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dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC) which exhibits significant and selective degradation of BRD4 BD1 but is inactive on BRD4 BD2. dBET57 mediates recruitment to the CRL4CRBN E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1.
| Molecular Weight | 699.18 |
| Formula | C34H31ClN8O5S |
| CAS Number | 1883863-52-2 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage | 2-8°C, protect from light |
| Related PROTAC Products |
|---|
| ML 2-14
ML 2-14 is a E3-recruiting (RNF114, RNF4)-based PROTAC. ML 2-14 is targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219, the target protein ligand JQ-1, and the PROTAC linker. ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells. |
| GDC-2992
GDC-2992 is an orally active androgen receptor (AR) degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. |
| Setidegrasib
Setidegrasib is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib has antitumor effect. |
| PROTAC HK2 Degrader-1
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. |
| ZXH-4-130 TFA
ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). |
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