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HECT E3 ubiquitin ligases 1

" in MedChemExpress (MCE) Product Catalog:

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By Research Areas:	Cancer (2730) Cardiovascular Disease (14) Endocrinology (9) Infection (60) Inflammation/Immunology (125) Metabolic Disease (32) Neurological Disease (54)
Click Chemistry:	ADC Synthesis (6) TCO (18) DBCO (2) PROTAC Synthesis (45) Azide (55) Tetrazine (1) Alkynes (43)
Oligonucleotides:	Pegylated Lipids (2) Cap Analogs (2) Antisense Oligonucleotides (7)

3048

Inhibitors & Agonists

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132

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Oligonucleotides

Targets Recommended: E1/E2/E3 Enzyme Ligands for E3 Ligase E3 Ligase Ligand-Linker Conjugates

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-A0003

Lenalidomide 55+ Cited Publications CC-5013	Ligands for E3 Ligase Molecular Glues Apoptosis	Inflammation/Immunology Cancer
Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a *ligand of ubiquitin* E3 ligase cereblon (CRBN)*, and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin* ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells ^[1] .

HY-N0170

Indole-3-carbinol Maximum Cited Publications 16 Publications Verification Indole-3-methanol	NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite	Cancer
Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of *WWP1* (WW domain-containing ubiquitin E3 ligase 1).

HY-110204

Heclin 3 Publications Verification	E1/E2/E3 Enzyme Akt MyD88	Others
Heclin is a **HECT E3 ubiquitin ligases** inhibitor. Heclin inhibits Smurf2, Nedd4, WWP1 (IC₅₀ values are 6.8, 6.3, 6.9 μM) and can be used for the research of gastric cancer ^[1] .

HY-44432

Navitoclax-piperazine ABT-263-piperazine	Ligands for Target Protein for PROTAC Bcl-2 Family	Cancer
Navitoclax-piperazine (ABT-263-piperazine) is a Navitoclax (HY-10087) analog and BCL-XL inhibitor. Navitoclax-piperazine is the ligand for target protein of PROTAC DT2216 (HY-130604). Navitodax-pperaie and E3 ubiquitin ligase VHL ligand can be used to synthesize PROTAC DT2216 (HY-130604) ^[1].

HY-160525

NVS-VHL720	Molecular Glues	Cancer
NVS-VHL720 is a selective VHL-based cysteine dioxygenase (CDO1) molecular glue degrader. NVS-VHL720 recruits CDO1 to the VHL E3 ligase complex, driving ubiquitin-dependent proteasomal degradation of CDO1. NVS-VHL720 can be used for the research of cancer ^[1].

HY-W015450

D-Ala-D-Ala D-Alanyl-D-alanine; H-D-Ala-D-Ala-OH	Endogenous Metabolite	Others
D-Ala-D-Ala is a bacterial endogenous metabolite. D-Ala-D-Ala constitutes the terminus of the peptide part of the peptidoglycan monomer unit and is involved in the transpeptidation reaction as the substrate. D-Ala-D-Ala is catalyzed by D-Alanine-D-Alanine ligase .

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 ^[1].

HY-49444

EN450	NF-κB Molecular Glues E1/E2/E3 Enzyme	Cancer
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the *E2 ubiquitin* ligase UBE2D*. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase* and proteasome-dependent mechanism ^[1].

HY-130815A

MAK683-C2-acid hydrochloride	Ligands for Target Protein for PROTAC Histone Methyltransferase	Cancer
MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615) ^[1].

HY-134417

NSC2805 1 Publications Verification	E1/E2/E3 Enzyme	Cancer
NSC2805 is a WWP2 ubiquitin ligase inhibitor that can significant inhibit WWP2 activity with an IC₅₀ of 0.38 μM. NSC2805 can be used for the research of cancer ^[1].

HY-10949

SMER3	E1/E2/E3 Enzyme	Cancer
SMER3, a Rapamycin enhancer, is a selective **Skp1-Cullin-F-box (SCF) ^Met30 ubiquitin ligase** inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCF ^Met30 ^[1].

HY-169325

(S)-ACE-OH	Molecular Glues	Cancer
(S)-ACE-OH is a molecular glue with anticancer activity. (S)-ACE-OH promotes nucleoporin degradation and disruption of nucleocytoplasmic trafficking by inducing the interaction between E3 ubiquitin ligase TRIM21 and nucleoporin NUP98 ^[1].

