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Results for "

proteasome system

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Proteasome (4) Akt (2) Anaplastic lymphoma kinase (ALK) (7) Androgen Receptor (4) Apoptosis (22) ATM/ATR (1) Aurora Kinase (1) AUTACs (2) Autophagy (2) Bcl-2 Family (3) c-Met/HGFR (1) c-Myc (1) Cannabinoid Receptor (1) Casein Kinase (1) Caspase (4) CDK (4) Deubiquitinase (3) DNA/RNA Synthesis (3) DYRK (1) E1/E2/E3 Enzyme (6) EGFR (6) Epigenetic Reader Domain (11) ERK (2) Estrogen Receptor/ERR (2) FAK (1) Fat Mass and Obesity-associated Protein (FTO) (1) FLT3 (1) HDAC (1) Hexokinase (1) Histone Demethylase (1) Histone Methyltransferase (2) HIV (1) HSP (6) HyT (5) IKZF Family (1) Interleukin Related (2) IRAK (2) Isotope-Labeled Compounds (1) JAK (1) JNK (1) Keap1-Nrf2 (1) Ligands for Target Protein for PROTAC (1) MDM-2/p53 (1) Microtubule/Tubulin (1) Molecular Glues (12) mTOR (1) NAMPT (1) NEKs (1) NF-κB (2) Oct3/4 (1) p38 MAPK (2) p97 (1) PARP (6) PD-1/PD-L1 (2) PI3K (1) PROTAC Linkers (11) PROTACs (55) RAD51 (1) Raf (1) Ras (3) Reference Standards (2) RET (1) RIO Kinase (1) SARS-CoV (1) SOS1 (1) Src (1) STAT (7) STING (1) Tau Protein (1) TNF Receptor (1) Virus Protease (1) WDR5 (1) Wnt (1) YAP (1) YTHDF (1) α-synuclein (1) β-catenin (1)
By Research Areas:	Cancer (92) Endocrinology (1) Infection (3) Inflammation/Immunology (16) Metabolic Disease (5) Neurological Disease (9)
Click Chemistry:	PROTAC Synthesis (3) Azide (1) Alkynes (1)

106

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Proteasome Complement System Proteasome Cap Targeting Chimeras

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-106443A

Arimoclomol maleate 5 Publications Verification BRX-220	HSP	Neurological Disease Metabolic Disease Inflammation/Immunology
Arimoclomol maleate (BRX-220) is an orally active co-inducer of heat shock proteins (HSP) . Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system .Arimoclomol maleate can be used for the study of Niemann–Pick disease type C.

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-106443

Arimoclomol 5 Publications Verification BRX-220 free base	HSP	Neurological Disease Metabolic Disease Inflammation/Immunology
Arimoclomol (BRX-220 free base) is an orally active co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.Arimoclomol can be used for the study of Niemann–Pick disease type C. Arimoclomol can cross the blood-brain barrier and can be used in research on Niemann-Pick disease type C .

HY-172162

LC-04-045	Molecular Glues NEKs Interleukin Related	Inflammation/Immunology Cancer
LC-04-045 is a selective NIMA-related kinase 7 (NEK7) molecular glue degrader. LC-04-045 induces NEK7 degradation via the CRBN-based ubiquitin-proteasome system, dependent on the glycine 57-containing degron motif. LC-04-045 inhibits secretion of downstream cytokines IL-1β and IL-18. LC-04-045 can be used for the research of lymphoblastic leukemia .

HY-155008

PROTAC HK2 Degrader-1 2 Publications Verification	PROTACs 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-106443B

Arimoclomol citrate 5 Publications Verification BRX-220 citrate	HSP	Neurological Disease Metabolic Disease Inflammation/Immunology
Arimoclomol citrate (BRX-220 citrate) is an orally active co-inducer of heat shock proteins (HSP) . Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system . Arimoclomol citrate can be used for the study of Niemann–Pick disease type C.

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-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-162250

MS8847	PROTACs Histone Methyltransferase	Cancer
MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC₅₀=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer .

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-150602

20S Proteasome activator 1	Proteasome	Neurological Disease
20S Proteasome activator 1 is a potent 20S proteasome activator with EC₂₀₀ values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases .

HY-162563

AK59	STING	Inflammation/Immunology Cancer
AK59 is a STING degrader that works by leveraging HERC4, a hect domain E3 ligase. AK59 can be used in the study of autoimmune diseases and cancer .

