About 24 results found for searched term "ER degrader 6" (0.13 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M43601 | ER degrader 6 | Estrogen Receptor |
| ER degrader 6 is a potent Estrogen Receptor (ER)α degrader. | ||
| M43603 | ERα degrader 6 | Estrogen Receptor |
| ERα degrader 6 is an ERα degrader (KI: 75 nM). | ||
| 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. | ||
| 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. | ||
| 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. | ||
| M29154 | FKBP12 PROTAC dTAG-13 | PROTAC |
| dTAG-13 | ||
| FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12F36V and CRBN, thereby selectively degrading FKBP12F36V. | ||
| 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. | ||
| M29215 | WBC100 | c-Myc |
| 14-D-Valine-TPL | ||
| WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c‐Myc molecule glue degrader. WBC100 is a c‐Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c‐Myc overexpressing tumors research. | ||
| 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). | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| M43517 | ITK degrader 1 | Itk |
| ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). | ||
| 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. | ||
| M54872 | BMS-986365 | Androgen Receptor |
| CC-94676 | ||
| BMS-986365 (CC-94676) is a selective heterobifunctional ligand-directed degrader (LDD) with a dual mechanism-of-action and best-in-class potential, targeting the androgen receptor (AR). In animal models of advanced prostate cancer, BMS-986365 demonstrates on-target activity, degrading AR, suppressing AR signaling, and inhibiting tumor growth. | ||
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