Search Result

Results for "

recruiting

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ligands for E3 Ligase (227) 5-HT Receptor (3) Adenosine Receptor (2) Akt (2) Androgen Receptor (2) Antibiotic (1) Apelin Receptor (APJ) (5) Apoptosis (10) Arrestin (14) Autophagy (80) Bacterial (2) Bcl-2 Family (1) Bcr-Abl (3) Btk (4) c-Myc (1) Cannabinoid Receptor (2) Carbonic Anhydrase (1) CCR (1) CD20 (1) CD3 (2) CFTR (2) Constitutive Androstane Receptor (1) CRISPR/Cas9 (1) CXCR (8) DNA/RNA Synthesis (2) Dopamine Receptor (4) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (16) EGFR (2) Endogenous Metabolite (1) Epigenetic Reader Domain (5) ERK (1) Estrogen Receptor/ERR (2) FXR (1) GLP Receptor (1) GPR35 (1) GPR55 (2) HCV (1) Histamine Receptor (2) Histone Acetyltransferase (1) Histone Methyltransferase (4) HIV (3) HuR (1) Isotope-Labeled Compounds (1) JAK (2) Ligands for Target Protein for PROTAC (1) LPL Receptor (1) MAP3K (1) MAPKAPK2 (MK2) (1) MDM-2/p53 (2) MEK (2) Microtubule/Tubulin (1) Mitochondrial Metabolism (1) Mitophagy (1) Molecular Glues (2) MyD88 (1) NF-κB (3) Notch (1) Nucleoside Antimetabolite/Analog (1) Opioid Receptor (3) P2Y Receptor (2) p62 (1) PARP (1) PERK (2) Phosphodiesterase (PDE) (2) PI3K (2) PPAR (2) PROTAC Linkers (1) PROTACs (28) Protease Activated Receptor (PAR) (1) RAD51 (1) Ras (1) ROR (1) SHP2 (1) SNIPERs (1) STAT (1) STING (2) Syk (2) Target Protein Ligand-Linker Conjugates (9) Tau Protein (1) Thyroid Hormone Receptor (3) TNF Receptor (2) Toll-like Receptor (TLR) (2) Wee1 (4)
By Research Areas:	Cancer (328) Cardiovascular Disease (5) Endocrinology (4) Infection (6) Inflammation/Immunology (34) Metabolic Disease (9) Neurological Disease (14)
Click Chemistry:	DBCO (1) Azide (5) Alkynes (2)

386

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Ligands for E3 Ligase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-133137

SJF620

PROTACs Btk Cancer

SJF620 is a PROTAC connected by ligands for Cereblon and Btk with a DC₅₀ of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .

SJF620	PROTACs Btk	Cancer
SJF620 is a PROTAC connected by ligands for Cereblon and Btk with a DC₅₀ of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .

HY-156157

GPR55 agonist 4	GPR55	Cancer
GPR55 agonist 4 (Compound 28) is a GPR55 agonist (EC₅₀: 131 nM, and 1.41 nM for hGPR55 and rGPR55). GPR55 agonist 4 induces β-arrestin recruitment to human GPR55 .

HY-133137A

SJF620 hydrochloride	PROTACs Btk	Cancer
SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and Btk with a DC₅₀ of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .

HY-156107

GPR55 agonist 3	GPR55	Cancer
GPR55 agonist 3 (Compound 26) is a GPR55 agonist (EC₅₀: 0.239 nM, and 1.76 nM for hGPR55 and rGPR55). GPR55 agonist 3 induces β-arrestin recruitment to human GPR55 (EC₅₀: 6.2 nM) .

HY-136572

CEM114	Epigenetic Reader Domain CRISPR/Cas9	Cancer
CEM114 is an effective chemical epigenetic modifier (CEM) that recruits endogenous chromatin machinery through CRISPR-Cas9 systems .

HY-143345

EN523

Others Cancer

EN523 is a OTUB1 recruiter. EN523 targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1 .

EN523	Others	Cancer
EN523 is a OTUB1 recruiter. EN523 targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1 .

HY-116088

W123	LPL Receptor	Inflammation/Immunology
W123, a FTY720 analog, is a competitive sphingosine 1-phosphate type 1 (S1P1) receptor antagonist. W123 is measured by GTPγS activation, MAPK recruitment, cell migration, and ligand-induced receptor internalization .

HY-152247

DDO3711	MAP3K	Cancer
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC₅₀ =164.1 nM) not ASK2 (IC₅₀>20 μM). DDO3711 significantly dephosphorylates p-ASK1 ^T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research .

HY-128121

MLS1547	Dopamine Receptor	Neurological Disease
MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (K_i=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC₅₀=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC₅₀=9.9 μM) .

HY-119339

SX-682 4 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity .

HY-141513

NH-3 1 Publications Verification	Thyroid Hormone Receptor	Neurological Disease
NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC₅₀ of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment . NH-3 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-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) .

HY-145696

SJ10542	PROTACs JAK	Inflammation/Immunology Cancer
SJ10542 is a potent and selective JAK2/3 directing phenyl glutarimide (PG)-PROTAC with DC₅₀s of 14, 11, and 24 nM for JAK2, JAK3, and JAK2-fusion ALL, respectively. SJ10542 utilizes a PG ligand as the cereblon (CRBN) recruiter .

HY-163277

PIPE-3297	Opioid Receptor	Inflammation/Immunology
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC₅₀ of 1.1 nM and exhibits lowβ-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .

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 .

HY-119486A

(Rac)-Tavapadon (Rac)-PF-06649751; (Rac)-CVL-751	Dopamine Receptor Arrestin	Neurological Disease
(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC₅₀=0.8 nM; β-arrestin2, EC₅₀=68 nM). (Rac)-Tavapadon has antiparkinsonian activity .