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-163944

LL-K12-18	DNA/RNA Synthesis Molecular Glues CDK Apoptosis RAD51 ATM/ATR PARP	Cancer
LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC₅₀ value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .

HY-158342

PROTAC TEAD degrader-1	PROTACs YAP	Cancer
PROTAC TEAD degrader-1 is a TEAD2 degrader and antiproliferative agent with selective activity toward TEAD2 relative to other TEAD family members. PROTAC TEAD degrader-1 relies on CRBN and the proteasome system for TEAD2 degradation; disruption of CRBN binding attenuates this activity. PROTAC TEAD degrader-1 decreases expression of YAP target genes CYR61 and CTGF. PROTAC TEAD degrader-1 can be used for the research of NF2-deficient cancer .

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-176792

ACBI-4	PROTACs Ras	Cancer
ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader, with K_d values of 141 nM against KRAS ^G12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer .

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-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-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-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-168566

EV206	HSP	Cancer
EV206 is a Hsp70 binder and apoptosis inducer that binds to the N-terminal domain of Hsp70, promotes Hsp70 degradation via the ubiquitin-proteasome system, and reduces Hsp70 protein stability. EV206 induces apoptotic cell death, inhibits colony formation, and downregulates the expression of cancer stem cell-related markers in non-small cell lung cancer cells. EV206 inhibits the growth of H460 xenograft tumors in nude mice and can be used for the research of non-small cell lung cancer .

HY-147007

β-catenin-IN-3 1 Publications Verification	β-catenin Wnt CDK	Cancer
β-catenin-IN-3 (Compound C2) is a selective β-catenin inhibitor. β-catenin-IN-3 binds to allosteric site on the surface of β-catenin with K_D calculated at 54.96 nM. β-catenin-IN-3 selectively inhibits β-catenin via targeting a cryptic allosteric modulation site, lowers its cellular load. β-catenin-IN-3 significantly reduces viability of β-catenin driven cancer cells, and triggers β-catenin degradation via proteasome system in β-catenin-overexpressing cancer cells .

HY-175764

FIP22	PROTACs IRAK NF-κB p38 MAPK TNF Receptor Interleukin Related	Inflammation/Immunology
FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC₅₀ = 3.2 nM; THP-1 cells: DC₅₀ = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC₅₀ = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis (Pink: IRAK4 ligand (HY-175765); Blue: CRBN ligand (HY-W087383); Black: Linker (HY-46871)) .

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-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-171825

SIAIS001	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
SIAIS001 is a CRBN-dependent ALK PROTAC degrader with a DC₅₀ of 3.9 nM. SIAIS001 induces ALK protein degradation via the ubiquitin-proteasome system. SIAIS001 induces G1/S phase cell cycle arrest and inhibits proliferation of cancer cells. SIAIS001 can be used for the research of anaplastic large-cell lymphomas .

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-155552

GSPT1 degrader-1	Apoptosis CDK Caspase	Cancer
GSPT1 degrader-1 is a highly selective degrader targeting GSPT1. GSPT1 degrader-1 induces degradation via the ubiquitin-proteasome system. GSPT1 degrader-1 induces G₀/G₁ phase arrest, apoptosis (apoptosis) and inhibits proliferation in leukemia cells. GSPT1 degrader-1 reduces the levels of CDK6 and Cyclin B1, while increases the levels of activated caspase-3 and caspase-9 in leukemia cells. GSPT1 degrader-1 can be used in leukemia research .

HY-155361

PROTAC BRD9 Degrader-7	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD9 Degrader-7 is an orally active, selective BRD9 PROTAC degrader (DC₅₀ = 1.02 nM). PROTAC BRD9 Degrader-7 mediates BRD9 degradation via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-7 exhibits proliferation inhibitory activity in the MV4-11 cells. PROTAC BRD9 Degrader-7 can be used in the research of acute myeloid leukemia and other related malignancies. (Pink: BI 7271: HY-123616, Blue: 5-Aminothalidomide: HY-W023573, Blue + Black: Thalidomide-5-piperazine: HY-W834174, Black: N,N'-Dimethylpiperazine: HY-W539783) .

