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Pathways Recommended:	MAPK/ERK Pathway

Results for "

Proteasome pathway

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Proteasome (4) Adrenergic Receptor (1) Amyloid-β (2) Anaplastic lymphoma kinase (ALK) (1) Androgen Receptor (5) AP-1 (1) Apoptosis (17) ASK1 (1) Autophagy (1) Bacterial (3) Bcl-2 Family (4) Bcr-Abl (1) c-Fms (1) c-Kit (1) c-Met/HGFR (1) c-Myc (2) Cadherin (1) Caspase (2) CDK (3) Cholinesterase (ChE) (1) DNA Methyltransferase (1) E1/E2/E3 Enzyme (3) EGFR (4) Epigenetic Reader Domain (1) Epoxide Hydrolase (1) ERK (2) Estrogen Receptor/ERR (3) Ferroptosis (1) FGFR (1) FLT3 (2) Glutathione Peroxidase (1) GSK-3 (1) HDAC (1) Histone Demethylase (1) Histone Methyltransferase (1) HSP (1) IAP (1) IFNAR (1) IGF-1R (1) Isotope-Labeled Compounds (1) JAK (1) JNK (1) Keap1-Nrf2 (1) Ligands for E3 Ligase (5) MDM-2/p53 (2) Mitophagy (1) Molecular Glues (2) NAMPT (1) Necroptosis (1) NF-κB (3) p38 MAPK (1) PD-1/PD-L1 (2) PDGFR (1) PERK (1) Phosphatase (1) Phosphodiesterase (PDE) (1) PROTACs (26) Raf (1) Reactive Oxygen Species (ROS) (1) Reference Standards (1) Ser/Thr Kinase (1) SNIPERs (4) STAT (2) STING (1) Survivin (1) VEGFR (1) Wnt (2) α-synuclein (3) β-catenin (2)
By Research Areas:	Cancer (60) Endocrinology (2) Infection (2) Inflammation/Immunology (7) Metabolic Disease (2) Neurological Disease (6)
Click Chemistry:	PROTAC Synthesis (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

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Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Proteasome Tissue Factor Pathway Inhibitor (TFPI)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-19726

NSC59984 2 Publications Verification	MDM-2/p53	Cancer
NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway . NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling .

HY-144841A

(Rac)-Cemsidomide (Rac)-CFT7455	Molecular Glues	Cancer
(Rac)-Cemsidomide ((Rac)-CFT7455) is the racemate of Cemsidomide (HY-144841) with antitumor activity . Cemsidomide is a ubiquitin ligase pathway Ikaros/Aiolos degrader with molecular glue activity. Cemsidomide has a GI₅₀ of 0.05 nM for NCIH929.1 cells.

HY-P11028

M1-20	CDK	Cancer
M1-20 is a CDK1 inhibitor. M1-20 promotes CDK1 ubiquitination by CUL4-DDB1-DCAF1 complexes and degradation through the proteasome pathway. M1-20 abolishes the formation of CDK1/CCNB1 complexes. M1-20 has significant anticancer activity of spontaneous breast cancer in FVB/N MMTV-PyVT mice model .

HY-143535

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

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-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-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-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-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-141432

NX-1607 Cbl-b-IN-3	E1/E2/E3 Enzyme	Cancer
NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC₅₀ value of less than 1 nM. NX-1607 can be used in cancer research .

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-N7695

Physalin B	Apoptosis Autophagy	Cancer
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .

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-P5819

xStAx-VHLL 1 Publications Verification	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-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-P4910

Baceridin	Proteasome Apoptosis	Cancer
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research .

HY-161180

Antitumor agent-136	NAMPT	Cancer
Antitumor Agent-136 (Compound 17) is a potent broad-spectrum antitumor agent and a NAMPT inhibitor with an IC₅₀ of 9.5 nM. Antitumor Agent-136 can reduce the levels of intracellular and extracellular NAMPT protein through the ubiquitin proteasome pathway, thus achieving tumor inhibition .

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 .

HY-P5819A

xStAx-VHLL TFA 1 Publications Verification	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-174266

WB156	MDM-2/p53	Cancer
WB156 is a dual MDM2 and GSPT1 degrader. WB156 can recruit CRBN (Cereblon, a substrate receptor of the E3 ubiquitin-ligase complex) to induce the ubiquitination-proteasome pathway-mediated degradation of MDM2 and GSPT1. WB156 is promising for research of cancers, such as leukemia .

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 .

HY-145898

WBC100 14-D-Valine-TPL	c-Myc Molecular Glues	Cancer
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 .

HY-172595

Apoptotic agent-5	Apoptosis E1/E2/E3 Enzyme	Cancer
Apoptotic agent-5 (5d) is an apoptotic agent. Apoptotic agent-5 inhibits the growth of triple-negative breast cancer cells. Apoptotic agent-5 attenuates proteasomal degradation via the *ubiquitin-proteasome* pathway, leading to G2/M phase cell cycle arrest and the induction of apoptotic .

