ezh2-in-3

EZH2-IN-3 is an inhibitor of EZH2 and EZH1 with selective impact on diffuse large B cell lymphoma cell growth.

3-Deazaneplanocin A HCl is a synthetically derived inhibitor of the histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (SAHH). By regulating epigenetic methylation pathways, 3-deazaneplanocin A induces apoptosis and inhibits tumor cell proliferation, demonstrating significant antitumor activity in various tumor models. 3-deazaneplanocin A HCl can be used in research on epigenetic regulation, tumorigenesis and progression, and stem cell differentiation.

TC-5115 is a highly potent, selective inhibitor of the SET domain of the histone lysine methyltransferase MLL1 (KMT2A), with an IC₅₀ value of 16 nM. TC-5115 exhibits weak inhibitory activity against other methyltransferases such as SET7/9, DOT1L, and EZH2 (IC₅₀ > 1 μM). TC-5115 induces differentiation and growth arrest in leukemia cells and can be used in leukemia research.

PROTAC EZH2 Degrader-3 (compound ZJ-20) is a potent EZH2 degrader that exhibits strong inhibitory effects not only on EZH2 protein expression but also on the levels of other PRC2 subunits and H3k27me3 protein. Additionally, PROTAC EZH2 Degrader-3 demonstrates antiproliferative activity by blocking the cell cycle at the G0-G1 phase and inducing apoptosis (cell death). At a concentration of 5 μM and over a period of 24 hours, it effectively suppresses the expression of these critical proteins involved in cell regulation and growth.

PROTACEZH2 Degrader-9 is an orally active EZH2 PROTAC degrader, operating through the ubiquitin-proteasome pathway. It effectively reduces the PRC2 core subunit and potently inhibits H3K27me3 without affecting common CRBN neo-substrates, showing selectivity towards GSPT1 and IKZF1/3. The compound exhibits strong antiproliferative effects on various cancer cell lines by inducing cell cycle arrest and apoptosis (apoptosis). Additionally, PROTACEZH2 Degrader-9 reverses PRC2-mediated gene silencing and suppresses the activation of EZH2 non-catalytic target genes. This compound is applicable in research on leukemia, lymphoma, and non-small cell lung cancer.

3-Deazaneplanocin A (DZNep) is a dual inhibitor of histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (AHCY) with antipoxidative activity that inhibits hepatic, renal, peritoneal, and airway fibrosis by inducing proteasomal degradation of its targets and reducing toxicity in animal models.