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Results for "

Ubiquitin-proteasome system (UPS)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Anaplastic lymphoma kinase (ALK) (1) Androgen Receptor (1) Apoptosis (4) Aurora Kinase (1) AUTACs (2) Autophagy (2) Bcl-2 Family (1) Cannabinoid Receptor (1) EGFR (3) Epigenetic Reader Domain (1) ERK (1) Estrogen Receptor/ERR (1) HyT (2) MDM-2/p53 (1) Molecular Glues (1) mTOR (1) NAMPT (1) p97 (1) PARP (1) PI3K (1) PROTACs (13) Proteasome (2) Raf (1) RIO Kinase (1) Src (1) STAT (2) Tau Protein (1) α-synuclein (1)
By Research Areas:	Cancer (20) Infection (1) Inflammation/Immunology (2) Neurological Disease (1)

By Targets:

Akt (1)

Anaplastic lymphoma kinase (ALK) (1)

Androgen Receptor (1)

Apoptosis (4)

Aurora Kinase (1)

AUTACs (2)

Autophagy (2)

Bcl-2 Family (1)

Cannabinoid Receptor (1)

EGFR (3)

Epigenetic Reader Domain (1)

ERK (1)

Estrogen Receptor/ERR (1)

HyT (2)

MDM-2/p53 (1)

Molecular Glues (1)

mTOR (1)

NAMPT (1)

p97 (1)

PARP (1)

PI3K (1)

PROTACs (13)

Proteasome (2)

Raf (1)

RIO Kinase (1)

Src (1)

STAT (2)

Tau Protein (1)

α-synuclein (1)

By Research Areas:

Cancer (20)

Infection (1)

Inflammation/Immunology (2)

Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Targets Recommended: Complement System

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-157839

PROTAC α-Synuclein/Tau degrader 1	PROTACs α-synuclein Tau Protein	Neurological Disease
PROTAC α-Synuclein/Tau degrader 1 is a blood-brain barrier-penetrant dual PROTAC degrader of α-synuclein (α-Syn) and tau, with DC₅₀ of 1.57 μM and 4.09 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 binds to α-Syn and tau PFF, with K_Ds of 0.47 and 2.78 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 exhibits degradation effect mediated by the ubiquitin-proteasome system (UPS). PROTAC α-Synuclein/Tau degrader 6 can be used for the study of Parkinson’s disease (PD) (Pink: α-Synuclein/Tau ligand (HY-151035); Blue: CRBN ligase ligand (HY-14658); Black: Linker (HY-128803)) .

HY-137487

PROTAC BRAF-V600E degrader-1	PROTACs Raf	Cancer
PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits K_d values 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) and inhibits the growth of melanoma cells . (In the molecular structure, target protein ligand: BI-882370 (HY-107779), red part; E3 ubiquitin enzyme ligand: Pomalidomide (HY-10984), blue part; PROTAC linker: G007-LK (HY-12438), black part.

HY-139606

VCP/p97 inhibitor-1	p97	Cancer
VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC₅₀ of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS) .

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	Inflammation/Immunology 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-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-170574

CQ627	Molecular Glues Apoptosis RIO Kinase	Cancer
CQ627 is a molecular glue targeting the degradation of RIOK2. It effectively induces the degradation of RIOK2 in the MOLT4 leukemia cell line via the ubiquitin-proteasome system (UPS) by recruiting the E3 ubiquitin ligase RNF126, with a DC₅₀ value of 410 nM. CQ627 dose-dependently induces apoptosis in MOLT4 leukemia cells, blocks their cell cycle in the G2/M phase, and exhibits antiproliferative activities in various cancer cell lines. CQ627 also demonstrates in vivo anticancer activity in a MOLT4 xenograft mouse model .