HY-161597

PROTAC DYRK2 degrader 1	PROTACs DYRK	Cancer
PROTAC DYRK2 degrader 1 is a DYRK2 PROTAC degrader with DC₅₀ values of 1.607 μM (MDA-MB-231 cells) and 3.265 μM (HeLa cells), respectively. PROTAC DYRK2 degrader 1 induces DYRK2 degradation via the ubiquitin-proteasome system. It is applicable to the research of triple-negative breast cancer and cervical cancer .

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-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 (Blue: JQ-1 (carboxylic acid) (HY-78695), Black: linker (HY-W004640); Pink: E3 ligase ligand, L321 (HY-169359)) .

HY-175453

MRT-23227	Molecular Glues	Neurological Disease Cancer
MRT-23227 is a molecular glue degrader that targets cereblon (CRBN). MRT-23227 forms a ternary complex with CRBN and G3BP2, activating the ubiquitin-proteasome system, leading to G3BP2 degradation. MRT-23227 has potential applications in the research of G3BP2-related cancers (such as breast and lung cancer) and neurodegenerative diseases .

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-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-175885

PROTAC FTO degrader 1	PROTACs Fat Mass and Obesity-associated Protein (FTO) Apoptosis Caspase PARP YTHDF	Cancer
PROTAC FTO degrader 1 is a Fat Mass and Obesity-associated Protein (FTO) PROTAC degrader. PROTAC FTO degrader 1 selectively degrades FTO depending on VHL E3 ligase and ubiquitin-proteasome system. PROTAC FTO degrader 1 can increase m₆A modifications on mRNAs associated with ribosome biogenesis and promote their YTHDF2-mediated decay. PROTAC FTO degrader 1 can inhibit cancer cells proliferation and induce apoptosis. PROTAC FTO degrader 1 can be used for the research of cancer, such as acute myeloid leukemia (AML) . (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))

HY-175025

CH091138	PROTACs Ras Apoptosis	Cancer
CH091138 is a potent and selective KRASG12D PROTAC degrader with DC₅₀s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS ^WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)) .

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-152145

PROTAC SOS1 degrader-3	SOS1 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-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-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-174329

MRT-5702D	Molecular Glues	Neurological Disease Cancer
MRT-5702D is a G3BP2 molecular glue degrader. MRT-5702D forms a CRBN-MRT-5702D-G3BP2 ternary complex to activate the ubiquitin-proteasome system for G3BP2 degradation. MRT-5702D can be used for research of G3BP2-related cancers and neurodegenerative diseases .

HY-175036

YTHu78	PROTACs Histone Demethylase Apoptosis Caspase PARP	Cancer
YTHu78 is a KDM5B PROTAC-type degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 exhibits significant antiproliferative activity against a variety of hematological cancer cell lines and can be used to study hematological cancers. (Pink: KDM5B ligand: (HY-116761); Blue: Thalidomide ligand: (HY-14658), Black + Pink: KDM5B ligand + linker: (HY-175145)) .

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)) .

Cat. No.	Product Name

HY-L151

PROTAC Library

515 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 515 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-L934

CRBN Ligand Library

125 compounds

CRBN, namely cereblon, is the substrate recognition subunit of the E3 ubiquitin ligase complex in the ubiquitin-proteasome system. A CRBN ligand library refers to a collection of numerous fragments that can specifically bind to the CRBN protein.

These ligands are mostly designed based on validated CRBN-binding warheads and modified through AI-driven molecular generation optimization systems. They not only include classic lenalidomide-derived structures but also cover novel non-lenalidomide scaffolds. After drug-likeness filtering, these ligands exhibit structural diversity and favorable druggable properties. They can be further optimized and modified to facilitate the development of novel molecular glue degraders, accelerate the discovery of molecular glues that induce interactions between CRBN and new substrate proteins, and enable the exploration of novel CRBN substrates for identifying previously unknown CRBN-binding proteins.

MCE compiles 125 fragments that can specifically bind to the CRBN protein, with molecular weights ranging from 200 to 500. Compounds developed based on the library ligands target multiple disease targets such as cancer and autoimmune diseases, further advancing the development of Molecular Glues and PROTACs therapeutic agents.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N10332

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 .

Cat. No.	Product Name	Chemical Structure

HY-40178S

NH2-C4-NH-Boc-d8

NH2-C4-NH-Boc-d₈ is the deuterium labeled NH2-C4-NH-Boc (HY-40178). 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 .

Cat. No.	Product Name		Classification