | |
|
V75854 | LSD1-IN-22 | 2821068-05-5 | LSD1-IN-22 is a potent lysine-specific demethylase 1 (LSD1) inhibitor (antagonist) with a Ki of 98 nM. |
|
V79972 | LSD1-IN-23 | LSD1-IN-23 is a mixed competitive/noncompetitive inhibitor of lysine-specific demethylase 1 LSD1. | |
|
V51842 | LSD1-IN-24 | 4734-59-2 | LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor (antagonist) with IC50 = 0.247 μM. |
|
V51841 | LSD1-IN-25 | 2911585-60-7 | LSD1-IN-25 (Compound 9j) is a specific, orally bioactive LSD1 inhibitor (antagonist) with IC50 of 46 nM (Ki = 30.3 nM). |
|
V80623 | LSD1-IN-26 | LSD1-IN-26 (compound 12u) is a potent LSD1 inhibitor (antagonist) with IC50 of 25.3 nM. | |
|
V56072 | LSD1-IN-27 | 2904571-94-2 | LSD1-IN-27 (Compound 5ac) is an LSD1 inhibitor (IC50= 13 nM). |
|
V56073 | LSD1-UM-109 | 2252446-26-5 | LSD1-UM-109 is a potent and reversible inhibitor of LSD1 with IC50 of 3.1 nM. |
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