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EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
| Cell Experiment | |
|---|---|
| Cell lines | WSU-DLCL2 cells |
| Preparation method | For assessment of cell proliferation and viability, exponentially growing cells are plated, in triplicate, in 96-well plates. Cells are incubated with increasing concentrations of EPZ011989. Viable cell number is determined every 3-4 days for up to 11 days using the Guava Viacount assay. |
| Concentrations | 0-10 μM |
| Incubation time | 0-11 days |
| Animal Experiment | |
|---|---|
| Animal models | SCID mice |
| Formulation | 0.5% methyl cellulose and 0.1% Tween-80 |
| Dosages | 250 and 500 mg/kg |
| Administration | p.o. |
| Molecular Weight | 605.81 |
| Formula | C35H51N5O4 |
| CAS Number | 1598383-40-4 |
| Solubility (25°C) | DMSO: ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone Methyltransferase Products |
|---|
| WDR5-IN-4
WDR5-IN-4 is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity. |
| CMP-5 dihydrochloride
CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. |
| MS67
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. |
| MS8511
MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). |
| TM2-115
TM2-115 inhibits malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death. |
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