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EPZ-6438 , CAS 1403254-99-8
EPZ-6438 , CAS 1403254-99-8
Artikelnummer
BPS27626-3
Verpackungseinheit
100 mg
Hersteller
BPS Bioscience
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Background: EPZ-6438 competitively binds to the S-adenosylmethionine (SAM) binding site of EZH2 and also non-competitively binds to the binding sites of peptide or nucleosome substrate. EPZ-6438 selectively inhibits EZH2 with selectivity 35-fold greater than EZH1. Study results have suggested that EPZ-6438 exhibits dramatic and permanent anti-tumor activity in MRT models through synergistic effects of EPZ-6438-mediated EZH2 inhibition on several cancer pathways.
Biological Activity: EPZ-6438 is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM, exhibiting a 35-fold selectivity versus EZH1 and over 4,500-fold selectivity relative to 14 other HMTs.
CAS Number: 1403254-99-8
Description: EPZ-6438 is a potent and bio-available inhibitor of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27), that inhibits the activity of human PRC2-containing wild-type EZH2 (Ki = 2.5 nM).
Purity: ≥99% by HPLC
Solubility: Soluble in EtOH
Storage Stability: Store desiccated at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: EZH2
Warnings: Protect from moisture.
Biosafety Level: Not applicable (BSL-1)
References: Knutson, SK, et al. PNAS 2013; 110(19): 7922-7927.
Background: EPZ-6438 competitively binds to the S-adenosylmethionine (SAM) binding site of EZH2 and also non-competitively binds to the binding sites of peptide or nucleosome substrate. EPZ-6438 selectively inhibits EZH2 with selectivity 35-fold greater than EZH1. Study results have suggested that EPZ-6438 exhibits dramatic and permanent anti-tumor activity in MRT models through synergistic effects of EPZ-6438-mediated EZH2 inhibition on several cancer pathways.
Biological Activity: EPZ-6438 is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM, exhibiting a 35-fold selectivity versus EZH1 and over 4,500-fold selectivity relative to 14 other HMTs.
CAS Number: 1403254-99-8
Description: EPZ-6438 is a potent and bio-available inhibitor of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27), that inhibits the activity of human PRC2-containing wild-type EZH2 (Ki = 2.5 nM).
Purity: ≥99% by HPLC
Solubility: Soluble in EtOH
Storage Stability: Store desiccated at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: EZH2
Warnings: Protect from moisture.
Biosafety Level: Not applicable (BSL-1)
References: Knutson, SK, et al. PNAS 2013; 110(19): 7922-7927.
| Artikelnummer | BPS27626-3 |
|---|---|
| Hersteller | BPS Bioscience |
| Hersteller Artikelnummer | 27626-3 |
| Green Labware | Nein |
| Verpackungseinheit | 100 mg |
| Mengeneinheit | STK |
| Produktinformation (PDF) |
|
| MSDS (PDF) |
|
Immer für Sie da
Gernot Ensinger, M.Sc.
Laurent Haze
