About 14 results found for searched term "ER degrader 7" (0.229 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M41544 | ER degrader 7 | Microtubule |
| ER degrader 7 is an ERα and ERβ degrader. | ||
| M25607 | ARV-766 | PROTAC |
| Luxdegalutamide | ||
| ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations. ARV-766 has the potential to be first- and best-in class PROTAC AR degrader in mCRPC. | ||
| M25473 | HaloPROTAC3 | Ligand for E3 Ligase |
| VH285-PEG4-C4-Cl | ||
| HaloPROTAC3 is a conjugate of ligands for E3 and 16-atom-length linker, and it is also a highly potent and efficacious degrader of GFP-HaloTag7 fusion proteins with a DC50 of 19 nM. | ||
| M29136 | PROTAC TBK1 degrader-2 | PROTAC |
| PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM). | ||
| M29153 | FKBP12 PROTAC dTAG-7 | PROTAC |
| dTAG-7 | ||
| FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN. | ||
| M29317 | UT-34 | Androgen Receptor |
| UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy. | ||
| M29440 | TL12-186 | PROTAC |
| TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM). | ||
| M29507 | ERD-308 | PROTAC |
| ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively). | ||
| M29541 | XZ739 | PROTAC |
| XZ739, a Cereblon-dependent PROTAC BCL-XL (Bcl-2 family member) degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis. | ||
| M29689 | SK-575 | PARP |
| SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations. | ||
| M29837 | Akt3 degrader 1 | Akt |
| Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer. | ||
| M43429 | PROTAC α-synuclein degrader 5 | PROTAC |
| PROTAC α-synuclein degrader 5 is a highly selective small-molecule degraders (PROTAC) of α-synuclein aggregates, with an DC50 of 7.51 μM and the highest degradation rate Dmax of 89%. | ||
| M43475 | PROTAC BTK Degrader-5 | BTK |
| PROTAC BTK degraders-5is a selective BTK degrader with a DC50 value of 7.0 nM in JeKo-1 cells. | ||
| M43603 | ERα degrader 6 | Estrogen Receptor |
| ERα degrader 6 is an ERα degrader (KI: 75 nM). | ||
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