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Results for "

ubiquitin-proteasome system

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Proteasome (2) Akt (1) Apoptosis (4) ATM/ATR (1) AUTACs (2) Autophagy (2) BCL6 (1) c-Met/HGFR (1) CDK (2) Deubiquitinase (3) Dipeptidyl Peptidase (1) E3 Ligase Ligand-Linker Conjugates (1) EGFR (3) Epigenetic Reader Domain (1) FLT3 (1) Hexokinase (1) Histone Methyltransferase (1) Isotope-Labeled Compounds (1) Ligands for Target Protein for PROTAC (1) Molecular Glues (6) NAMPT (1) p97 (1) PGE synthase (1) PROTAC Linkers (10) PROTACs (15) Raf (1) Ras (2) STAT (3) STING (1)
By Research Areas:	Cancer (43) Inflammation/Immunology (2)
Click Chemistry:	DBCO (1) PROTAC Synthesis (2) Azide (1) Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Proteasome Complement System E1/E2/E3 Enzyme

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-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-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-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-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-169358

L134	PROTACs Epigenetic Reader Domain	Cancer
L134 is a potent PROTAC BRD4 degrader with a DC₅₀ value of 7.36 nM. L134 mediates the degradation of BRD4 via the ubiquitin-proteasome system in a DCAF11-dependent manner .

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-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-143883

MS143	PROTACs Akt	Cancer
MS143 is a potent PROTAC AKT degrader (DC₅₀=46 nM and GI₅₀=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth (Pink: AKT ligand (HY-15431); Blue: E3 ligase ligand (HY-125845); Black: linker) .

HY-161696

AN5777	Apoptosis	Cancer
AN5777 is a GSPT1 degrader. AN5777 significantly reduces GSPT1 through the ubiquitin-proteasome system. AN5777 induces G1 block and Apoptosis. AN5777 has antitumor activity .

HY-158105

ARV-393	PROTACs BCL6	Cancer
ARV-393 is an orally active PROTAC that utilizes the ubiquitin-proteasome system to target the degradation of BCL6. ARV-393 consists of ligand conjugates targeting BCL6 and the E3 ligase cereblon, respectively. ARV-393 has DC₅₀ and GI₅₀ values of <1 nM in multiple cell lines of diffuse large B-cell lymphoma (DLBCL) and Burkitt lymphoma (BL). ARV-393 also demonstrated considerable tumor suppressor activity in tumor xenograft models. ARV-393 is being studied to inhibit non-Hodgkin lymphoma.

HY-149228

USP28-IN-2	Deubiquitinase	Cancer
USP28-IN-2 is a USP28 inhibitor (IC₅₀=0.3 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-2 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-2 also decreases the ankyrase-1/2 level in vitro. USP28-IN-2 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .

HY-149229

USP28-IN-3	Deubiquitinase	Cancer
USP28-IN-3 is a USP28 inhibitor (IC₅₀=0.1 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-3 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-3 also decreases the ankyrase-1/2 level in vitro. USP28-IN-3 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .

HY-149230

USP28-IN-4	Deubiquitinase	Cancer
USP28-IN-4 is a USP28 inhibitor (IC₅₀=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-4 also decreases the ankyrase-1/2 level in vitro. USP28-IN-4 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .

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-152261

MS6105	PROTACs	Cancer
MS6105 is an LDH protein hydrolysis-targeted chimera (PROTAC) that effectively degrades LDHA and LDHB in a time- and ubiquitin-proteasome system-dependent manner and has anticancer activity . MS6105 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-162250

MS8847	PROTACs Histone Methyltransferase	Cancer
MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells .

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-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-161828

JWZ-5-13	PROTACs CDK	Cancer
JWZ-5-13 is a potent CDK7 PROTAC degrader that significantly degrades CDK7 via the ubiquitin-proteasome system. JWZ-5-13 has antitumor activity. (Pink: Target protein ligand (HY-161830); Black: linker (HY-Y0925); Blue: E3 ligase ligand (HY-112078)) .