HY-157788

ZX703	PROTACs Reactive Oxygen Species (ROS) Ferroptosis Glutathione Peroxidase	Cancer
ZX703 (compound 5I) is a PROTAC that significantly degrades GPX4 in a dose- and time-dependent manner through the ubiquitin-proteasome and autophagy-lysosome pathways (DC₅₀=0.315 µM). ZX703 induces ferroptosis by inducing Reactive Oxygen Species (ROS) accumulation in cells. ZX703 can be used for cancer research .

HY-160864

Torbafylline HWA 448	Phosphodiesterase (PDE)	Cancer
Torbafylline is a PDE inhibitor. Torbafylline mitigates protein breakdown in rat skeletal muscle following burns by activating the PDE4/cAMP/EPAC/PI3K/Akt signaling pathway. Torbafylline suppresses the increased ubiquitin-proteasome-dependent protein degradation observed in the skeletal muscles of rats susceptible to cancer and sepsis .

HY-149127

Rosolutamide ASC-JM17; ALZ-003	Keap1-Nrf2 Androgen Receptor HSP Mitophagy	Metabolic Disease
Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .

HY-147942

MS9449	PROTACs EGFR	Cancer
MS9449 is a potent PROTAC EGFR degrader with K_ds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .

HY-147941

MS9427	PROTACs EGFR	Cancer
MS9427 is a potent PROTAC EGFR degrader with K_ds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .

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 .

HY-147373

DA-PROTAC	PROTACs Ligands for E3 Ligase	Cancer
DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research .

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-147941A

MS9427 TFA	PROTACs EGFR	Cancer
MS9427 TFA is a potent PROTAC EGFR degrader with K_ds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .

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-N4225

Aaptamine 2 Publications Verification	Adrenergic Receptor Proteasome Cholinesterase (ChE) Bacterial Apoptosis AP-1 NF-κB	Infection Neurological Disease Inflammation/Immunology Endocrinology Cancer
Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the *proteasome* and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects .

HY-144323

YF135	PROTACs PERK	Cancer
YF135 is an efficient and reversible-covalent KRAS ^G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS ^G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .

HY-158331

Gal-ARV-771	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
Gal-ARV-771, PROTAC prodrug, is a gal modified ARV-771 (HY-100972). Gal-ARV-771 can be activated in SA-β-Gal-expressed cancer senescent cells to release ARV-771. Gal-ARV-771 induces selective degradation of BRD4 protein by the ubiquitin-proteasome pathway in senescent cells. Gal-ARV-771 promotes apoptosis of senescent cancer cells .

HY-153896

LMTK3-IN-1 1 Publications Verification	c-Met/HGFR	Cancer
LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (K_d=2.5 μM)，that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM .

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-141431

Cbl-b-IN-2	E1/E2/E3 Enzyme	Inflammation/Immunology Cancer
Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent .

HY-155406

Estrogen receptor modulator 10	Estrogen Receptor/ERR Caspase Bcl-2 Family	Cancer
Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC₅₀=6.7 nM) and degrader (DC₅₀=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research .

HY-170951

AR antagonist 10	Androgen Receptor	Cancer
AR antagonist 10 (Compound Y5) is potent and orally active androgen receptor (AR) antagonist with an IC₅₀ of 0.04 μM. AR antagonist 10 demonstrates dual mechanisms of action, antagonizes AR by disrupting AR dimerization, and induces AR degradation via the ubiquitin-proteasome pathway. AR antagonist 10 exhibits excellent activity against variant drug-resistant AR mutants. AR antagonist 10 effectively suppresses the tumor growth of the LNCaP xenograft. AR antagonist 10 is potential to be used for drug-resistant prostate cancer .

HY-158432

GT-653	Histone Demethylase PROTACs	Cancer
GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))

HY-168274

PROTAC TRIB2 degrader-1	PROTACs Apoptosis	Cancer
PROTAC TRIB2 degrader-1 (Compound 5k) is an effective TRIB2 degrader that selectively induces TRIB2 degradation through the CRBN-dependent ubiquitin-proteasome pathway. PROTAC TRIB2 degrader-1 can inhibit cell proliferation and induce cell apoptosis, and can be used in cancer research. (Target protein ligand (Pink): HY-168275; linker (black): HY-168276; E3 Ligase Ligand-Linker Conjugates: HY-168277; E3 ligase (Blue): HY-W023573) .

HY-125834

GMB-475	PROTACs Bcr-Abl Apoptosis STAT JAK	Cancer
GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .

