About 31 results found for searched term "ER degrader 5" (0.108 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M10383 | Homo-PROTAC cereblon degrader 1 (OUN20985) | PROTAC |
| OUN20985 | ||
| Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3. | ||
| M43602 | ER degrader 5 | Estrogen Receptor |
| ER degrader 5 is a potent estrogen receptor (ER) 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. | ||
| M10254 | SAR439859 (Amcenestrant) | Estrogen Receptor |
| SAR-439859; Amcenestrant | ||
| SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation. | ||
| M14875 | PROTAC FAK degrader 1 | PROTAC |
| PROTAC FAK degrader 1 is a selective and potent von Hippel-Lindau-based focal adhesion kinase (FAK) degrader with an IC50 of 6.5 nM, DC50 of 3 nM. | ||
| 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). | ||
| M29225 | PROTAC Sirt2 Degrader-1 | Sirtuin |
| PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM). | ||
| M29314 | PROTAC Mcl1 degrader-1 | PROTAC |
| PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM. | ||
| 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. | ||
| M29357 | JH-XI-10-02 | PROTAC |
| JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19. | ||
| 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). | ||
| M29518 | TD-428 | PROTAC |
| TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation. | ||
| M29520 | BSJ-04-132 | PROTAC |
| BSJ-04-132 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity. | ||
| M29530 | PROTAC IRAK4 degrader-1 | PROTAC |
| PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively. | ||
| M29538 | CRBN-6-5-5-VHL | PROTAC |
| CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3. | ||
| 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. | ||
| M29544 | TMX-4100 | PDE |
| TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC50 values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma. | ||
| M29548 | PROTAC PARP1 degrader | PROTAC |
| PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM. | ||
| M29618 | Pomalidomide-C3-adavosertib | Wee1 |
| Pomalidomide-C3-adavosertib is a rapid and selective Wee1 degrader (IC50=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces 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. | ||
| M29813 | PROTAC STING Degrader-1 | STING |
| PROTAC STING Degrader-1 (Compound SP23) is a STING PROTAC degrader with a DC50 of 3.2 μM. PROTAC STING Degrader-1 shwos anti-inflammatory activity. | ||
| 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. | ||
| M31276 | PROTAC CDK2/9 Degrader-1 | PROTAC |
| PROTAC CDK2/9 Degrader-1 is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand. | ||
| M43381 | PROTAC GSK-3β Degrader-1 | GSK-3 |
| PROTAC GSK-3β Degrader-1 is a degrader targets GSK-3β degradation with an IC50 value of 833 nM. | ||
| M43406 | PROTAC BTK Degrader-6 | BTK |
| PROTAC BTK Degrader-6 is a PROTAC BTK degrader (DC50: 3.18 nM. | ||
| M43411 | PROTAC BRD9 Degrader-6 | Epigenetic Reader Domain |
| PROTAC BRD9 Degrader-6 is a potent degrader of BRD9 (IC50=0.13 nM), can be used for research of BAF complex-related disorders. | ||
| M43413 | ERD-3111 | Estrogen Receptor |
| ERD-3111 is an orally active PROTAC ERα degrader (DC50: 0.5 nM). | ||
| 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%. | ||
| M43430 | PROTAC CDK12/13 Degrader-1 TFA | PROTAC |
| PROTAC CDK12/13 Degrader-1 TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. | ||
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