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 |
|---|---|---|---|---|
|
V76508 | SKLB325 | SKLB325 is a JMJD6 inhibitor (antagonist) with a binding affinity (KD) value of 0.755 μM and IC50 of 0.7797 μM. | |
|
V0373 | SP2509 (HCI-2509) | 1423715-09-6 | SP2509 (HCI2509) is a novel, potent and selective histone demethylase LSD1(KDM1A) antagonistwith antineoplastic activity. |
|
V5227 | T-3775440 HCl | 1422535-52-1 | T-3775440 (T3775440) HCl is a novel, potent, selective, and irreversible lysine-specific histone demethylase(LSD1)inhibitor with anticancer activity. |
|
V76412 | TK-129 | TK-129 is an orally bioavailable, low-toxic, and potent KDM5B inhibitor (with high affinity; IC50=44 nM). | |
|
V56068 | Zavondemstat | 1851412-93-5 | Zavondemstat (QC8222; TACH 101) is a histone lysine demethylase 4D (KDM4D) inhibitor (antagonist) with anti-tumor activity. |
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