HY-179243

S3D5	PROTACs STAT MDM-2/p53	Cancer
S3D5 is a highly efficient and selective PROTAC degrader targeting STAT3 (KD = 4.35 μM). S3D5 induces degradation of STAT3 in HepG2 cells without significant effects on other STAT proteins. S3D5 exhibits good anti-hepatocellular carcinoma cell proliferation activity, which can be explained by activating the p53 pathway. S3D5 degradation of the STAT3 protein is mediated by the ubiquitin–proteasome system (UPS). S3D5 can be used for the study of hepatocellular carcinoma .

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-179433

PROTAC AR Degrader-12	PROTACs Androgen Receptor Estrogen Receptor/ERR Src	Cancer
PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .

HY-147941A

MS9427 TFA	PROTACs EGFR	Infection Inflammation/Immunology 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-175525

MS44	PROTACs Aurora Kinase	Cancer
MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC₅₀ = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors (Pink: Target protein ligand (HY-175526); Blue: E3 ligand (HY-112078); Black: Linker; E3 ligand + Linker (HY-132938)) .

HY-178176

PROTAC CB1R Degrader-1	PROTACs Cannabinoid Receptor Akt ERK Bcl-2 Family Apoptosis	Cancer
PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC₅₀ of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)) .

HY-176261

DDD2	PROTACs	Cancer
DDD2 is a selective and potent VHL-mediated PROTAC NUDT5 degrader. DDD2 induces robust NUDT5 degradation. DDD2 can be used in cancer research, such as lymphocytic leukemia and osteosarcoma . (Structure Note: Pink: NUDT5 inhibitor (HY-176262); Blue: E3 (HY-125845); Black: linker (HY-W001958))

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-175849

ALK degrader 1	HyT Anaplastic lymphoma kinase (ALK) Apoptosis STAT	Cancer
ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC₅₀ = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research .

HY-N10332

Leptosphaerodione	Proteasome	Cancer
Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent **ubiquitin-proteasome system** (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC₅₀ value of 3.2 μM. Anti-tumor agent .

HY-183555

MS108	PROTACs Epigenetic Reader Domain	Cancer
MS108 is a selective VHL-based eleven-nineteen leukemia protein (ENL) PROTAC degrader with DC₅₀ of 0.6 nM. MS108 recruits VHL E3 ligase to induce ENL degradation in a VHL- and ubiquitin-proteasome system (UPS)-dependent manner. MS108 degrades the ENL paralog AF9, which shares a highly conserved YEATS domain with ENL. MS108 suppresses proliferation of cancer cells .

HY-181460

PARP1 degrader-2	HyT PARP	Cancer
PARP1 degrader-2 (Compound 11e) is a potent, selective PARP1 HYT degrader (DC₅₀: 2.16 μM). PARP1 degrader-2 selectively binds to and degrades PARP1 but not PARP2. PARP1 degrader-2 mediates the degradation of PARP1 via the ubiquitin-proteasome system (UPS). PARP1 degrader-2 exhibits anticancer activity against triple-negative breast cancer and colon cancer (hydrophobic tag: (HY-W022007); PARP1 ligand: (HY-75706); Linker: (HY-W015300)) .

HY-180261

GP262	PROTACs mTOR PI3K Apoptosis	Cancer
GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC₅₀ values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. GP262 induces degradation of p110α and p110γ with a DC₅₀ of 227.4 and 42.23 nM. GP262 efficient modulates the PI3K/AKT/mTOR pathway, achieving degradation through the ubiquitin-proteasome system (UPS). GP262 also exhibits robust antiproliferative activity and induces apoptosis in vitro. GP262 exhibits tumor growth suppression capability and biosafety profile. GP262 can be used for leukemia and triple-negative breast cancer (TNBC) .

Cat. No.	Product Name

HY-L151

PROTAC Library	512 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 512 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

512 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 512 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.

Leptosphaerodione	Quinones Monophenols Microorganisms Classification of Application Fields Phenols Naphthalene Quinones Disease Research Fields Cancer Source Classification	Proteasome
Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent **ubiquitin-proteasome system** (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC₅₀ value of 3.2 μM. Anti-tumor agent .

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