cullin

By Targets:	Androgen Receptor (1) Apoptosis (7) Autophagy (3) E1/E2/E3 Enzyme (8) Epigenetic Reader Domain (1) Histone Acetyltransferase (1) Ligands for E3 Ligase (3) Molecular Glues (2) NEDD8-activating Enzyme (2) NF-κB (1) Progesterone Receptor (1) PROTACs (3) Reactive Oxygen Species (1) TGF-beta/Smad (1)
By Research Areas:	Cancer (14) Cardiovascular Disease (3) Inflammation/Immunology (3)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 .

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 .

HY-145733

DI-1859	E1/E2/E3 Enzyme	Cardiovascular Disease
DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage .

HY-160799

HA-9104	E1/E2/E3 Enzyme Apoptosis	Cancer
HA-9104 is a potent and selective inhibitor of cullin-5 neddylation via virtually targeting the V30 pocket of UBE2F. HA-9104 binds to UBE2F, reduces its protein levels, and consequently inhibits cullin-5 neddylation. HA-9104 has potent growth suppression and radiosensitizing activities via targeting the UBE2F-CRL5 axis and causing DNA damage, leading to induction of apoptosis and G2/M arrest in lung and pancreatic cancer cells .

HY-14658

Thalidomide 10+ Cited Publications	Ligands for E3 Ligase Autophagy Apoptosis	Inflammation/Immunology Cancer
Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a K_d of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.

HY-14658S

Thalidomide-d4	Molecular Glues Ligands for E3 Ligase Autophagy Apoptosis	Inflammation/Immunology Cancer
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][2].

HY-124602

DI-591	E1/E2/E3 Enzyme	Cancer
DI-591 is a potent, high-affinity and cell-permeable inhibitor of the DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with K_i values of 12 nM and 10.4 nM, respectively and has no appreciable binding to DCN3, DCN4, and DCN5 proteins. DI-591 selectively inhibits neddylation of cullin 3 but has no or minimal effect on neddylation of other cullin family members .

HY-169026

DCN1-IN-2	TGF-beta/Smad	Cardiovascular Disease
DCN1-IN-2 is a DCN1 inhibitor with an IC₅₀ value of 2.96 nM. DCN1-IN-2 can alleviate Ang II/TGFβ-induced activation of cardiac fibroblasts. DCN1-IN-2 can reduce ISO-induced cardiac fibrosis and remodeling in mice by selectively inhibiting cullin 3 .

HY-163524

NAE-IN-2	Apoptosis	Cancer
NAE-IN-2 (compound III-26) is N2–(1-benzylpiperidin-4-yl)quinazoline-2,4-diamine derivative, and inhibits Cullin1 and Cullin3. NAE-IN-2 inhibits migration and induces cell apoptosis of gastric cancer cells .

HY-14658R

Thalidomide (Standard)	Ligands for E3 Ligase Autophagy Apoptosis	Inflammation/Immunology Cancer
Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a K_d of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.

HY-122874

DI-404	E1/E2/E3 Enzyme	Cardiovascular Disease
DI-404 is a potent inhibitor of DCN1 with a KK_d value of 6.7 nM. DI-404 selectively inhibits neddylation of cullin 3 in a dose-dependent manner .

HY-111505

NAcM-OPT 1 Publications Verification	E1/E2/E3 Enzyme NEDD8-activating Enzyme	Cancer
NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction .

HY-161268

NAE-IN-1	Apoptosis NEDD8-activating Enzyme Reactive Oxygen Species	Cancer
NAE-IN-1 (compound X-10) is a potent NAE1 inhibitor. NAE-IN-1 induces apoptosis and cell cycle arrest at the G2/M phase. NAE-IN-1 increases ROS levels and prevents cell migration. NAE-IN-1 shows anti-proliferation activity .

HY-153937

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

HY-139659

ARD-61	PROTACs Androgen Receptor Progesterone Receptor Apoptosis	Cancer
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 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-158113

CBPD-409	Histone Acetyltransferase PROTACs	Cancer
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC₅₀ of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC₅₀s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .

