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Results for "

proteasome degradation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Proteasome (9) Akt (1) Androgen Receptor (4) Apoptosis (19) AUTACs (2) Autophagy (2) Bacterial (2) Bcl-2 Family (4) BCL6 (1) Bcr-Abl (2) Btk (1) c-Fms (1) c-Kit (1) c-Met/HGFR (2) c-Myc (1) CaMK (1) Caspase (1) CDK (8) Deubiquitinase (2) DNA Methyltransferase (1) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (1) EGFR (4) Endogenous Metabolite (2) Epigenetic Reader Domain (7) Estrogen Receptor/ERR (6) Ferroptosis (3) FGFR (1) FLT3 (3) Glutaminase (1) Glutathione Peroxidase (1) HDAC (1) Hexokinase (1) Histone Demethylase (1) Histone Methyltransferase (9) HSP (1) IAP (1) IGF-1R (1) Interleukin Related (1) JAK (1) Keap1-Nrf2 (3) Ligands for E3 Ligase (5) Ligands for Target Protein for PROTAC (1) MAP4K (2) MDM-2/p53 (1) Mitophagy (1) Molecular Glues (8) NAMPT (2) NEKs (1) NF-κB (1) p97 (1) PDGFR (1) PERK (1) Phosphatase (2) Phosphodiesterase (PDE) (1) PIN1 (2) PROTAC Linkers (9) PROTACs (56) RAD51 (2) Raf (2) RAR/RXR (1) Ras (2) Reactive Oxygen Species (2) Ribosomal S6 Kinase (RSK) (1) SARS-CoV (1) Ser/Thr Kinase (1) SHP2 (1) SNIPERs (6) STAT (4) STING (1) Target Protein Ligand-Linker Conjugates (1) Tau Protein (1) VEGFR (1) WDR5 (2) Wnt (4) YAP (1) α-synuclein (1) β-catenin (8)
By Research Areas:	Cancer (121) Endocrinology (1) Infection (1) Inflammation/Immunology (7) Metabolic Disease (4) Neurological Disease (5)
Click Chemistry:	PROTAC Synthesis (2) Azide (1) Alkynes (1)

136

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Click Chemistry

Targets Recommended: Proteasome

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W054146

RAMB4 1 Publications Verification	Proteasome	Cancer
RAMB4 is a *ubiquitin-proteasome* system (UPS)-stressor*. RAMB4 inhibits ubiquitin-mediated protein degradation* upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity .

HY-120722

TCH-165 1 Publications Verification	Proteasome	Cancer
TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation .

HY-136242

UT-34	Estrogen Receptor/ERR	Endocrinology Cancer
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC₅₀ values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.

HY-120035

DD1	Proteasome Ribosomal S6 Kinase (RSK) Apoptosis	Cancer
DD1, a *proteasome* inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation .

HY-149964

PROTAC CDK9 degrader-7	CDK	Cancer
PROTAC CDK9 degrader-7 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-7 mediates CDK9 degradation via the proteasome .

HY-155506

NAMPT degrader-3	NAMPT	Cancer
NAMPT degrader-3 (compound C5) is a NAMPT degrader, depending on VHL- and proteasome manner. NAMPT degrader-3 displays cytotoxicity and inhibits A2780 cells proliferation .

HY-152145

PROTAC SOS1 degrader-3	PROTACs Ras	Cancer
PROTAC SOS1 degrader-3 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-3 effectively targeted SOS1 for degradation through the ubiquitin-proteasome system .

HY-169135

PROTAC 20S proteasome subunit β5 degrader 2	PROTACs Proteasome	Cancer
PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader for *20S proteasome* subunit β5, with a DC₅₀** of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 inhibits the proliferation of cancer cell FaDu with IC₅₀ of 0.23 μM. PROTAC 20S proteasome subunit β5 degrader 2 exhibits antitumor efficacy in mice models . (Pink: Ligand for target protein (HY-10227); Blue: Ligand for E3 ligase (HY-103596); Black: Linker (HY-Y1760))

HY-157230

XIAP antagonist 1	IAP	Cancer
XIAP antagonist 1 degrades rather than inhibits XIAP, catalyzing rapid degradation of XIAP through the ubiquitin-proteasome pathway [2].

HY-153582

ML 2-23	PROTACs Bcr-Abl	Cancer
ML 2-23 is a potent PROTAC BCR-ABL degrader. ML 2-23 is selectively degrade BCR-ABL in a proteasome-dependent manner in leukemia cells .

