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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
28 Results for "
EZH2-IN-2
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "EZH2-IN-2" in MCE Product Catalog:
Cat. No.: HY-A0298
CAS No.: 2238821-31-1
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EZH2-IN-2 (Example 69) is a EZH2 inhibitor with an IC50 and a TR-FRET IC50 of 64 nM and 20 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity .
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3 Cited Publications
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MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2-PRC2 and noncanonical EZH2-cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest .
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2 Cited Publications
Cat. No.: HY-N5024
CAS No.: 173932-75-7
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Ketones, Aldehydes, Acids Guttiferae Phenols Polyphenols Plants Garcinia hanburyi Hook. f. Disease Research Fields Cancer
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PROTAC EZH2 Degrader-2 is a PROTAC EZH2 inhibitor. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner. PROTAC EZH2 Degrader-2 induces apoptosis and reduces mitochondrial membrane potential in SU-DHL-6 cells. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .
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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 .
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GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .
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TDI-6118 (Compound 5) is a potent brain-penetrant inhibitor of EZH2. EZH2-IN-12 has the potential for the research of central nervous system malignancies .
Cat. No.: HY-161083
CAS No.: 3026744-15-7
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PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
Cat. No.: HY-122640
CAS No.: 864819-54-5
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NPD13668 is an EZH2-mediated gene silencing modulator. NPD13668 inhibits EZH2/PRC2 (polycomb repressive complex 2) activity. NPD13668 reactivates the expression of silenced H3K27me3 target genes together with depletion of the H3K27me3 modification. NPD13668 can be used for the study of prostate cancer and ovarian cancer .
Cat. No.: HY-178694
CAS No.: 120430-77-5
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DC-PRC2in-01 is a potent EZH2-EED interaction inhibitor with an IC50 of 4.21 μM and a Kd of 4.56 μM. DC-PRC2in-01 disrupts the EZH2-EED interaction, leading to degradation of PRC2 core proteins and decrease of H3K27me3 levels, inhibition of PRC2-driven lymphoma cell proliferation, and cell cycle arrest. DC-PRC2in-01 can be used for the research of PRC2-related cancers, such as Diffuse Large B-cell Lymphoma (DLBCL) and follicular lymphoma (FL) .
Cat. No.: HY-P2266
CAS No.: 1453222-26-8
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Cat. No.: HY-149463
CAS No.: 2238820-26-1
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EZH2-IN-16 (Compound 24) is an inhibitor for histone methyltransferase (EZH2). EZH2-IN-16 inhibits EZH2 and EZH2 Y641F, with IC50 of 37.6 and 79.1 nM. EZH2-IN-16 inhibits proliferation of WSU-DLCL2, with GI50 of 0.2 μM .
Cat. No.: HY-143616
CAS No.: 2659225-28-0
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EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259) .
Cat. No.: HY-181325
CAS No.: 2653338-68-0
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PROTAC EZH2 Degrader-24 (compound 9) is an EZH2-targeting PROTAC with EZH2 methyltransferase inhibitory activity .
Cat. No.: HY-181309
CAS No.: 2653338-64-6
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PROTAC EZH2 Degrader-15 (compound 5) is an EZH2-targeting PROTAC. PROTAC EZH2 Degrader-15 functionally inhibits EZH2 methyltransferase activity .
Cat. No.: HY-185582
CAS No.: 3050872-19-7
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EZH2 ligand-4 (Precursor 1) is a ligand for the target protein for PROTAC (EZH2). EZH2 ligand-4 can be used to synthesize MS8847 (HY-162250) .
Cat. No.: HY-179500
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EZH2 ligand-Linker Conjugate 1 is a target protein ligand-lnker conjugate that incorporates a target protein ligand for EZH2. EZH2 ligand-Linker Conjugate 1 can be used for the synthesis of PROTAC EZH2 Degrader-9 (HY-179499) .
Cat. No.: HY-181318
CAS No.: 3093642-35-1
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PROTAC EZH2 Degrader-20 (compound 54) is an EZH2-target PROTAC degrader with antiproliferative activity and IC50 values of about 10 μM against lymphoma cells. PROTAC EZH2 Degrader-20 can be used for the research of lymphoma .
Cat. No.: HY-181308
CAS No.: 2653338-63-5
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PROTAC EZH2 Degrader-13 is an EZH2-targeting PROTAC with an IC50 of 2.70 nM. PROTAC EZH2 Degrader-13 exerts antiproliferative effects in cancer cells. PROTAC EZH2 Degrader-13 can be used for the research of cancer .
Cat. No.: HY-181391
CAS No.: 2653338-71-5
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PROTAC EZH2 Degrader-34 (compound E7 (13)) is an EZH2-target PROTAC degrader with a human EZH2 IC50 of 6.30 μM. PROTAC EZH2 Degrader-34 can be used for the research of pfeiffer cancer, prostate cancer .
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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