HY-130612

PROTAC BRD2/BRD4 degrader-1	Epigenetic Reader Domain PROTACs	Cancer
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library	54 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2). MCE carefully prepared a unique collection of 54 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

E3 Ligase Ligand Library

54 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.

Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).

MCE carefully prepared a unique collection of 54 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

Cat. No.	Product Name	Target	Research Area

HY-P5022

Cullin-Associated NEDD8-Dissociated Protein 1 (548-566)	Peptides	Others
Cullin-Associated NEDD8-Dissociated Protein 1 (548-566) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .

Species:	Human (10)
Tag:	His (6) Strep (4) Tag Free (4)
Source:	Sf9 insect cells (9) E. coli (1)

Cat. No.	Compare	Product Name	Species	Source

HY-P702070

	CUL5 Protein, Human (Sf9) CUL5; cullin-5; CUL-5; Vasopressin-activated calcium-mobilizing receptor 1; VACM-1	Human	Sf9 insect cells
	The CUL5 protein is a core component of the SCF-like ECS E3 ubiquitin-protein ligase complex. CUL5 Protein, Human (Sf9) is the recombinant human-derived CUL5 protein, expressed by Sf9 insect cells , with tag free. The total length of CUL5 Protein, Human (Sf9) is 779 a.a., .

HY-P703245

	CUL3-RBX1 Protein, Human (Active, Sf9, His, Strep) KIAA0617; cullin-4A	Human	Sf9 insect cells

HY-P703242

	CUL1-RBX1 Protein, Human (Active, Sf9) cullin-1; CUL1; Homo sapiens; Human; CUL-1	Human	Sf9 insect cells

HY-P703244

	CUL2-RBX1 Protein, Human (Sf9, His) cullin-2; CUL2; Homo sapiens; Human; CUL-2	Human	Sf9 insect cells

HY-P703246

	CUL4A-RBX1 Protein, Human (Active, Sf9) cullin-4A; CUL4A; Homo sapiens; Human	Human	Sf9 insect cells

HY-P703243

	CUL1-RBX1 Protein, Human (Active, Sf9, His, Strep) cullin-1; CUL1; Homo sapiens; Human; CUL-1	Human	Sf9 insect cells

HY-P702071

	CUL5 Protein, Human (Sf9, His, Strep) CUL5; cullin-5; CUL-5; Vasopressin-activated calcium-mobilizing receptor 1; VACM-1	Human	Sf9 insect cells
	The CUL5 protein is a core component of the SCF-like ECS E3 ubiquitin-protein ligase complex. CUL5 Protein, Human (Sf9, His, Strep) is the recombinant human-derived CUL5 protein, expressed by Sf9 insect cells , with N-Strep, N-8*His labeled tag. The total length of CUL5 Protein, Human (Sf9, His, Strep) is 779 a.a., .

HY-P701587

	KLHL42 Protein, Human (Sf9) KLHL42; Kelch-like protein 42; cullin-3-binding protein 9; Ctb9; Kelch domain-containing protein 5	Human	Sf9 insect cells
	KLHL42 serves as a substrate-specific linker in the BCR E3 ubiquitin ligase complex and plays a critical role in mitotic progression and cytokinesis. The BCR(KLHL42) complex actively ubiquitinates and degrades KATNA1, contributing to the regulation of microtubule dynamics during mitosis. KLHL42 Protein, Human (Sf9) is the recombinant human-derived KLHL42 protein, expressed by Sf9 insect cells , with tag free. The total length of KLHL42 Protein, Human (Sf9) is 504 a.a., .

HY-P701588

	KLHL42 Protein, Human (Sf9, His, Strep) KLHL42; Kelch-like protein 42; cullin-3-binding protein 9; Ctb9; Kelch domain-containing protein 5	Human	Sf9 insect cells
	KLHL42 serves as a substrate-specific linker in the BCR E3 ubiquitin ligase complex and plays a critical role in mitotic progression and cytokinesis. The BCR(KLHL42) complex actively ubiquitinates and degrades KATNA1, contributing to the regulation of microtubule dynamics during mitosis. KLHL42 Protein, Human (Sf9, His, Strep) is the recombinant human-derived KLHL42 protein, expressed by Sf9 insect cells , with N-Strep, N-8*His labeled tag. The total length of KLHL42 Protein, Human (Sf9, His, Strep) is 504 a.a., .

