Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit
Note
10mg卖完停产，不再备货
Product Description
Information
Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with K i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.
Targets
EZH2 (Cell-free assay) 2.5 nM(Ki)
In vitro
EPZ-6438 concentration-dependently reduces global H3K27Me3 levels in wild-type or SMARCB1 mutant cells, and induces strong antiproliferative effects with IC50 ranging from 32 nM to 1000 nM in SMARCB1-deleted MRT cell lines. EPZ-6438 induces gene expression of neuronal differentiation and cell cycle inhibition, while inhibtis expression of Hedgehog pathway genes, MYC and EZH2. The antiproliferative effect of EPZ-6438 is enhanced by either prednisolone or dexamethasone in several EZH2 mutant lymphoma cell lines.
In vivo
In SCID mice bearing s.c. G401 xenografts, EPZ-6438 induces tumor stasis during the administration period and produces a significant tumor growth delay with minimal effect on body weight.
Cell Research(from reference)
Cell lines：Mutant cell lines (G401, A204, G402, KYM-1), Wild type cell line (RD, 293, SJCRH30)
1.Hornick JL, Dal Cin P, Fletcher CD. (2009) Loss of INI1 expression is characteristic of both conventional and proximal-type epithelioid sarcoma.. Am J Surg Pathol, 33 (4):(542-50). [PMID:19033866]
2.Patil PA, Lombardo K, Sturtevant A, Mangray S, Yakirevich E. (2018) Loss of Expression of a Novel Chromatin Remodeler SMARCA1 in Soft Tissue Sarcoma.. J Cytol Histol, 9 (6):(524). [PMID:31093468]
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C2419472
