Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13834 | PROTAC BRD4 Degrader-2 | Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM). | |||
T18598 |
PROTAC BRD2/BRD4 degrader-1
|
Others | Others |
PROTAC BRD2/BRD4 degrader-1 (compound 15) serves as a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination of BRD4 and BRD2 compared to BRD3. Its efficacy in suppressing solid tumors manifest with minimal cytotoxic effects. This compound comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN)/cullin 4A[1]. | |||
T78956 |
PROTAC BRD3/BRD4-L degrader-2
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTACBRD3/BRD4-L degrader-2 是一款可以特异性地降解BRD3和BRD4-L的PROTAC分子,其对BRD3的Ki值为16.91 nM,对BRD4-L为2.8 nM。在小鼠异种移植模型中,该分子展示了卓越的抗肿瘤效果,可被应用于癌症相关研究。 | |||
T5435 |
ARV-771
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
ARV-771 是基于 PROTAC 技术的有效 BET 降解剂,对 BRD2(1)、BRD2(2)、BRD3(1)、BRD3(2)、BRD4 (1) 和 BRD4(2)的 Kd 分别为 34、4.7、8.3、7.6、9.6 和 7.6 nM。 | |||
T36628 |
PROTAC BRD4 Degrader-8
PROTAC BRD4 Degrader-8 |
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PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1]. PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].PROTAC BRD4 Degrader-8 (4 h) potently degra... | |||
T18067 |
Lenalidomide-PEG1-azide
|
Others | Others |
Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1]. |