HY-146231

SS47	PROTACs MAP4K	Inflammation/Immunology Cancer
SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy .

HY-169134

PROTAC 20S proteasome subunit β5 degrader 1	PROTACs Apoptosis	Cancer
PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) is a targeted degrader of PROTAC for 20S proteasome subunit β5, with a DC₅₀ value of 0.11 μM in FaDu cells. PROTAC 20S proteasome subunit β5 degrader 1 disrupts the cell cycle, promotes apoptosis, and inhibits cell proliferation and migration in both FaDu and KM3/BTZ cells. PROTAC 20S proteasome subunit β5 degrader 1 can be used to study the resistance of pharyngeal cancer and multiple myeloma to Bortezomib (HY-10227) (Pink: Target protein ligand (HY-10227); Blue: E3 ligase ligand (HY-103596); Black: Linker (HY-169142)) .

HY-143535

HG122	Androgen Receptor	Cancer
HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.

HY-148523

HQ005	Molecular Glues CDK	Cancer
HQ005 is a potent CCNK degrader with an DC₅₀ value of 0.041 µM. HQ005 is a molecular-glue degrader that mediates interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation .

HY-144983

E3 ligase Ligand 22	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 22 (compound 139) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .

HY-144980

E3 ligase Ligand 21	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 21 (compound 2) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .

HY-152154

Nampt degrader-2	PROTACs NAMPT	Cancer
Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC₅₀ of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD ⁺ and exerts potent antitumor activities .

HY-W940797

Thalidomide-O-amido-C7-NH2	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-O-amido-C7-NH2 is a E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACT .

HY-144985

E3 ligase Ligand 23	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .

HY-149963

PROTAC CDK9 degrader-6	CDK	Cancer
PROTAC CDK9 degrader-6 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-6 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-6 degrades CDK9 with DC₅₀s of 0.10 μM and 0.14 μM for the CDK9₄₂ and CDK9₅₅ isoforms, respectively .

HY-149962

PROTAC CDK9 degrader-5	PROTACs CDK	Cancer
PROTAC CDK9 degrader-5 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-5 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-5 degrades CDK9 with DC₅₀s of 0.10 μM and 0.14 μM for the CDK9₄₂ and CDK9₅₅ isoforms, respectively .

HY-155643

PROTAC TG2 degrader-1	PROTACs Glutaminase	Cancer
PROTAC TG2 degrader-1 (compound 11) is a von Hippel-Lindau (VHL)-based PROTAC targeting tissue transglutaminase (TG2) with a K_D of 68.9 μM. PROTAC TG2 degrader-1 reduces TG2 in ovarian cancer cells in a proteasome-dependent manner .

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-155552

GSPT1 degrader-1	Molecular Glues Apoptosis	Cancer
GSPT1 degrader-1 (compound 9q) is a potent degrader of G1 to S phase transition 1 (GSPT1) via ubiquitin-proteasome system, serves as one of Molecular Glues. GSPT1 degrader-1 also induces cell G0/G1 phase arrest and apoptosis .

HY-P1259

PR-39	Proteasome Bacterial	Inflammation/Immunology
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric *proteasome* inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-P1259A

PR-39 TFA	Proteasome Bacterial	Inflammation/Immunology
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric *proteasome* inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-152134

HDAC6 degrader-3	HDAC PROTACs	Cancer
HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC₅₀ value of 19.4 nM. HDAC6 degrader-3 has IC₅₀s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin .

HY-168099

ERα degrader 10	Estrogen Receptor/ERR	Cancer
ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC₅₀ of 24.0 nM) and degradation ability (EC₅₀ of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer .

HY-W039233

Lenalidomide-F	Ligands for E3 Ligase	Cancer
Lenalidomide-F is a E3 ligase ligand for LWY713. LWY713 is a PROTAC-class FLT3 degrader (DC₅₀ = 0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways .

HY-163019

EN884	Target Protein Ligand-Linker Conjugates Epigenetic Reader Domain	Metabolic Disease
EN884 is a BRD4 degrader via a SKP1- and proteasome-dependent manner. EN884 can be used in synthetic proteolysis targeting chimeras (PROTACs) .

HY-162679

c-Met degrader-1	c-Met/HGFR Apoptosis	Cancer
c-Met degrader-1 (Compound H11) is an orally active c-Met degrader (through the ubiquitin proteasome system). c-Met degrader-1 has anti-hepatocellular carcinoma activity (HCC) and inhibits tumor growth in MHCC97H xenografts. c-Met degrader-1 inhibits HCC cell growth, arrests cell cycle, and induces apoptosis. c-Met degrader-1 may overcome resistance to type Ib inhibitors .