HY-176528

PROTAC ERK5 degrader-1	ERK PROTACs	Cancer
PROTAC ERK5 degrader-1 (compound 2) is a bifunctional ERK5 PROTAC degrader. PROTAC ERK5 degrader-1 induces ERK5 degradation via VHL-mediated proteasome pathway in MOLT-4 cells. PROTAC ERK5 degrader-1 can be used for the study of a disease or disorder characterized by aberrant ERK5 activity (Pink: ERK5 ligand (HY-176529); Blue: VHL ligand (HY-42424); Black: linker (HY-43191); VHL ligand + linker: HY-176530) .

HY-139996

Pomalidomide-C5-Dovitinib	PROTACs Apoptosis FLT3 c-Kit FGFR VEGFR PDGFR c-Fms	Cancer
Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD ⁺ acute myeloid leukemia .

Cat. No.	Product Name

HY-L151

PROTAC Library

386 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 386 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-L050

Ubiquitination Compound Library

365 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 365 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 1 Publications Verification	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-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-P5819A

xStAx-VHLL TFA 1 Publications Verification	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-P11028

M1-20	CDK	Cancer
M1-20 is a CDK1 inhibitor. M1-20 promotes CDK1 ubiquitination by CUL4-DDB1-DCAF1 complexes and degradation through the proteasome pathway. M1-20 abolishes the formation of CDK1/CCNB1 complexes. M1-20 has significant anticancer activity of spontaneous breast cancer in FVB/N MMTV-PyVT mice model .

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-P4910

Baceridin	Proteasome Apoptosis	Cancer
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research .

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	Category	Target	Chemical Structure

HY-N7695

Physalin B	other families Classification of Application Fields Ketones, Aldehydes, Acids Source classification Plants Disease Research Fields Cancer	Apoptosis Autophagy
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .

HY-N4225

Aaptamine 2 Publications Verification	Alkaloids Structural Classification Animals Classification of Application Fields Marine natural products Source classification Quinoline Alkaloids Sponge Disease Research Fields Endocrinology	Adrenergic Receptor Proteasome Cholinesterase (ChE) Bacterial Apoptosis AP-1 NF-κB
Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the *proteasome* and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects .

HY-W010041

Scyllo-Inositol	Structural Classification Natural Products Source classification Endogenous metabolite	α-synuclein Amyloid-β
Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .

HY-N6929

Angelic acid	Structural Classification Ketones, Aldehydes, Acids Source classification Umbelliferae Plants Echinacea angustifolia DC.	Others
Angelic acid is a ferroptosis inducer, targeting NRF2 degradation. Angelic acid binds to NRF2 protein and promotes NRF2 degradation via ubiquitination-proteasome pathway, relieves the inhibitory effect of NRF2 on oxidative stress and lipid peroxidation. Then, Angelic acid induces ferroptosis in tumor cells. Angelic acid can enhance the accumulation of intracellular reactive oxygen species (ROS), upregulate ferroptosis-related markers CHAC1 and PTGS2, and synergize with ferroptosis inducers to enhance anti-tumor effects. Angelic acid also has the activity of scavenging UVA-induced ROS in vitro, inhibiting skin fibroblast senescence and extracellular matrix degradation. Angelic Acid helps wound healing with sedative activity .

HY-N8146

Bruceantinol	Infection Triterpenes Simaroubaceae Classification of Application Fields Brucea antidysenterica J.F.Mill. Terpenoids Source classification Plants Disease Research Fields Brucea javanica (L.) Merr. Cancer	STAT Bcl-2 Family Ser/Thr Kinase Survivin c-Myc Apoptosis Necroptosis CDK
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC₅₀ = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .

HY-N6929R

Angelic acid (Standard)	Structural Classification Ketones, Aldehydes, Acids Source classification Umbelliferae Plants Echinacea angustifolia DC.	Reference Standards Others
Angelic acid (Standard)) is the analytical standard of Angelic acid (HY-N6929). This product is intended for research and analytical applications. Angelic acid is a ferroptosis inducer, targeting NRF2 degradation. Angelic acid binds to NRF2 protein and promotes NRF2 degradation via ubiquitination-proteasome pathway, relieves the inhibitory effect of NRF2 on oxidative stress and lipid peroxidation. Then, Angelic acid induces ferroptosis in tumor cells. Angelic acid can enhance the accumulation of intracellular reactive oxygen species (ROS), upregulate ferroptosis-related markers CHAC1 and PTGS2, and synergize with ferroptosis inducers to enhance anti-tumor effects. Angelic acid also has the activity of scavenging UVA-induced ROS in vitro, inhibiting skin fibroblast senescence and extracellular matrix degradation. Angelic Acid helps wound healing with sedative activity .

Cat. No.	Product Name	Chemical Structure

HY-W707693

Scyllo-Inositol-d6

Scyllo-Inositol-d₆ is the deuterium labeled Scyllo-Inositol (HY-W010041). Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .

Cat. No.	Product Name		Classification

HY-114402

ARD-69		PROTAC Synthesis
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study the treatment of castration-resistant prostate cancer (mCRPC) . ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).

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