3004503-12-9
3004503-12-9
Chemical Structure
NUCC-0226272
- CAS No.: 3004503-12-9
- Formula:C67H91N9O8S
- Molecular Weight:1182.56
InChIKey: GQULETMWOLCBGK-MUSRFAHESA-N
SMILES: CCN(C1CCOCC1)C2=CC(C3=CC=C(C=C3)CN4CCN(CC4)C(CCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O)=O)=CC(C(NCC8=C(C=C(NC8=O)C)C)=O)=C2C
Biological Activity: NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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NUCC-0226272 | 99.68% | NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research. | ||||||||||||||||||||
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YM281 | YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma. | |||||||||||||||||||||
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MS8815 | 99.95% | MS8815 is a EZH2 PROTAC degrader, with a DC50 of 140 nM in MDA-MB-453 triple-negative breast cancer (TNBC) cells and an IC50 of 8.6 nM against human EZH2. MS8815 induces ubiquitin-proteasome system-mediated degradation of EZH2, reduces the levels of EED, SUZ12, FOXM1, H3K27me3 and global m6A, and increases the protein level of HMGCS2. MS8815 can be used in the research of breast cancer and prostate cancer. | ||||||||||||||||||||
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MS8815N | MS8815N is a negative control of EZH2 PROTAC degrader MS8815 (HY-148334). MS8815N is incapable of recruiting the VHL E3 ligase but retains the same EZH2 binding moiety and linker. MS8815N can be used for triple-negative breast cancer (TNBC) research. | |||||||||||||||||||||
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MS8847 | 99.78% | MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC50=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer. | ||||||||||||||||||||
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PROTAC EZH2 Degrader-28 | PROTAC EZH2 Degrader-28 is an EZH2 PROTAC degrader. PROTAC EZH2 Degrader-28 promotes the ubiquitination and degradation of EZH2. PROTAC EZH2 Degrader-28 can be used for lymphoma-related research. | |||||||||||||||||||||
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PROTAC EZH2 Degrader-43 | PROTAC EZH2 Degrader-43 (compound 59) is a PROTAC protein degrader targeting EZH2 with an IC50 of 21.73 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-43 can be used for the research of lymphoma. | |||||||||||||||||||||
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PROTAC EZH2 Degrader-44 | PROTAC 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-45 | PROTAC EZH2 Degrader-45 (compound 61) is a PROTAC protein degrader targeting EZH2 with an IC50 of 22.97 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-45 can be used for the research of diffuse large b-cell lymphoma. | |||||||||||||||||||||
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MS8847N1 | MS8847N1 is a negative control analog of MS8847 (HY-162250), which abolishes binding to EZH2 while retaining the activity of recruiting VHL. MS8847N1 does not induce EZH2 degradation. MS8847N1 can be used in PROTAC-related research. | |||||||||||||||||||||
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MS8847N2 | MS8847N2 is a negative control analog of an EZH2 PROTAC degrader that binds EZH2 but does not bind the VHL E3 ligase or induce EZH2 degradation. | |||||||||||||||||||||
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