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 |
|---|---|---|---|---|
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V56071 | S1427 | 2447061-40-5 | S1427 is a tranylcypromine-derived LSD1 inhibitor (antagonist) with IC50 of 390 nM and a Ki of 80 nM. |
|
V37863 | S2116 | 2262489-89-2 | S2116 is an N-alkylated trans-cyclopropylamine (TCP) analogue and a potent lysine-specific demethylase 1 (LSD1) inhibitor. |
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V37842 | S2157 | 2262488-39-9 | S2157 is an N-alkylated trans-cyclopropylamine (TCP) analogue and a potent lysine-specific demethylase 1 (LSD1) inhibitor. |
|
V3833 | Seclidemstat | 1423715-37-0 | Seclidemstat (formerly also known as SP-2577; SP2577) is a novel, potent small molecule inhibitor of epigenetic enzyme LSD1 (lysine-specific demethylase 1) with anticancer activity. |
|
V37130 | Seclidemstat mesylate (SP-2577 mesylate) | 2044953-70-8 | Seclidemstat (SP-2577) mesylate is a potent, noncompetitive, reversible inhibitor of KDM1A (LSD1) (Ki=31 nM, IC50). |
|
V76508 | SKLB325 | SKLB325 is a JMJD6 inhibitor (antagonist) with a binding affinity (KD) value of 0.755 μM and IC50 of 0.7797 μM. | |
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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. |
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V76412 | TK-129 | TK-129 is an orally bioavailable, low-toxic, and potent KDM5B inhibitor (with high affinity; IC50=44 nM). | |
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V56068 | Zavondemstat | 1851412-93-5 | Zavondemstat (QC8222; TACH 101) is a histone lysine demethylase 4D (KDM4D) inhibitor (antagonist) with anti-tumor activity. |
|
V85238 | Zavondemstat L-lysine (QC8222; TACH 101) | 2908753-10-4 |
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