About 28 results found for searched term "ER degrader 4" (0.15 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M43444 | PROTAC ERα Degrader-4 | PROTAC |
| PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). | ||
| M43599 | ER degrader 4 | Estrogen Receptor |
| ER degrader 4 is a selective and orally active estrogen receptor degrader. | ||
| M14865 | VH032-cyclopropane-F | Ligand for E3 Ligase |
| VHL ligand 3; E3 ligase Ligand 19 | ||
| VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4. | ||
| M28222 | PROTAC AR Degrader-4 | PROTAC |
| PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs). | ||
| 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. | ||
| M29188 | Rintodestrant | Estrogen Receptor |
| G1T48 | ||
| Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor. | ||
| M29228 | BRD4 degrader AT1 | PROTAC |
| BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4BD2 in cells. | ||
| 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. | ||
| M29372 | MI-389 | PROTAC |
| MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4CRBN E3 ligase. | ||
| 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. | ||
| 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. | ||
| M31078 | PROTAC AR Degrader-4 TFA | PROTAC |
| PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs). | ||
| M41653 | PROTAC BRD4 Degrader-20 | Epigenetic Reader Domain |
| PROTAC BRD4 Degrader-20 is an bifunctional compound and an degrader of BRD4. | ||
| M41659 | PROTAC BRD4 Degrader-21 | Epigenetic Reader Domain |
| PROTAC BRD4 Degrader-21 is a PROTAC degrader of BRD4. | ||
| M43433 | PROTAC BRAF-V600E degrader-2 | PROTAC |
| PROTAC BRAF-V600E degrader-2 is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. | ||
| M43434 | PROTAC BRD4 Degrader-16 | PROTAC |
| PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC50 values of 34.58 nM (BRD4 (BD1)) and 40.23 nM (BRD4 (BD2)). | ||
| M43435 | PROTAC BRD4 Degrader-17 | PROTAC |
| PROTAC BRD4 Degrader-17 is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). | ||
| M45098 | CPS2 | PROTAC |
| CPS2 is a first-in-class, highly potent, selective, and irreversible PROTAC CDK2 degrader (IC50= 24 nM) for AML-related studies. | ||
| M49775 | PROTAC STAT3 degrader-2 | PROTAC |
| PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC50 of 3.54 μM in Molm-16 Cell. | ||
| M49777 | PPM-3 | PROTAC |
| PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. | ||
| M54671 | BTX-6654 | PROTAC |
| BTX-6654 is a targeted and specific cerebellar-based bifunctional SOS1 PROTAC degrader.BTX-6654 reduces the downstream signaling markers pERK and pS6 and displays antiproliferative activity in a wide range of KRAS-mutant cells. In two KRAS G12C xenograft models, BTX-6654 degraded SOS1 in a dose-dependent manner correlating with tumor growth inhibition, additionally exhibiting synergy with KRAS and MEK inhibitors. | ||
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