HY-164895

PIN1 degrader-1	PIN1	Cancer
PIN1 degrader-1 (Compound 158H9) is the inhibitor for proline cis trans isomerase (Pin1) with an IC₅₀ of 21.5 nM. PIN1 degrader-1 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation. PIN1 degrader-1 inhibits the cell viability of multi cancer cells, and can be used in cancer research .

HY-158105

ARV-393	PROTACs BCL6	Cancer
ARV-393 is a potent and orally active BCL6 PROTAC degrader. ARV-393 induces ubiquitination of BCL6 and its subsequent degradation by the proteasome. ARV-393 has the potential for the research of advanced non-hodgkin lymphoma .

HY-P5819

xStAx-VHLL	Wnt PROTACs β-catenin	Cancer
xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity .

HY-156152A

CARM1 degrader-1 hydrochloride	Histone Methyltransferase PROTACs	Cancer
CARM1 degrader-1 hydrochloride is the hydrochloride salt form of CARM1 degrader-1 (HY-156152). CARM1 degrader-1 hydrochloride is a PROTAC degrader for co-activator associated argininemethyltransferase 1 (CARM1), which degrades CARM1 in a VHL- and proteasome-dependent manner with a DC₅₀ of 8.1 nM. CARM1 degrader-1 hydrochloride inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, and thus inhibits breast cancer cell migration .

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-156153

CARM1 degrader-2	Histone Methyltransferase	Cancer
PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC₅₀=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .

HY-156152

CARM1 degrader-1	Histone Methyltransferase	Cancer
PROTAC CARM1 degrader-1 (compound 3b) is a degrader (DC₅₀=8.1 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-1 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .

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-111876A

SNIPER(TACC3)-1 hydrochloride	SNIPERs	Cancer
SNIPERTACC3-1 hydrochloride targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPERTACC3-1 hydrochloride induces cancer cell death .

HY-141797

MS33	Histone Methyltransferase PROTACs WDR5	Cancer
MS33 is a potent WDR5 degrader, with K_ds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia .

HY-137487

PROTAC BRAF-V600E degrader-1	PROTACs Raf	Cancer
PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with K_d value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth .

HY-161719

NF764	β-catenin	Cancer
NF764 is a potent β-catenin (CTNNB1) degrader. NF764 reduces CTNNB1 protein levels in a proteasome-dependent manner. NF764 can be used in the study of cancer .

HY-P5819A

xStAx-VHLL TFA	PROTACs β-catenin Wnt	Cancer
xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity .

HY-158048

UNC9036	PROTACs STING	Inflammation/Immunology
UNC9036 is a PROTAC-based STING degrader, with a DC₅₀ of 227 nM. UNC9036-mediated STING degradation is proteasome and VHL dependent (Structure Note: Red, STING agonist diABZI (HY-112921A); Blue, VHL ligand VH032 (HY-120217); Black, linker) .

HY-111876

SNIPER(TACC3)-1	SNIPERs	Cancer
SNIPER(TACC3)-1 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-1 induces cancer cell death .

HY-111877

SNIPER(TACC3)-2	SNIPERs	Cancer
SNIPER(TACC3)-2 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-2 induces cancer cell death .

HY-111877A

SNIPER(TACC3)-2 hydrochloride	SNIPERs	Cancer
SNIPER(TACC3)-2 hydrochloride targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-2 hydrochloride induces cancer cell death .

HY-163815

CDK2 degrader 2	PROTACs CDK	Others
CDK2 degrader 2 is a PROTAC class CDK2 degrader. The CDK2 binding moiety (CBM) binds to the CDK2 protein and subsequently undergoes ubiquitination, leading to the degradation of CDK2 through the ubiquitin proteasome pathway (UPP). CDK2 degrader 2 can cause degradation of CDK2 in MKN1 cells, with a DC₅₀ value less than 100 nM and an average D_max value greater than 75%. (Red: CBM; Blue: DIM; Black: linker)

HY-173002

MS9024	DNA Methyltransferase	Cancer
MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC₅₀ of 35 nM (DC₅₀ in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC₅₀ of 0.43 μM .

