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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
51 Results for "
PRC2
" in MedChemExpress (MCE) Product Catalog:
Products (51)
51 Results for "PRC2" in MCE Product Catalog:
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MS181 is a BMI1 and RING1B degrader with antiproliferative activity. MS181 induces degradation via an EED-, CRBN-, and ubiquitin-proteosome system-dependent pathway, with preferential targeting over PRC2 components. MS181 acts in VHL-defective cancer cells. MS181 serves as a chemical biology tool to study PRC1 roles in cancer. MS181 can be used for the research of myelogenous leukemia, renal cell carcinoma, metastatic prostate cancer, triple negative breast cancer .
Cat. No.: HY-P2254
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Cat. No.: HY-W003282
CAS No.: 39919-65-8
Cat. No.: HY-162384
CAS No.: 3034959-68-4
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EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency .
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-174372
CAS No.: 3095068-20-2
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EZH2-IN-23 (Compound 25) is an EZH2 inhibitor that exhibits potent enzymatic inhibition of the PRC2 complex (EZH2, EED, SUZ12, AEBP2, RbAp48) with a biochemical IC50 of 0.8 nM. EZH2-IN-23 inhibits H3K27 trimethylation in cellular assays, showing an IC50 of 40 nM. EZH2-IN-23 displays good rat PKproperties with 100 % oral bioavailability.
Cat. No.: HY-168131
CAS No.: 3098718-46-5
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PROTAC EZH2 Degrader-3 is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 induces the global degradation of the PRC2 complex (including EZH2, SUZ12, EED, RbAp48) via the ubiquitin-proteasome pathway and downregulates H3K27me3 levels. PROTAC EZH2 Degrader-3 inhibits cancer cell proliferation and induces their apoptosis. PROTAC EZH2 Degrader-3 can be used in research related to lymphoblastoma and diffuse large B-cell lymphoma .
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EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.
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-P2252
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Cat. No.: HY-101512D
CAS No.: 2747996-65-0
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rel-A-395 hydrochloride is the relative configuration of A-395 (HY-101512) hydrochloride. A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM .
Cat. No.: HY-P2253
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Cat. No.: HY-174397
CAS No.: 3051817-48-9
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EED-IN-3 is an orally active EED inhibitor. EED-IN-3 effectively inhibits PRC2 by binding to EED (IC50 = 0.62 μM for EED) and downregulates H3K27me3. EED-IN-3 can efficiently and selectively inhibit PC3 cells with the IC50 of 3.69 μΜ and could significantly suppress colony formation and migration. EED-IN-3 can be used for research on prostate cancer.
Cat. No.: HY-P2266
CAS No.: 1453222-26-8
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Cat. No.: HY-101117R
CAS No.: 2083627-02-3
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EED226 (Standard) is the analytical standard of EED226 (HY-101117). This product is intended for research and analytical applications. EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor [2]. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
Cat. No.: HY-188147
CAS No.: 2636048-41-2
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EZH2-IN-25 is an EZH2 inhibitor that inhibits the catalytic subunit of PRC2. EZH2-IN-25 can be used for the research of diffuse large B cell lymphoma .
Cat. No.: HY-117947
CAS No.: 1809336-19-3
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(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-100846R
CAS No.: 1913252-04-6
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JQEZ5 (Standard) is the analytical standard of JQEZ5 (HY-100846). This product is intended for research and analytical applications. JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects .
Cat. No.: HY-101512R
CAS No.: 2089148-72-9
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A-395 (Standard) is the analytical standard of A-395 (HY-101512). This product is intended for research and analytical applications. A-395, a chemical probe, is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM .
Cat. No.: HY-181320
CAS No.: 2653338-65-7
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PROTAC EZH2 Degrader-19 (compound 6) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.00 nM. PROTAC EZH2 Degrader-19 induces strong degradation of all PRC2 subunits (EZH2, SUZ12, EED, RbAp48) in a concentration- and time-dependent manner.PROTAC EZH2 Degrader-19 exhibits antiproliferative effects in cancer cells.PROTAC EZH2 Degrader-19 can be used for the research of 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
