About 30 results found for searched term "PROTAC" (0.03 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M10379 | BSJ-03-123 | PROTAC |
| PROTAC CDK6 Degrader | ||
| BSJ-03-123 is a novel, potent CDK6-selective small-molecule degrader (PROTAC). | ||
| M10382 | PROTAC SGK3 degrader-1 | PROTAC |
| SGK3-PROTAC1 | ||
| PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a potent SGK3 degrader, it is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3. | ||
| 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. | ||
| M10384 | Homo-PROTAC pVHL30 degrader 1 | PROTAC |
| CM11 VHL inhibitor | ||
| Homo-PROTAC pVHL30 degrader 1 is a pVHL30 degrader based on PROTAC and a potent VHL inhibitor. | ||
| M14871 | Gefitinib-based PROTAC 3 | PROTAC |
| Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively. | ||
| M14873 | PROTAC BET Degrader-1 | PROTAC |
| PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration. | ||
| M14874 | PROTAC BET degrader-2 | PROTAC |
| PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression. | ||
| 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. | ||
| M21231 | PROTAC CDK9 Degrader-1 | PROTAC |
| PROTAC CDK9 Degrader-1 is a PROTAC linked by Cereblon ligand and CDK ligand and is a selective CDK9 degrader. | ||
| 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. | ||
| 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). | ||
| M28867 | VH032-PEG5-C6-Cl | PROTAC |
| HaloPROTAC 2 | ||
| VH032-PEG5-C6-Cl (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. VH032-PEG5-C6-Cl incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays. | ||
| M28878 | PROTAC RIPK degrader-2 | PROTAC |
| PROTAC RIPK degrader-2 is a nonpeptidic PROTAC based on von Hippel-Lindau ligand which potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation. | ||
| 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. | ||
| 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. | ||
| M29496 | PROTAC ERRα Degrader-1 | PROTAC |
| PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader. | ||
| M29501 | PROTAC BRD4 Degrader-3 | PROTAC |
| PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for von Hippel-Lindau and BRD4. | ||
| M29528 | PROTAC CRBN Degrader-1 | PROTAC |
| PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader. | ||
| 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. | ||
| M29542 | HaloPROTAC-E | SGK |
| HaloPROTAC-E is a novel HaloPROTAC potent degrader, inducing reversible degradation of two endosomally localized proteins, SGK3 and VPS34, with a DC50 of 3-10 nM, remarkably selective inducing only degradation of the Halo tagged endogenous VPS34 complex (VPS34, VPS15, Beclin1, and ATG14). | ||
| 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. | ||
| M29577 | PROTAC Bcl2 degrader-1 | PROTAC |
| PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1. | ||
| M29635 | PROTAC IRAK4 degrader-7 | PROTAC |
| KT-474; SAR444656 | ||
| PROTAC IRAK4 degrader-7 (Compound I-417) is a potentially first-in-class, orally active PROTAC IRAK4 degrader with antitumor activity for studies related to hidradenitis suppurativa (HS) and atopic dermatitis (AD). | ||
| M29649 | PROTAC PD-1/PD-L1 degrader-1 | PROTAC |
| PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner. | ||
| 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. | ||
| 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). | ||
| 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. | ||
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