PROTACs
PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.
Alle PROTACs Isoform-spezifische Produkte anzeigen
All Product Categories
-
PROTACs Verwandte Produkte (1334)
Verwandte Produkte (1334)
-
Antibodies (1)
-
PROTACs Isoform Comparison
-
PROTAC NAMPT Degrader-28
0 ImagesArt. -Nr.: HY-181880PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research.
-
DeDPP4
0 ImagesArt. -Nr.: HY-182336DeDPP4 is a DPP-4 PROTAC degrader. DeDPP4 induces sustained elevation of glucagon-like peptide-1 (GLP-1), enhances glucose tolerance, causes persistent reduction of blood glucose, and achieves long-term blood glucose regulation in animal models of type 2 diabetes. DeDPP4 mediates dose-dependent DPP-4 depletion in cancer cells, and also targets and degrades DPP-4 in the liver and adipose tissues of animal models with type 2 diabetes. DeDPP4 can be used for the research of type 2 diabetes and non-small cell lung cancer.
-
PROTAC BRD3/BRD4-L degrader-2
0 ImagesArt. -Nr.: HY-149948PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer.
-
PROTAC SMARCA2 degrader-26
0 ImagesArt. -Nr.: HY-169278CAS. Nr.: 2760247-27-4PROTAC SMARCA2 degrader-26 (compound 45) is a potent SMARCA2 PROTAC degrader. PROTAC SMARCA2 degrader-26 induces SMARCA2 and SMARCA4 degradation in VCaP cells with the percent degradation of 94% and 57% for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2 degrader-26 shows antiproliferative activity.
-
SMD-1087
0 ImagesArt. -Nr.: HY-170828CAS. Nr.: 3033586-04-5SMD-1087 is a PROTAC that selectively targets SMARCA2 (DC50=8 nM, Dmax=89%) and SMARCA4 with a DC50 of 1 μM. SMD-1087 consists of the E3 ligase ligand (S,R,S)-AHPC-Me (blue part) (HY-112078), the target protein ligand SMI-1074 (red part) (HY-170817), and the PROTAC linker (1r,4r)-tert-Butyl 4-(bromomethyl)cyclohexanecarboxylate (black part) (HY-W890392). Among them, its target protein ligand + Linker part corresponds to SMARCA2 Ligand-Linker Conjugate-1 (HY-170829).
-
MA191
0 ImagesArt. -Nr.: HY-175273MA191 is a FLT3 PROTAC degrader. MA191 abrogates FLT3 inhibitor resistance from rebound activation of mitogen-activated kinases. MA191 mediates rapid FLT3-ITD degradation through a mechanism requiring VHL, neddylation, and BIM. MA191 reduces FLT3-ITD levels before inducing apoptosis. MA191 halts AML cell proliferation in Danio rerio. MA191 can be used for the study of acute myeloid leukemia (AML) (Pink: FLT3 ligand: (HY-175311), Blue: E3 ligase CRBN Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175312)).
-
10-SLF
0 ImagesArt. -Nr.: HY-173082CAS. Nr.: 2765058-89-510-SLF is a PROTAC FKBP12 degrader. 10-SLF induces a ternary complex between FKBP12 and FBXW7-R465C, and promotes FBXW7-R465C-dependent proteasomal degradation of FKBP12. 10-SLF selectively reduces FKBP12 levels in cells expressing FBXW7-R465C.
-
PROTAC AR-NTD degrader 1
0 ImagesArt. -Nr.: HY-149434CAS. Nr.: 3032601-92-3PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively.
-
PROTAC SMARCA2/4 degrader-31
0 ImagesArt. -Nr.: HY-162744CAS. Nr.: 2568273-83-4PROTAC SMARCA2/4-degrader-31 (Compound I-280) is a degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-31 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM.
-
YT117R
0 ImagesArt. -Nr.: HY-169148YT117R is a PROTAC degrader targeting BRD4. YT117R binds stereoselectively and site-specifically to the cysteine residue C1113 of DCAF1 to form a covalent interaction. YT117R promotes BRD4 degradation via a DCAF1-dependent, proteasome- and cullin-RING E3 ligase-mediated process. YT117R exhibits stereoselective activity dependent on wild-type DCAF1, which is blocked by the DCAF1C1113A mutation.
-
PROTAC SMARCA2 degrader-12
0 ImagesArt. -Nr.: HY-163874CAS. Nr.: 2568277-42-7SMARCA2 degrader-13 (compound I-406) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment.
-
PROTAC ER Degrader-15
0 ImagesArt. -Nr.: HY-170332PROTAC ER Degrader-15 (Compound 40) is an orally active degrader of the estrogen receptor (ER) with anticancer activity，which can be used in breast cancer research (Pink: Target Protein Ligand (HY-170334); Black: Linker (HY-30756); Blue: E3 Ligase Ligand (HY-138793); E3 Ligase Ligand-Linker Conjugate (HY-169979)).
-
PROTAC ER Degrader-16
0 ImagesArt. -Nr.: HY-183804CAS. Nr.: 2847829-86-9
-
PROTAC ERα Degrader-10
0 ImagesArt. -Nr.: HY-170336CAS. Nr.: 2421260-43-5PROTAC ERα Degrader-10 is an orally active estrogen receptor α (ERα) PROTAC degrader, with DC50 values of 0.37, 1.1, and 0.47 nM in MCF7, T47D, and CAMA-1 cells, respectively. PROTAC ERα Degrader-10 exhibits significant anti-tumor activity both in vitro and in vivo, and can be used for breast cancer research.
-
PROTAC AURKA degrader 1
0 ImagesArt. -Nr.: HY-175830PROTAC AURKA degrader 1 (Compound A16 + X7) is a Aurora kinase A (AURKA) PROTAC degrader. PROTAC AURKA degrader 1 can be used for cancers research. Pink: AURKA ligand (HY-175827); Blue: CRBN ligase ligand (HY-W867704); Black: linker (HY-132208)
-
PROTAC BRD4 Degrader-6
0 ImagesArt. -Nr.: HY-131203CAS. Nr.: 2410947-56-5PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research.