HY-P70093

	DCN1-like protein 1/DCUN1D1 Protein, Human (His) rHuDCN1-like protein 1/DCUN1D1, His; DCN1-Like Protein 1; DCUN1 Domain-Containing Protein 1; Defective in cullin Neddylation Protein 1-Like Protein 1; Squamous Cell Carcinoma-Related Oncogene; DCUN1D1; DCUN1L1; RP42; SCCRO	Human	E. coli
	DCN1-like protein 1 (DCUN1D1) is an important component of the E3 ubiquitin ligase complex and promotes neddylation of the cullin component within the E3 cullin-RING ubiquitin ligase complex. By binding to the cullin-RBX1 complex in the cytoplasm, DCUN1D1 promotes its nuclear translocation, enhances E2-NEDD8 thioester recruitment, and optimizes protein orientation for efficient NEDD8 transfer. DCN1-like protein 1/DCUN1D1 Protein, Human (His) is the recombinant human-derived DCN1-like protein 1/DCUN1D1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of DCN1-like protein 1/DCUN1D1 Protein, Human (His) is 259 a.a., with molecular weight of ~32.0 kDa.

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Cat. No.	Product Name	Chemical Structure

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][2].

Cat. No.	Compare	Product Name	Application	Reactivity

HY-P82840

	Cullin 5 Antibody (YA2585) CUL-5; VACM1; VACM-1	WB	Human, Mouse, Rat
	Cullin 5 Antibody (YA2585) is a biotin-conjugated non-conjugated IgG antibody, targeting Cullin 5, with a predicted molecular weight of 91 kDa (observed band size: 91 kDa). Cullin 5 Antibody (YA2585) can be used for WB experiment in human, mouse, rat background.

HY-P82633

	Cullin 1 Antibody (YA2378) CUL1; cullin1	WB, IHC-P, ICC/IF, IP, FC	Human, Mouse, Rat
	Cullin 1 Antibody (YA2378) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2378), targeting Cullin 1, with a predicted molecular weight of 90 kDa (observed band size: 90 kDa). Cullin 1 Antibody (YA2378) can be used for WB, IHC-P, ICC/IF, IP, FC experiment in human, mouse, rat background.

HY-P82457

	Cullin 2 Antibody (YA2202) Cul2; CUL 2; CUL2; cullin 2	WB, ICC/IF, IP, FC	Human, Mouse, Rat
	Cullin 2 Antibody (YA2202) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2202), targeting Cullin 2, with a predicted molecular weight of 87 kDa (observed band size: 87 kDa). Cullin 2 Antibody (YA2202) can be used for WB, ICC/IF, IP, FC experiment in human, mouse, rat background.

HY-P82833

	Cullin 3 Antibody (YA2578) CUL3; KIAA0617; cullin-3; CUL-3	WB, IP	Human, Mouse, Rat
	Cullin 3 Antibody (YA2578) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2578), targeting Cullin 3, with a predicted molecular weight of 89 kDa (observed band size: 89 kDa). Cullin 3 Antibody (YA2578) can be used for WB, IP experiment in human, mouse, rat background.

HY-P82838

	Cullin 4A/4B Antibody (YA2583) CUL4B; KIAA0695; cullin-4B; CUL-4B	WB, IHC-P	Human, Hamster, Rat
	Cullin 4A/4B Antibody (YA2583) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2583), targeting Cullin 4A/4B, with a predicted molecular weight of 104 kDa (observed band size: 88,104 kDa). Cullin 4A/4B Antibody (YA2583) can be used for WB, IHC-P experiment in human, hamster, rat background.

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Inhibitors & Agonists

Screening Libraries

Peptides

Recombinant Proteins

Isotope-Labeled Compounds

Antibodies