Histone Methyltransferase Degrader
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PROTAC EZH2 Degrader-44
0 ImagesCat. No.: HY-181413CAS No.: 3093642-25-9PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer.
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PROTAC EZH2 Degrader-21
0 ImagesCat. No.: HY-181319CAS No.: 3093642-36-2PROTAC EZH2 Degrader-21 is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-21 induces the degradation of the target protein EZH2 via specific recruitment of the cIAP E3 ligase. PROTAC EZH2 Degrader-21 exhibits significant inhibitory activity in a variety of lymphoma cell lines. PROTAC EZH2 Degrader-21 can be used for research on the pathogenesis of lymphoma.
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P-SETDB1-4
0 ImagesCat. No.: HY-184362P-SETDB1-4 is a SETDB1 PROTAC degrader with a Kd of 86 nM. P-SETDB1-4 recruits CRBN to SETDB1, induces proteasome-dependent degradation of SETDB1, and forms a ternary complex with CRBN to achieve targeted degradation. P-SETDB1-4 reduces DNA synthesis. P-SETDB1-4 exhibits anticancer activity against breast cancer. P-SETDB1-4 can be used in breast cancer-related research.
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PROTAC EZH2 Degrader-16
0 ImagesCat. No.: HY-181296CAS No.: 3093642-22-6PROTAC EZH2 Degrader-16 (compound 51) is a PROTAC protein degrader targeting EZH2 with an IC50 of 13.74 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-16 exerts antiproliferative activity against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-16 can be used for the research of diffuse large B-cell lymphoma.
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PROTAC PRMT3 degrader 1
0 ImagesCat. No.: HY-159728PROTAC PRMT3 degrader 1 is a selective PRMT3 PROTAC degrader with a DC50 of 2.566 μM. PROTAC PRMT3 degrader 1 forms a ternary complex with MDM2 E3 ubiquitin ligase to induce proteasomal and neddylation-dependent degradation of PRMT3. PROTAC PRMT3 degrader 1 activates intrinsic apoptosis, endoplasmic reticulum stress signaling pathways. PROTAC PRMT3 degrader 1 downregulates E2F, MYC, oxidative phosphorylation pathways. PROTAC PRMT3 degrader 1 reduces cellular asymmetric dimethylarginine (ADMA) levels. PROTAC PRMT3 degrader 1 inhibits acute leukemia cell growth. PROTAC PRMT3 degrader 1 acts with glycolysis inhibitor 2-DG to reduce ATP production, induce intrinsic apoptosis, drive synergistic antiproliferative effects. PROTAC PRMT3 degrader 1 can be used for the research of acute leukemia.
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PROTAC EZH2 Degrader-14
0 ImagesCat. No.: HY-181295CAS No.: 3093642-21-5PROTAC EZH2 Degrader-14 is an EZH2 PROTAC degrader, with an IC50 of 18.21 μM against diffuse large B-cell lymphoma cells, and exhibits no antiproliferative activity against non-target cells at concentrations up to 30.00 μM. PROTAC EZH2 Degrader-14 can be used in studies related to diffuse large B-cell lymphoma.
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PROTAC CARM1 degrader-1
0 ImagesCat. No.: HY-156152CAS No.: 3032785-00-2PROTAC CARM1 degrader-1 is a highly selective CARM1 PROTAC degrader, with a DC50 of 8.1 nM in MCF‑7 cells. PROTAC CARM1 degrader-1 recruits the VHL E3 ubiquitin ligase complex to act on CARM1, inducing a proteasome-dependent degradation process. PROTAC CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in breast cancer cells, inhibits breast cancer cell migration, and exhibits no significant inhibitory effect on cell proliferation. PROTAC CARM1 degrader-1 is applicable for related research on breast cancer.
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PROTAC EZH2 Degrader-42
0 ImagesCat. No.: HY-181411CAS No.: 3093642-42-0
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PROTAC PRMT1 degrader-1
0 ImagesCat. No.: HY-182275PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma.
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ND-L11B TFA
0 ImagesCat. No.: HY-170674AND-L11B TFA is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with the DC50 of 1.48 and 0.8 μM, the Dmax is closed to 80 %.
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UNC10415667
0 ImagesCat. No.: HY-178322UNC10415667 is a non-competitive, non-prodrug NSD2 degrader with a DC50 of 460 nM in U2OS NSD2 HiBiT cells. UNC10415667 forms a reversible covalent hemithioacetal bond with Cys326 of FBXO22, promoting the formation of a ternary complex with FBXO22 and NSD2, which in turn triggers the polyubiquitination and degradation of NSD2 via the ubiquitin-proteasome system. UNC10415667 can form complexes with FBXO22, NSD2 and BACH1 simultaneously, driving the synchronized degradation of NSD2 and BACH1 without competition. UNC10415667 can be used in research related to multiple myeloma, acute lymphoblastic leukemia, and prostate cancer.
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WIZ degrader 2
0 ImagesCat. No.: HY-163818CAS No.: 2839552-69-9WIZ degrader 2 (Compound 142) is a molecular glue degrader for widely interspaced zinc (WIZ) finger motifs with an AC50 of 0.011 μM. WIZ degrader 2 induces the expression of fetal hemoglobin (HbF) with an EC50 of 0.038 μM. WIZ degrader 2 can be used in research related to hereditary blood disorders, such as sickle cell disease (SCD) and thalassemia.
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C199
0 ImagesCat. No.: HY-174445CAS No.: 3107801-96-4C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity.