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-130715

tert-Butyl 11-aminoundecanoate	PROTAC Linkers	Cancer
tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate 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 .

HY-129773

Phthalimide-PEG4-PDM-OTBS	PROTAC Linkers	Cancer
Phthalimide-PEG4-PDM-OTBS is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-PDM-OTBS 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 .

HY-129774

Phthalimide-PEG4-MPDM-OH	PROTAC Linkers	Cancer
Phthalimide-PEG4-MPDM-OH is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-MPDM-OH 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 .

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-158325

PROTAC FLT-3 degrader 4	PROTACs FLT3 Apoptosis	Cancer
PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor) .

HY-69220

7-Octynoic acid	PROTAC Linkers	Cancer
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-129772

Phthalimide-PEG3-C2-OTs	PROTAC Linkers	Cancer
Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG3-C2-OTs 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 .

HY-40178

NH2-C4-NH-Boc	PROTAC Linkers	Cancer
NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc 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 .

HY-130618

Boc-C1-PEG3-C4-OH	PROTAC Linkers	Cancer
Boc-C1-PEG3-C4-OH is a PROTAC linker, which refers to the Alkyl/ether composition. Boc-C1-PEG3-C4-OH 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 .

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-156730

KT-333	Molecular Glues STAT	Cancer
KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .

HY-156730B

KT-333 diammonium	Molecular Glues STAT	Cancer
KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .

HY-156730A

KT-333 ammonium	Molecular Glues STAT	Cancer
KT-333 ammonium (Compound A) is a molecular glues that degrades STAT3 protein. KT-333 ammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 ammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 ammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .

HY-130619

Boc-C1-PEG3-C4-OBn	PROTAC Linkers	Cancer
Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). 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 .

HY-155008

PROTAC HK2 Degrader-1 2 Publications Verification	Hexokinase	Cancer
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .

HY-108374

4-Azidobutylamine	PROTAC Linkers	Cancer
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.

HY-141431

Cbl-b-IN-2	E3 Ligase Ligand-Linker Conjugates	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-162331

STING Degrader-1	Molecular Glues STING	Inflammation/Immunology Cancer
STING Degrader-1 (compound 2), a molecular glue, is a potent STING degrader that covalently binds to STING and E3 ligase. STING Degrader-1 exhibits a "hook effect", that degrades 75% STING protein at 10 μM, and degrades ca. 30% STING protein at 30 μM .

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-A0023AS2

Alogliptin-13C,d3 benzoate SYR-322-¹³C,d₃ benzoate	Isotope-Labeled Compounds Dipeptidyl Peptidase	Others
Sulfo DBCO-PEG4-Maleimide TEA is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs .

HY-140307A

Sulfo DBCO-PEG4-Maleimide TEA	PROTAC Linkers	Others
Sulfo DBCO-PEG4-Maleimide TEA is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs . Sulfo DBCO-PEG4-Maleimide (TEA) is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

HY-157764

PROTAC ATR degrader-1	PROTACs ATM/ATR	Cancer
PROTAC ATR degrader-1 (compound ZS-7) is a potent PROTAC degrader of ataxia telangiectasia and Rad3-related (ATR), with DC₅₀ of 0.53 μM. PROTAC ATR degrader-1 plays an importnt role in cancer research .

HY-161173

PROTAC SOS1 degrader-5	PROTACs Ras	Cancer
PROTAC SOS1 degrader-5 (compound 4) is a potent PROTAC SOS1 degrader, with the DC₅₀ of 13 nM. PROTAC SOS1 degrader-5 strongly inhibits NCI-H358 cells proliferation with an IC₅₀ of 5 nM .

HY-110167

TFC 007	PGE synthase Ligands for Target Protein for PROTAC	Cancer
TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC₅₀ value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon) .

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.

Cat. No.	Product Name	Category	Target	Chemical Structure