Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
13 Results for "
EZH1/EZH2
" in MedChemExpress (MCE) Product Catalog:
Products (13)
13 Results for "EZH1/EZH2" in MCE Product Catalog:
98
98 Cited Publications
Synonyms: EPZ-6438; E-7438
Target:
Research Areas:
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells [1].
6
6 Cited Publications
Target:
Research Areas:
EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
Synonyms: CPI-0209
Target:
Research Areas:
Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor that targets and inhibits the EZH2 enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies [1] [2] .
Cat. No.: HY-13803R
CAS No.: 1403254-99-8
Synonyms: EPZ-6438 (Standard); E-7438 (Standard)
Research Areas:
Tazemetostat (Standard) is the analytical standard of Tazemetostat. This product is intended for research and analytical applications. Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells [1].
Target:
Research Areas:
EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 [1].
Cat. No.: HY-144881
CAS No.: 2202678-05-3
Target:
Research Areas:
(S)-HH2853 (compound 200), a PYRIDINO five membered aromatic ring compound, is a potent EZH1/2 dual inhibitor with an IC50 of <100 nM for EZH2_Y641F. (S)-HH2853 has the potential to be used in the research of anti-tumor or autoimmune diseases [1].
Cat. No.: HY-P2266
CAS No.: 1453222-26-8
Target:
Research Areas:
Cat. No.: HY-122595
CAS No.: 1377997-28-8
Target:
Research Areas:
EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research [1].
Cat. No.: HY-181327
CAS No.: 2641601-66-1
Target:
Research Areas:
PROTAC EZH2 Degrader-26 (compound 11) is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-26 has an IC50 of 5.80 nM against EZH2. PROTAC EZH2 Degrader-26 exhibits micromolar-level enzyme inhibitory activity against EZH1, with an EZH1 IC50 of 0.06 μM [1].
Cat. No.: HY-181307
CAS No.: 2653338-62-4
Target:
Research Areas:
PROTAC EZH2 Degrader-12 (compound 3) is a CRBN-recruiting PROTAC-based EZH2 degrader with an EZH2 IC50 of 3.90 nM and EZH1 IC50 of 5.24 μM [1].
Cat. No.: HY-117947
CAS No.: 1809336-19-3
Target:
Research Areas:
(R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
Cat. No.: HY-181334
CAS No.: 2653338-75-9
Target:
Research Areas:
PROTAC EZH2 Degrader-39 (compound 18) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 61.00 nM. PROTAC EZH2 Degrader-39 functionally inhibits EZH2 methyltransferase activity [1].
Cat. No.: HY-181305
CAS No.: 2653338-60-2
Target:
Research Areas:
PROTAC EZH2 Degrader-10 is a selective PROTAC protein degrader targeting EZH2. PROTAC EZH2 Degrader-10 can be used for the research of cancer [1].
- 1
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