HY-128756

SIAIS178	PROTACs Bcr-Abl	Cancer
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC₅₀ of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity ^[1].

HY-A0003B

Lenalidomide hemihydrate 55+ Cited Publications CC-5013 hemihydrate	Ligands for E3 Ligase Molecular Glues Apoptosis	Cancer
Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a *ligand of ubiquitin* E3 ligase cereblon (CRBN)*, and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin* ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells ^[1] .

HY-W145436

Thalidomide-Piperazine 5-fluoride hydrochloride	E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis	Cancer
Thalidomide-Piperazine 5-fluoride hydrochloride is a derivative of cereblon (CRBN) inhibitor Thalidomide (HY-14658), which can be used as ligands for E3 ubiquitin ligase (Ligands for E3 Ligase) for PROTACs Synthesis ^[1].

HY-43722

Lenalidomide-Br	Ligands for E3 Ligase	Cancer
Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602) ^[1] .

HY-108640A

HLI373 dihydrochloride	MDM-2/p53 Parasite Apoptosis	Infection Cancer
HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents ^[1]. Antimalarial activity .

HY-130683

Lenalidomide-propargyl-C2-NH2 hydrochloride 1 Publications Verification	E3 Ligase Ligand-Linker Conjugates	Cancer
Lenalidomide-propargyl-C2-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a linker. Lenalidomide-propargyl-C2-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312) ^[1]. Lenalidomide-propargyl-C2-NH2 (hydrochloride) 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-174872

Pomalidomide-PEG3-acid	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide-PEG3-acid is a synthetic E3 ubiquitin ligase ligand-linker conjugate that can be used to synthesize PROTACs such as AY-4 (HY-174867) ^[1].

HY-101460

Tz-Thalidomide	E3 Ligase Ligand-Linker Conjugates Drug Derivative	Cancer
Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of *ERK1/2* in cells. Tz-Thalidomide can be used in cancer-related research ^[1].

HY-103436

NSC624206	E1/E2/E3 Enzyme	Cancer
NSC624206 is an inhibitor of **ubiquitin E1 (UBA1), with an IC₅₀** of ~9 μM. NSC624206 specifically blocks ubiquitin-thioester formation (IC₅₀=13 μM) but has no effect on ubiquitin adenylation ^[1].

HY-153178

HECT E3-IN-1	E1/E2/E3 Enzyme	Others
HECT E3-IN-1 (compound 3) is a HECT E3 ligase inhibitor. HECT E3-IN-1 (compound 3) disrupts Ub binding to the noncovalent Ub-binding site of Nedd4-1 ^[1].

HY-156382

SPOP-IN-1	Akt ERK E1/E2/E3 Enzyme	Cancer
SPOP-IN-1 is a selective SPOP E3 ubiquitin ligase inhibitor. SPOP-IN-1 leads to the accumulation of tumor suppressors PTEN and DUSP7 and decreased levels of phosphorylated AKT and ERK in clear-cell renal cell carcinoma ^[1].

HY-149316

Smurf1-IN-1	E1/E2/E3 Enzyme	Cardiovascular Disease
Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC₅₀ of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension ^[1].

HY-123967

RNF5 inhibitor inh-02	E1/E2/E3 Enzyme Atg8/LC3	Inflammation/Immunology
RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 rescues F508del-CFTR function in F508del-CFTR-expressing immortalized cells (CFBE41o⁻, EC₅₀ = 2.6 μM; FRT, EC ₅₀ = 2.2 μM). RNF5 inhibitor inh-02 increases LC3IIB expression and autophagic vacuole number via reducing ATG4B ubiquitylation and promotes cell motility. RNF5 inhibitor inh-02 can be used for the study of cystic fibrosis ^[1].

HY-175358

PROTAC USP7 Degrader-1	PROTACs Deubiquitinase	Cancer
PROTAC USP7 Degrader-1 is a VHL-recruiting PROTAC and USP7 degrader with binding activity to both USP7 and the VHL E3 ubiquitin ligase. PROTAC USP7 Degrader-1 recruits the VHL E3 ligase to mediate the ubiquitination and subsequent proteolytic degradation of USP7 ^[1].

HY-143715

Cereblon inhibitor 1	Ligands for E3 Ligase	Cancer
Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.

HY-W062696

BC-1382	E1/E2/E3 Enzyme	Inflammation/Immunology
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC₅₀≈ 5 nM).Anti-inflammatory activity ^[1].

