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Results for "

degradation tag

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amyloid-β (1) Apoptosis (1) AUTACs (5) Autophagy (6) Bacterial (1) Deubiquitinase (1) DNA Alkylator/Crosslinker (1) E3 Ligase Ligand-Linker Conjugates (1) EGFR (1) Epigenetic Reader Domain (1) ERK (1) FKBP (3) Histone Methyltransferase (1) Ligands for E3 Ligase (1) Molecular Glues (1) Polo-like Kinase (PLK) (1) PROTAC Linkers (1) PROTACs (6) Proteasome (2) SGK (1) WDR5 (1)
By Research Areas:	Cancer (19) Metabolic Disease (1) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-160695

PT-179	Ligands for E3 Ligase Molecular Glues	Cancer
PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms .

HY-147098

dTAG-47	PROTACs FKBP	Cancer
dTAG-47, heterobifunctional dTAG molecule, targets mutant FKBP12 (FKBP12 ^F36V). FKBP12 ^F36V serves as a degradation tag (dTAG) and is fused to a protein of interest. dTAG-47 can be used for the research of basal-like breast cancers (BBC) .

HY-129652

HaloAUTAC tt15	AUTACs	Cancer
HaloAUTAC tt15 is an autophagy-targeting chimera (AUTAC), that targets the Halo Tag carrying proteins, and degrades via the autophagy mechanism .

HY-141676

HyT36	EGFR	Others
HyT36 is a low molecular weight hydrophobic tag that promotes the degradation of fusion protein and pseudokinase Her3 .

HY-133869

cGMP-HTL cGMP-Halotag-ligand	Autophagy	Cancer
cGMP-HTL contains a HT-ligand, a linker and the Cys-S-cGMP (autophagy tag). cGMP-HTL increases the K63-linked ubiquitination of mitochondria. AUTAC (autophagy-targeting chimera) is a novel targeted-clearance strategy that contains a degradation tag (guanine derivatives) and a warhead to provide target specificity .

HY-134183

AUTAC1	AUTACs Autophagy	Metabolic Disease Cancer
AUTAC1 is a MetAP2-targeting autophagy-mediated degrader (AUTAC). AUTACs contain a degradation tag and a warhead to provide target specificity. AUTAC1 contains an FBnG (p-Fluorobenzyl Guanine) and a Fumagillol moiety. Fumagillol binds covalently to MetAP2 .

HY-149679

PROTAC eDHFR Degrader-2	PROTACs Bacterial	Cancer
PROTAC eDHFR Degrader-2 (compound 7b) is a potent degrader targeting Escherichia coli dihydrofolate reductase (eDHFR), enabling robust degradation of eDHFR-tagged proteins .

HY-163208

VH 032 amide-alkylC9-amine hydrochloride (S,R,S)-AHPC-C9-NH2 hydrochloride	PROTAC Linkers	Others
VH 032 amide-alkylC9-amine hydrochloride (Linker 33) is TRK ligand conjugated to the degradation tag .

HY-170989

BRD4 degrader-5	AUTACs Epigenetic Reader Domain Autophagy	Cancer
BRD4 degrader-5 (Compound 23) is a hydrophobic tag (HyTag)-based protein degrader for BRD4 (DC₅₀ = 24.7 μM) through ER stress and autophagy-lysosome pathway. BRD4 degrader-5 inhibits the proliferation of cancer cell 4T1 with an IC₅₀ of 20.6 μM .

HY-158985

Amino-PEG3-2G degrader-1	AUTACs Autophagy	Cancer
Amino-PEG3-2G degrader-1 (compound ) is a conjugate of a PEG Linker and a pyrazole-linked FBnG tag for ubiquitin-proteasome system (UPS) induction. Amino-PEG3-2G degrader-1 can be used to synthesize autophagy-targeting chimeras (AUTACs) .

HY-23020

Boc3Arg	Proteasome	Cancer
Boc3Arg is the tert-butyl carbamate-protected arginine. Boc3Arg is an efficient tag to induce degradation through directly localizing the protein to the 20S proteasome .

HY-158985A

Amino-PEG3-2G degrader-1 hydrochloride	Autophagy AUTACs	Cancer
Amino-PEG3-2G degrader-1 hydrochloride is the hydrochloride salt form of Amino-PEG3-2G degrader-1 (HY-158985). Amino-PEG3-2G degrader-1 hydrochloride is a conjugate of a PEG Linker and a pyrazole-linked FBnG tag for ubiquitin-proteasome system (UPS) induction. Amino-PEG3-2G degrader-1 hydrochloride can be used to synthesize autophagy-targeting chimeras (AUTACs) .