Cat. No.	Product Name

HY-L151

PROTAC Library

340 compounds

PROTACs (Proteolysis-targeting chimeras) is a class of molecules that utilize ubiquitin-proteasome system (UPS) to ubiquitinate and degrade target proteins. The PROTACs molecule consists of two ligands joined by a linker. The one-to-one interaction between PROTACs and target proteins determines the high efficiency of PROTACs, making it a potential molecule for targeted protein degradation (TPD) therapy.

MCE supplies a unique collection of 340 PROTACs that effectively degrade target proteins with more powerful screening capability. MCE PROTAC Library is a useful tool for signal pathway research, protein degradation therapy research, drug discovery and drug repurposing, etc.

HY-L137

Molecular Glue Compound Library

55 compounds

Targeted protein degradation(TPD) is a novel and promising approach to new drug discovery and development. It shows great potential for treating diseases with “undruggable” pathogenic protein targets and for overcoming drug resistance. Molecular glues and PROTACs are both targeted protein degraders that have attracted the most attention.

Molecular glues are small molecular degraders that mainly induce novel interaction between an E3 ligase and a target protein to form a ternary complex, leading to protein ubiquitination and subsequent proteasome degradation. Compared with PROTACs, molecular glues generally possess more favorable drug-like properties, such as lower MW, higher cell permeability, and better oral absorption. Molecular glues are emerging as a promising new therapeutic strategy.

MCE supplies a unique collection of 55 molecular glues which target various proteins. MCE Molecular Glue Compound Library is a useful tool to conduct scientific research and disease mechanism study.

HY-L129

Target Protein Ligand Library

54 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 54 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

HY-L128

E3 Ligase Ligand Library

65 compounds

Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).

MCE carefully prepared a unique collection of 65 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

HY-L050

Ubiquitination Compound Library

319 compounds

Protein ubiquitination is an enzymatic post-translational modification in which an ubiquitin protein is attached to a substrate protein. Ubiquitination involves three main steps: activation, conjugation, and ligation, performed by ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s), and ubiquitin ligases (E3s), respectively. Ubiquitination affects cellular processes such as apoptosis, cell cycle, DNA damage repair, and membrane transportation, etc. by regulating the degradation of proteins (via the proteasome and lysosome), altering the cellular localization of proteins, affecting proteins activity, and promoting or preventing protein-protein interactions. Deregulation of ubiquitin pathway leads to many diseases such as neurodegeneration, cancer, infection and immunity, etc.

MCE offers a unique collection of 319 small molecule modulators with biological activity used for ubiquitination research. Compounds in this library target the key enzymes in ubiquitin pathway. MCE Ubiquitination Compound Library is a useful tool for the research of ubiquitination regulation and the corresponding diseases.

Cat. No.	Product Name	Target	Research Area

HY-P1259A

PR-39 TFA	Proteasome Bacterial	Inflammation/Immunology
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric *proteasome* inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-P5819

xStAx-VHLL	Wnt PROTACs β-catenin	Cancer
xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity .

HY-P5819A

xStAx-VHLL TFA	PROTACs β-catenin Wnt	Cancer
xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity .

HY-P10438

Tat-braftide	Raf	Cancer
Tat-braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by Tat-braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers .

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-P1259

PR-39	Proteasome Bacterial	Inflammation/Immunology
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric *proteasome* inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-P10360

Tat-βsyn-degron	α-synuclein	Neurological Disease
Tat-βsyn-degron is an α-synuclein knockdown peptide that effectively degrades α-synuclein protein via the proteasome pathway. Tat-βsyn-degron effectively reduces α-synuclein protein levels in primary rat cortical neuron cultures. In a Parkinson's mouse toxicity model, Tat-βsyn-degron can alleviate parkinsonian toxin-induced neuronal damage and movement disorders .

Cat. No.	Product Name	Target	Research Area

HY-P99672

Istiratumab MM 141; MM-005	IGF-1R EGFR	Cancer
Istiratumab (M-6495) is bispecific monoclonal antibody targeting IGF-1R and ErbB3. Istiratumab induces IGF-1R and ErbB3 receptor degradation through the proteasome pathway Istiratumab can be used for research of cancers .

Cat. No.	Product Name		Classification

HY-69220

7-Octynoic acid		PROTAC Synthesis Alkynes
7-Octynoic acid (compound 42) is a PROTAC linker and can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins . 7-Octynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-108374

4-Azidobutylamine		Azide PROTAC Synthesis
4-Azidobutylamine is a PROTAC linker, which refers to the alkyl chain composition. 4-Azidobutylamine can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins . 4-Azidobutylamine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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