HY-W877989

BWA-522 intermediate-1	Ligands for E3 Ligase	Cancer
BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7 ^[1].

HY-137340

WH-10417-099	PROTACs Casein Kinase	Cancer
WH-10417-099 is a CRBN-based PROTAC multi-kinase degrader that induces the degradation of the maximum number of unique kinases (over 125 unique kinases, such as CSNK1E and PI3Kγ) simultaneously. WH-10417-099 induces protein degradation via the ubiquitin biotinylation (E-STUB) pathway, exhibits synergistic effects with SB-405483 (HY-W1135319). The E3 ligase ligand and linker of WH-10417-099 can form the conjugate Pomalidomide 4'-PEG5-acid (HY-131647) ^[1] .

HY-128843

PROTAC MDM2 Degrader-4	PROTACs MDM-2/p53 E1/E2/E3 Enzyme	Cancer
PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase .

HY-178873

PROTAC K-Ras Degrader-7	PROTACs Ras Keap1-Nrf2	Cancer
PROTAC K-Ras Degrader-7 is a potent PROTAC K-Ras degrader. PROTAC K-Ras Degrader-7 degrades K-Ras through recruiting the *Keap1* E3 ubiquitin ligase. PROTAC K-Ras Degrader-7 can be used for research in pancreatic and colorectal cancers ^[1].

HY-130815

MAK683-CH2CH2COOH	Histone Methyltransferase Ligands for Target Protein for PROTAC	Cancer
MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615) ^[1].

HY-108640

HLI373	MDM-2/p53 Parasite Apoptosis	Infection Cancer
HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents ^[1]. Antimalarial activity .

HY-153424

PROTAC SMARCA2 degrader-1	Target Protein Ligand-Linker Conjugates	Cancer
PROTAC SMARCA2 degrader-1 (compound ex7) is a BRM2 (SMARCA2) degrader (DC₅₀<0.1 μM). PROTAC SMARCA2 degrader-1 is also an E3 ubiquitin ligase binding linker useful in research of cancers. PROTAC SMARCA2 degrader-1 is a target protein ligand-linker conjugate ^[1].

HY-156499

RNF114 ligand 1	Ligands for E3 Ligase	Others
RNF114 ligand 1 is an E3 Ubiquitin ligase RNF114 ligand ^[1].

HY-133046

VHL Ligand-Linker Conjugates 17	E3 Ligase Ligand-Linker Conjugates	Cancer
VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader ^[1]. VHL Ligand-Linker Conjugates 17 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-W797383

Phthalimidinoglutarimide-6-piperazine	E3 Ligase Ligand-Linker Conjugates	Cancer
Phthalimidinoglutarimide-6-piperazine is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.

HY-P11493

ALAPYIP	Ligands for E3 Ligase	Cancer
ALAPYIP is a ligand for E3 ligase. ALAPYIP recruits the VHL-E3 ubiquitin ligase. ALAPYIP can be used for the synthesis of FPP29 (HY-P11228) ^[1].

HY-168602

NSC-217913	E1/E2/E3 Enzyme	Cancer
NSC-217913 is an inhibitor of *WWP1* with an IC₅₀ value of 158.3 μM ^[1].

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 ^[1].

HY-P10981

ErbB2 peptide	PI3K Ligands for E3 Ligase	Cancer
ErbB2 peptide is a peptide ligand of E3 ubiquitin ligase targeting PI3K for peptide PROTACs ^[1].

HY-144841A

(Rac)-Cemsidomide (Rac)-CFT7455	Molecular Glues	Cancer
(Rac)-Cemsidomide ((Rac)-CFT7455) is the racemate of Cemsidomide (HY-144841) with antitumor activity ^[1]. 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-111878

BzNH-BS	SNIPERs	Cancer
BzNH-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase .

HY-175680

Boc-4-(3-oxobutyl)piperidine-(S,R,S)-AHPC	E3 Ligase Ligand-Linker Conjugates	Cancer
Boc-4-(3-oxobutyl)piperidine-(S,R,S)-AHPC is an *E3 ligase* ligand-linker conjugatecan** be used in the synthesis of PROTAC BRD2 BD1 Degrader-1 (HY-175678) ^[1].

