Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation.E3 Ligase Binder, Linker, and Target Binder are the components of PROTACs. The Target Binder is a ligand (often a small-molecule inhibitor) for the protein of interest. When the PROTACs attach to the target protein, they can recruit E3 for target protein ubiquitination, which results in proteasome-mediated destruction of the protein. Because of this, PROTACs work by destroying the target proteins rather than blocking them, which is far more effective at overcoming resistance brought on by target mutation or overexpression. In order to overcome resistance, PROTAC technology has been used on a number of targets, including AR, ER, BTK, BET, and BCR-ABL.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V81224 | PROTAC BRD4 Degrader-22 | PROTAC BRD4 Degrader-22 (Compd 44h) is a potent BRD4 PROTAC protein degrader with pDC50 (MOLT4, 24 h) of 9.2. | |
|
V81225 | PROTAC BRD9 Degrader-7 | PROTAC BRD9 Degrader-7 is an orally bioactive BRD9 selective degrader with DC50 of 1.02 nM. | |
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V37560 | PROTAC BRD9-binding moiety 1 hydrochloride | PROTAC BRD9-binding moiety 1 HCl is a structure that can bind to BRD9 and inhibits the activity of BRD9 based on PROTAC technology. | |
|
V69681 | PROTAC BTK Degrader-1 | 2801715-13-7 | PROTAC BTK Degrader-1 is a specific and orally bioactive PROTAC BTK degrader with IC50s of 34.51 nM and 64.56 nM for wild-type BTK and mutant BTK-481S, respectively. |
|
V69700 | PROTAC BTK Degrader-2 | 2250382-66-0 | PROTAC BTK Degrader-2 is an effective BTK PROTAC protein degrader. |
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V69684 | PROTAC BTK Degrader-3 | 2563861-90-3 | PROTAC BTK Degrader-3 is a potent BTK PROTAC degrader with DC50 of 10.9 nM for BTK degradation in Mino cells. |
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V69694 | PROTAC BTK Degrader-6 | 2767204-39-5 | PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50= 3.18 nM). |
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V82335 | PROTAC EED degrader-1 | 2639882-72-5 | PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC molecule targeting EED with a pKD of 9.02. |
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V82336 | PROTAC EED degrader-2 | 2639882-69-0 | PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC molecule targeting EED with a pKD of 9.27. |
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V69375 | PROTAC EGFR degrader 4 | 2882845-50-1 | PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR. |
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V76594 | PROTAC EGFR degrader 7 diTFA | PROTAC EGFR degrader 7 diTFA (compound 13b) is a specific CRBN-recruiting degrader of PROTAC EGFRL858R/T790M with DC50 of 13.2 nM. | |
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V67667 | PROTAC ER Degrader-10 | 2504911-58-2 | PROTAC ER Degrader-10 is a potent PROTAC ER degrader for use in cancer research. |
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V37540 | PROTAC ER Degrader-2 | PROTAC ER Degrader-2 is an intermediate in the preparation /synthesis of PAC. | |
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V37539 | PROTAC ER α Degrader-1 | PROTAC ER α Degrader-1 is a PROTAC degrader | |
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V67722 | PROTAC ERRα Degrader-3 | 2306388-65-6 | PROTAC ERRα Degrader-3 is a potent and specific ERRα degrader based on von Hippel-Lindau ligand. |
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V37549 | PROTAC ERα Degrader-1 | PROTAC ERα Degrader-1 contains a ubiquitin E3 ligase binding group, linker and target protein binding group. | |
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V67656 | PROTAC ERα Degrader-1 | 2417369-94-7 | PROTAC ERα Degrader-1 contains a ubiquitin E3 ligase binding group, linker and target protein binding group. |
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V67713 | PROTAC ERα Degrader-4 | 2521299-80-7 | PROTAC ERα Degrader-4 is a highly efficient and selective estrogen receptor (Estrogen Receptor/ERR) ERα subtype PROTACs containing OBHSAs, linker and E3 ligase ligands. |
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V81229 | PROTAC EZH2 Degrader-2 | PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC consisting of Tazemetostat (EPZ6438) and an E3 ligase system ligand. | |
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V81231 | PROTAC GDI2 Degrader-1 | PROTAC GDI2 Degrader-1 (Compound 21) is an effective PROTAC GDI2 degrader. |
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