ubiquitinated

By Targets:	Apoptosis (1) E1/E2/E3 Enzyme (1) Endogenous Metabolite (1) Keap1-Nrf2 (2) Lipoxygenase (1) Prostaglandin Receptor (1) Proteasome (2)
By Research Areas:	Cancer (5) Inflammation/Immunology (1) Neurological Disease (3)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145879

Nrf2 activator-2	Keap1-Nrf2	Cancer
Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC₅₀ of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells .

HY-144634

DDO-7263	Keap1-Nrf2	Neurological Disease Inflammation/Immunology
DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD) .

HY-113366

Prostaglandin J2 PGJ2	Prostaglandin Receptor Endogenous Metabolite	Neurological Disease
Prostaglandin J2 (PGJ2), an endogenous metabolite of Prostaglandin D2 (PGD2; HY-101988), is a potent PGD2 receptor (DP) agonist with K_is of 0.9 nM and 6.6 nM for hDP and hCRTH2, respectively. Prostaglandin J2 stimulates intracellular cyclic AMP production with an EC₅₀ value of 1.2 nM. Prostaglandin J2 induces oxidative stress and neuronal apoptosis. Prostaglandin J2 induces the accumulation/aggregation of ubiquitinated (Ub) proteins. Prostaglandin J2 is highly neurotoxic and potentially contributes to many neurodegenerative conditions, including Alzheimer's (AD) and Parkinson's diseases (PD) .

HY-153937

Skp2 inhibitor 2	E1/E2/E3 Enzyme	Cancer
Skp2 inhibitor 2 (14f) is an inhibitor of F-box protein S-phase kinase-associated protein 2 (Skp2), with an IC₅₀ value of 10.2 μM (Skp2-Cks1). Skp2 is a part of cullin-RING ligases, which recruits and ubiquitinates substrates, involving in proteolytic and non-proteolytic process .

HY-111790

M3258 1 Publications Verification	Proteasome Apoptosis	Cancer
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC₅₀=3.6 nM) and cellular (IC₅₀=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .

HY-107412

Proteasome inhibitor IX PS-IX; AM114	Proteasome	Cancer
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC₅₀ value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 ^+/+ cells growth inhibitory activity with an IC₅₀ value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity .

HY-158204

CNB-001	Lipoxygenase	Neurological Disease
CNB-001 is a potent 5-lipoxygenase (5-LOX) inhibitor, decreases 5-LOX expression, and increases proteasome activity. CNB-001 also increases eIF2α phosphorylation and HSP90 and ATF4 levels in Alzheimer's disease transgenic mice, and limits the accumulation of soluble Aβ and ubiquitinated aggregated proteins. CNB-001 maintains the expression of synapse-associated proteins and improves memory. CNB-001 can be used for the research of Alzheimer's disease .

HY-164689

Cadmium pyrithione	Others	Cancer
Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .

Cat. No.	Product Name

HY-L151

PROTAC Library	296 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 296 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.

PROTAC Library

296 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 296 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.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113366

Prostaglandin J2 PGJ2	Structural Classification Neurological Disease Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields	Prostaglandin Receptor Endogenous Metabolite
Prostaglandin J2 (PGJ2), an endogenous metabolite of Prostaglandin D2 (PGD2; HY-101988), is a potent PGD2 receptor (DP) agonist with K_is of 0.9 nM and 6.6 nM for hDP and hCRTH2, respectively. Prostaglandin J2 stimulates intracellular cyclic AMP production with an EC₅₀ value of 1.2 nM. Prostaglandin J2 induces oxidative stress and neuronal apoptosis. Prostaglandin J2 induces the accumulation/aggregation of ubiquitinated (Ub) proteins. Prostaglandin J2 is highly neurotoxic and potentially contributes to many neurodegenerative conditions, including Alzheimer's (AD) and Parkinson's diseases (PD) .

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