HY-A0003A

Lenalidomide hydrochloride CC-5013 hydrochloride	Ligands for E3 Ligase Molecular Glues	Inflammation/Immunology Cancer
Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a *ligand of ubiquitin* E3 ligase cereblon (CRBN)*, and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin* ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells ^[1] .

HY-W595340

*E3 ubiquitin* ligase binder-1**	Ligands for E3 Ligase	Cancer
E3 ubiquitin ligase binder-1 (compound 11) is a potent E3 ubiquitin ligase binder. E3 ubiquitin ligase binder-1 is a ligand for E3 Ligase .

HY-18327

HLI98C	E1/E2/E3 Enzyme MDM-2/p53	Cancer
HLI98C is a ubiquitin ligase inhibitor. HLI98C inhibits p53 ubiquitylation. HLI98C inhibits HDM2 auto-ubiquitylation ^[1].

HY-171775

CRBN ligand-184	Ligands for E3 Ligase	Cancer
CRBN ligand-184 is a ligand for CRBN-type E3 ubiquitin ligases. CRBN ligand-184 can be used to synthesize PROTAC AU-24118 (HY-163410) ^[1].

HY-49514

VHL Ligand intermediate-1	Ligands for E3 Ligase SOS1	Cancer
VHL Ligand intermediate-1 (intermediate 18a) is an intermediate in the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs ^[1].

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2306

Aclacinomycin A 5 Publications Verification Aclarubicin	Quinones Structural Classification Microorganisms Anthraquinones	Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis ^[1] .

HY-N0170

Indole-3-carbinol Maximum Cited Publications 16 Publications Verification Indole-3-methanol	Alkaloids other families Classification of Application Fields Plants Endogenous metabolite Disease Research Fields Indole Alkaloids Source Classification Cancer	NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite
Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of *WWP1* (WW domain-containing ubiquitin E3 ligase 1).

HY-126752

Ophthalmic acid	Structural Classification Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reactive Oxygen Species (ROS)
Ophthalmic acid is a ubiquitous metabolite and glutathione modulator, with a K_i of 0.95 mM for glyoxalase I. Ophthalmic acid competitively inhibits glyoxalase I, glutathione S-transferase, glutaredoxin, glutamate-cysteine ligase, protein disulfide reductase (glutathione), as well as non-selective cation channels. Ophthalmic acid is applicable in diabetes-related research ^[1] .

HY-W015450

D-Ala-D-Ala D-Alanyl-D-alanine; H-D-Ala-D-Ala-OH	Structural Classification Natural Products Human Gut Microbiota Metabolites Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
D-Ala-D-Ala is a bacterial endogenous metabolite. D-Ala-D-Ala constitutes the terminus of the peptide part of the peptidoglycan monomer unit and is involved in the transpeptidation reaction as the substrate. D-Ala-D-Ala is catalyzed by D-Alanine-D-Alanine ligase .

HY-W013021

Norbornene	Structural Classification Natural Products Mangifera pajang Kosterm. Plants Anacardiaceae Source Classification	Ligands for E3 Ligase
Norbornene is a cycloolefin and building block for synthesis of porous organic polymeric materials via metathesis, addition, and CANAL polymerization. Norbornene can also be used as an E3 ligase ligand for the synthesis of PROTAC, such as PROTAC HyTTD Degrader-1 (HY-181895) ^[1].

HY-N10549

Gigantol 1 Publications Verification	Structural Classification Classification of Application Fields Orchidaceae Other Diseases Phenols Polyphenols Glucosinolates Plants Disease Research Fields Dendrobium nobile Lindl.	Ferroptosis c-Myc Glutathione Peroxidase JNK Reactive Oxygen Species (ROS) GSK-3
Gigantol is an orally active bibenzyl compound. Gigantol targets MYC to promote its ubiquitin-proteasomal degradation and inhibit the growth of lung cancer cells. Gigantol exerts anti-lung cancer activity by inducing ferroptosis (Ferroptosis) via the SLC7A11-GPX4 axis. Gigantol restores the sensitivity of mcr-harboring multidrug-resistant bacteria to colistin. Gigantol ameliorates carbon tetrachloride-induced liver injury by inhibiting the activation of the JNK/cPLA2/12-LOX inflammatory pathway. Gigantol promotes cholesterol metabolism and progesterone biosynthesis in Leydig cells. Gigantol can be used in studies related to diseases such as lung cancer, multidrug-resistant Gram-negative bacterial infections, and acute liver injury ^[1] .