HY-145752

HaloPROTAC-E 1 Publications Verification	PROTACs SGK Autophagy	Cancer
HaloPROTAC-E is a potent Halo PROTAC degrader that reversibly induces degradation of two Halo-tagged endoplasmic reticulum-localized proteins, SGK3 and VPS34, with a DC₅₀ of 3-10 nM. HaloPROTAC-E significantly and selectively induces degradation of endogenous VPS34 complexes (VPS34, VPS15, Beclin1, and ATG14) labeled with Halo and inhibits autophagy.

HY-145514C

dTAGV-1 hydrochloride 1 Publications Verification	FKBP PROTACs	Cancer
dTAGV-1 hydrochloride is a potent and selective degrader of FKBP12 ^F36V-tagged proteins PROTAC degrader. dTAGV-1 hydrochloride can induce degradation of FKBP12 ^F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A)) .

HY-131890

VH032 amide-PEG1-acid	DNA Alkylator/Crosslinker E3 Ligase Ligand-Linker Conjugates	Cancer
VH032 amide-PEG1-acid (linker 10) is a VHL-1 alkyl linker that can be used to bind CDK4/6 ligands (PI) and degradation/destruction tags (EL) (e.g.,E3 ligase ligands) .

HY-145514

dTAGV-1 TFA 1 Publications Verification	PROTACs FKBP	Cancer
dTAGV-1 TFA is a potent and selective degrader of FKBP12 ^F36V-tagged proteins PROTAC degrader. dTAGV-1 TFA can induce degradation of FKBP12 ^F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A))

HY-172769

CM112	Histone Methyltransferase	Cancer
CM112 is a selective protein arginine methyltransferase 1 (PRMT1) degrader by tethering hydrophobic tag, adamantane, to MS023 with a 5-PEG linker. CM112 induces the degradation of PRMT1 in various solid cancer cell lines. CM112 can also target the nonenzymatic function of PRMT1 by downregulating the stability of the orphan receptor TR3. CM112 is promising for research of cancers .

HY-153738

ERK1/2 inhibitor 9	ERK	Cancer
ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .

HY-129265

Poloxin-2	Polo-like Kinase (PLK)	Cancer
Poloxin-2 is a small molecule Plk1 PBD inhibitor that can effectively induce cell mitotic arrest with an EC50 of approximately 15 μM in HeLa cells. Poloxin-2HT was developed by conjugating a hydrophobic tag (HT) to Poloxin-2, a new application of inhibitors targeting protein-protein interactions. Poloxin-2HT significantly enhanced the effects on cell viability and apoptosis by selectively degrading Plk1 protein, and its effect was stronger than that of untagged Poloxin-2. These data validate hydrophobic tags as a new strategy for targeting and disrupting disease-associated proteins.

HY-P10714

Ub4ix	Proteasome Apoptosis Deubiquitinase	Cancer
Ub4ix is a DUB/26S proteasome inhibitor. Ub4ix can protect K48-linked Ub chains from being chopped up by deubiquitinating enzymes (DUBs) and prevent the proteasomal degradation of Ub-tagged proteins. Ub4ix can reduce the viability of Hela cells and induce apoptosis, with an IC₅₀ value of 1.6 μM .

HY-169389

OICR41114	PROTACs WDR5	Cancer
OICR41114 (PROTAC 4) is a WDR5-targeting PROTAC degrader. OICR41114 degrades endogenous WDR5 with an EC₅₀ and Dmax values of 40 nM and 49%, respectively. OICR41114 degrades HiBiT-tagged WDR5 in a proteasome-dependent manner . OICR41114 is composed of target protein ligand (red part) Dimethyl-F-OICR-9429-COOH (HY-141799), E3 ligase ligand (blue part) OICR-8268-acrylic acid (HY-169390) and PROTAC linker (black part) Amino-PEG9-amine (HY-140210). The conjugate of E3 ligase ligand and linker is OICR-8268-acrylic acid-amino-PEG9-amine (HY-169391).

HY-P1047

β-Sheet Breaker Peptide iAβ5 [Pro18, Asp21] β-Amyloid (17-21)	Amyloid-β	Neurological Disease
β-Sheet Breaker Peptide iAβ5 is an effective brain amyloid-β (Abeta) degrader. Abeta deposits are associated with Alzheimer's disease (AD), and the related toxicity arises from its β-sheet conformation and aggregation. β-Sheet Breaker Peptide iAβ5 can repeatedly induce the degradation of fibrillary amyloid deposits in vivo. Therefore, β-Sheet Breaker Peptide iAβ5 can prevent and/or reverse neuronal contraction caused by Abeta and reduce the range of interleukin IL-1beta positive microglial-like cells around Abeta deposits. β-Sheet Breaker Peptide iAβ5 can reduce the size and/or number of brain amyloid plaques in AD. β-Sheet Breaker Peptide iAβ5 is labeled with a hydrophobic benzyl alcohol (HBA) tag and shows a bright blue color under acidic conditions, which can be used for quantitative determination.