HY-N2306A

Aclacinomycin A hydrochloride Aclarubicin hydrochloride	Quinones Microorganisms Classification of Application Fields Anthraquinones Phenols Polyphenols Disease Research Fields Source Classification Cancer	Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic
Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis ^[1] .

HY-N7695

Physalin B	other families Classification of Application Fields Ketones, Aldehydes, Acids Plants Disease Research Fields Cancer Source Classification	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 ^[1] .

HY-N10159

1-Benzyl-I3C	Structural Classification Natural Products Brassica oleracea L. Plants Brassicaceae Source Classification	E1/E2/E3 Enzyme
1-Benzyl-I3C is a NEDD4-1 inhibitor with significant anticancer activity. 1-Benzyl-I3C can directly inhibit the ubiquitination activity of NEDD4-1 with an IC50 of 12.3μM, which is significantly better than its precursor compound I3C of 284μM. 1-Benzyl-I3C and its analogs showed good effects in inhibiting the proliferation of human melanoma cells, which is roughly related to their potency as NEDD4-1 enzyme inhibitors. By combining in vitro ubiquitination experiments and thermal stability analysis, 1-Benzyl-I3C was shown to be able to bind to the catalytic HECT domain of NEDD4-1 ^[1].

HY-N0170R

Indole-3-carbinol (Standard) Indole-3-methanol (Standard)	Alkaloids Structural Classification other families Plants Endogenous metabolite Indole Alkaloids Source Classification	NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite Reference Standards
Indole-3-carbinol (Standard) is the analytical standard of Indole-3-carbinol. This product is intended for research and analytical applications. Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).

HY-W009993

3,4-Methylenedioxycinnamic acid	Ketones, Aldehydes, Acids Piperaceae Plants Piper nigrum Linn. Source Classification	Parasite
3,4-Methylenedioxycinnamic acid is an inhibitor of the 4-hydroxycinnamoyl-CoA ligase (4CL) with a K_i of 100 μM. 3,4-Methylenedioxycinnamic acid exhibits the K_m value for the substrate ferulic acid of 4CL is 8.4 μM.3,4-Methylenedioxycinnamic acid increases the formation of soluble phenolics in particular of vanillic acid. 3,4-Methylenedioxycinnamic acid demonstrates larvicidal activity ^[1] .

HY-N2306R

Aclacinomycin A (Standard) Aclarubicin (Standard)	Quinones Structural Classification Microorganisms Anthraquinones	Reference Standards Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic
Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis ^[1] .

HY-78004

Bibenzyl s-Diphenylethane; Dibenzyl	Structural Classification Natural Products Orchidaceae Plants Dendrobium nobile Lindl. Source Classification	Drug Intermediate
Bibenzyl (s-Diphenylethane; Dibenzyl) is a compound containing two benzyl groups. Its derivatives possess various activities such as antioxidant, anti-inflammatory, and anti-cancer properties ^[1] .

HY-W015450R

D-Ala-D-Ala (Standard) D-Alanyl-D-alanine (Standard); H-D-Ala-D-Ala-OH (Standard)	Structural Classification Natural Products Human Gut Microbiota Metabolites Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite
D-Ala-D-Ala (Standard) is the analytical standard of D-Ala-D-Ala. This product is intended for research and analytical applications. D-Ala-D-Ala is a bacterial endogenous metabolite. D-Ala-D-Ala constitutes the terminus of the peptide part of the peptidoglycan monomer unit and is involved in the transpeptidation reaction as the substrate. D-Ala-D-Ala is catalyzed by D-Alanine-D-Alanine ligase .

HY-169796

Panepophenanthrin	Natural Products Microorganisms Source Classification	E1/E2/E3 Enzyme
Panepophenanthrin is a compound that can be isolated from the mushroom strain, Panus rudis Fr. IFO 8994. Panepophenanthrin is a ubiquitin-activating enzyme inhibitor ^[1].

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 ^[1].

HY-W009993R

3,4-Methylenedioxycinnamic acid (Standard)	Ketones, Aldehydes, Acids Piperaceae Plants Piper nigrum Linn. Source Classification	Parasite Reference Standards
3,4-Methylenedioxycinnamic acid (Standard) is the analytical standard of 3,4-Methylenedioxycinnamic acid (HY-W009993). This product is intended for research and analytical applications. 3,4-Methylenedioxycinnamic acid is an inhibitor of the 4-hydroxycinnamoyl-CoA ligase (4CL) with a Ki of 100 μM. 3,4-Methylenedioxycinnamic acid exhibits the Km value for the substrate ferulic acid of 4CL is 8.4 μM.3,4-Methylenedioxycinnamic acid increases the formation of soluble phenolics in particular of vanillic acid. 3,4-Methylenedioxycinnamic acid demonstrates larvicidal activity ^[1] .

HY-N12489

Ishophloroglucin A	Structural Classification Marine algae Marine natural products Phenols Polyphenols Source Classification	PI3K Akt
Ishophloroglucin A is an orally active phlorotannin compound found in Ishige okamurae. Ishophloroglucin A can alleviate Dexamethasone (HY-14648)-induced muscle atrophy through muscle protein metabolism. Ishophloroglucin A can improve impaired protein synthesis (PI3K and Akt) or degradation (muscle-specific ubiquitin ligase muscle RING finger and atrogin-1). Ishophloroglucin A can be used for research of muscle atrophy-related diseases ^[1].

Cat. No.	Product Name	Chemical Structure

HY-10984S2

Pomalidomide-d4
Pomalidomide-d₄ is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<

HY-10984S3

Pomalidomide-15N,13C5
Pomalidomide- ¹⁵N, ¹³C₅ is ¹⁵N and ¹³C labeled Pomalidomide (HY-10984). Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.

HY-A0003S

Lenalidomide-d5

Lenalidomide-d₅ is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells ^[1] .

HY-14658S

Thalidomide-d4
Thalidomide-d₄ is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties ^[1] .

HY-10984S1

Pomalidomide-d3
Pomalidomide-d₃ is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors ^[1] .

HY-138642S

Vepdegestrant-d5

Vepdegestrant-d₅ (ARV-471-d₅) is the deuterium labeled Vepdegestrant (HY-138642). Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a DC₅₀ of about 2 nM ^[1].

HY-A0003S2

Lenalidomide-13C5,15N

Lenalidomide- ¹³C₅, ¹⁵N is ¹⁵N and ¹³C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells ^[1] .

HY-10984S

Pomalidomide-d5
Pomalidomide-d₅ is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.

HY-132580S

Tofersen-d27

Tofersen-d₂₇ (BIIB067-d₂₇) is the deuterium labeled Tofersen (HY-132580). Tofersen (BIIB067) is an antisense oligonucleotide and SOD1 mRNA inhibitor with an IC₅₀ of 320 pM. Tofersen mediates RNase H-dependent degradation of SOD1 mRNA to reduce SOD1 protein levels in cerebrospinal fluid and serum. Tofersen downregulates cerebrospinal fluid neurofilament light chain, neurofilament heavy chain, amyloid-beta 1-40, amyloid-beta 1-42, neuropeptide Y, ubiquitin C-terminal hydrolase L1, neuropentraxins 1, 2, R, corticotropin-releasing hormone, IL-15, and serum neurofilament light chain, neurofilament heavy chain. Tofersen can be used for the research of superoxide dismutase 1-associated amyotrophic lateral sclerosis.

HY-A0003S3

Lenalidomide-d4

Lenalidomide-d₄ (CC-5013-d₄) is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells ^[1] .

HY-170126S

9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d3 Maleate
9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d₃ Maleate is the deuterium labeled CRBN ligand-74 (HY-170126). CRBN ligand-74 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.

HY-161447

USP1-IN-8
USP1-IN-8 (Compound 16) is an inhibitor for ubiquitin specific peptidase 1 (USP1) and its cofactor *UAF1, with IC₅₀* ≤50 nM. USP1-IN-8 inhibits proliferation of MDA-MB-436 with IC₅₀ ≤50 nM ^[1].

HY-10984S4

Pomalidomide-13C5
Pomalidomide- ¹³C₅ (CC-4047- ¹³C₅) is ¹³C labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.

HY-10250S1

Triciribine phosphate-d3

Triciribine phosphate-d3 (TCN-P-d3) is a deuterated compound of Triciribine phosphate (TCN-P). TCN-P inhibits adenosine monophosphate (AMP)-activated protein kinase through an allosteric mechanism, affecting the first key step in de novo purine biosynthesis. Triciribine phosphate also inhibits inosine monophosphate dehydrogenase, which is the first key step in guanosine nucleotide synthesis. Triciribine phosphate does not affect ligase activity ^[1].

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 ^[1].

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