Cat. No.	Product Name

HY-L918

Molecular Glue-like Compound Library	320 compounds
Targeted Protein Degradation (TPD) is a novel and promising approach to drug development. It shows great potential for targeting proteins traditionally considered "undruggable" due to the lack of enzymatic function and absence of binding sites by tagging them for degradation or recruiting natural degradation mechanisms. Molecular glues are a type of small-molecule degraders that primarily induce novel interactions between E3 ubiquitin ligases and target proteins, forming ternary complexes that lead to protein ubiquitination and subsequent proteasomal degradation. Compared with PROTACs, molecular glues generally have lower molecular weights, higher cell permeability, and better drug-like properties. Additionally, the design of molecular glues is relatively simple, without the requirements for complex linkers and ligand optimization. As a result, molecular glues have gradually emerged as a promising therapeutic approach for various diseases. Multiple types of molecular glues have been reported previously. Analysis of co-crystal complex structures reveals that CRBN-related molecular glues are more versatile. Therefore, MCE researchers select active molecules related to these targets as probes for artificial intelligence (AI) screening.Subsequently, molecular docking technology was used to verify whether the screened molecules retained the key pharmacophore features. Ultimately, we obtained 320 molecular glue analogs, and these compounds serve as powerful tools for the research of molecular glues.

Molecular Glue-like Compound Library

320 compounds

Targeted Protein Degradation (TPD) is a novel and promising approach to drug development. It shows great potential for targeting proteins traditionally considered "undruggable" due to the lack of enzymatic function and absence of binding sites by tagging them for degradation or recruiting natural degradation mechanisms.

Molecular glues are a type of small-molecule degraders that primarily induce novel interactions between E3 ubiquitin ligases and target proteins, forming ternary complexes that lead to protein ubiquitination and subsequent proteasomal degradation. Compared with PROTACs, molecular glues generally have lower molecular weights, higher cell permeability, and better drug-like properties. Additionally, the design of molecular glues is relatively simple, without the requirements for complex linkers and ligand optimization. As a result, molecular glues have gradually emerged as a promising therapeutic approach for various diseases.

Multiple types of molecular glues have been reported previously. Analysis of co-crystal complex structures reveals that CRBN-related molecular glues are more versatile. Therefore, MCE researchers select active molecules related to these targets as probes for artificial intelligence (AI) screening.Subsequently, molecular docking technology was used to verify whether the screened molecules retained the key pharmacophore features. Ultimately, we obtained 320 molecular glue analogs, and these compounds serve as powerful tools for the research of molecular glues.

Cat. No.	Product Name	Target	Research Area

HY-P10714

Ub4ix	Proteasome Apoptosis Deubiquitinase	Cancer
Ub4ix is a DUB/26S proteasome inhibitor. Ub4ix can protect K48-linked Ub chains from being chopped up by deubiquitinating enzymes (DUBs) and prevent the proteasomal degradation of Ub-tagged proteins. Ub4ix can reduce the viability of Hela cells and induce apoptosis, with an IC₅₀ value of 1.6 μM .

HY-P1047

β-Sheet Breaker Peptide iAβ5 [Pro18, Asp21] β-Amyloid (17-21)	Amyloid-β	Neurological Disease
β-Sheet Breaker Peptide iAβ5 is an effective brain amyloid-β (Abeta) degrader. Abeta deposits are associated with Alzheimer's disease (AD), and the related toxicity arises from its β-sheet conformation and aggregation. β-Sheet Breaker Peptide iAβ5 can repeatedly induce the degradation of fibrillary amyloid deposits in vivo. Therefore, β-Sheet Breaker Peptide iAβ5 can prevent and/or reverse neuronal contraction caused by Abeta and reduce the range of interleukin IL-1beta positive microglial-like cells around Abeta deposits. β-Sheet Breaker Peptide iAβ5 can reduce the size and/or number of brain amyloid plaques in AD. β-Sheet Breaker Peptide iAβ5 is labeled with a hydrophobic benzyl alcohol (HBA) tag and shows a bright blue color under acidic conditions, which can be used for quantitative determination.

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