HY-120645

BMS-986122	Opioid Receptor	Neurological Disease
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ ³⁵S]GTPγS binding in mouse brain membranes .

HY-P1682

Balixafortide POL6326	CXCR Arrestin	Cancer
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC₅₀ < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC₅₀s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .

HY-P1682A

Balixafortide TFA 1 Publications Verification POL6326 TFA	CXCR Arrestin	Cancer
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC₅₀ < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC₅₀s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .

HY-150057

CB1R Allosteric modulator 4	Cannabinoid Receptor	Others
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .

HY-150265

TNH

TMP-NVOC linker-Halo
Others Others

TNH is a dimer that can enter living cells and recruit proteins into cellular structures .

TNH TMP-NVOC linker-Halo	Others	Others
TNH is a dimer that can enter living cells and recruit proteins into cellular structures .

HY-118521

AS-041164	PI3K	Inflammation/Immunology
AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC₅₀ of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC₅₀s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects .

HY-161166

MM-02-57

Others Others

MM-02-57 is a covalent DDB1 CUL4A adaptor protein recruiter .

MM-02-57	Others	Others
MM-02-57 is a covalent DDB1 CUL4A adaptor protein recruiter .

HY-139544

Thalidomide-5-propoxyethanamine	Ligands for E3 Ligase	Cancer
Thalidomide-5-propoxyethanamine is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein .

HY-139548

Thalidomide-5-methyl

Ligands for E3 Ligase Cancer

Thalidomide-5-methyl is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein .
HY-143348

NJH-2-030

E3 Ligase Ligand-Linker Conjugates Others

NJH-2-030 can be used as a covalent recruiter for FEM1B in targeted protein degradation applications.

Thalidomide-5-methyl	Ligands for E3 Ligase	Cancer
Thalidomide-5-methyl is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein .

NJH-2-030	E3 Ligase Ligand-Linker Conjugates	Others
NJH-2-030 can be used as a covalent recruiter for FEM1B in targeted protein degradation applications.

HY-145232

PhosTAC7	PROTACs	Others
Similar to PROTACs in their ability to induce ternary complexes, PhosTAC7 focuses on recruiting a Ser/Thr phosphatase to a phosphosubstrate to mediate its dephosphorylation.

HY-11067

WHI-P97 2 Publications Verification	JAK	Inflammation/Immunology
WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo .

HY-123813

CCX-777

Arrestin Cancer

CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3) .

CCX-777	Arrestin	Cancer
CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3) .

HY-N3196

Neotuberostemonine	Bacterial	Infection Inflammation/Immunology
Neotuberostemonine, one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, attenuates bleomycin-induced pulmonary fibrosis by suppressing the recruitment and activation of macrophages .

HY-139549

Thalidomide-benzo	Ligands for E3 Ligase	Cancer
Thalidomide-benzo hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-benzo can be connected to the ligand for protein by a linker to form PROTACs .

HY-149307

CYCA-117-70

Others Others

CYCA-117-70 is a DCAF1 ligand (K_D: 70 μM). CYCA-117-70 is an ideal chemical handles for PROTACs recruiting DCAF1 .

CYCA-117-70	Others	Others
CYCA-117-70 is a DCAF1 ligand (K_D: 70 μM). CYCA-117-70 is an ideal chemical handles for PROTACs recruiting DCAF1 .

HY-130707

K-Ras ligand-Linker Conjugate 3	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-130822

K-Ras ligand-Linker Conjugate 4	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-130823

K-Ras ligand-Linker Conjugate 5	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-130991

K-Ras ligand-Linker Conjugate 6	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-115878

NJH-2-057

CFTR Others

NJH-2-057 is an EN523 OTUB1 recruiter linked to lumacaftor, a agent used to treat cystic fibrosis that binds ΔF508-CFTR.
HY-143343

LEB-03-153

Wee1 Cancer

LEB-03-153 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through no linker .

NJH-2-057	CFTR	Others
NJH-2-057 is an EN523 OTUB1 recruiter linked to lumacaftor, a agent used to treat cystic fibrosis that binds ΔF508-CFTR.

LEB-03-153	Wee1	Cancer
LEB-03-153 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through no linker .

HY-50688

SB-265610 2 Publications Verification	CXCR	Inflammation/Immunology
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC₅₀s of 3.7 nM and 70 nM, respectively .

HY-105999B

APC 366 TFA

Others Others

APC 366 (TFA) is an irreversible mast cell tryptase inhibitor. APC 366 (TFA) can be used for the research of allergic diseases .
HY-153385

TMX1

Epigenetic Reader Domain Apoptosis Cancer

TMX1 is a BRD4 covalent molecular glue degrader. TMX1 selectively recruits DCAF16 to BRD4BD2, resulting in the degradation of BRD4 .

APC 366 TFA	Others	Others
APC 366 (TFA) is an irreversible mast cell tryptase inhibitor. APC 366 (TFA) can be used for the research of allergic diseases .

TMX1	Epigenetic Reader Domain Apoptosis	Cancer
TMX1 is a BRD4 covalent molecular glue degrader. TMX1 selectively recruits DCAF16 to BRD4BD2, resulting in the degradation of BRD4 .

HY-131445A

SS-RJW100	Others	Metabolic Disease Inflammation/Immunology
SS-RJW100 is a enantiomer of RJW100, which is a racemic agonist of nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). SS-RJW100 promotes recruitment of coregulator protein fragments in vitro, recruits the transcriptional intermediary factor 2 (Tif2) coactivator to LRH-1. SS-RJW100 diminishes LRH-1 allosteric activation networks, shows poor thermal stability .

HY-132808

Atuzabrutinib SAR 444727; PRN473	Btk	Inflammation/Immunology
Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling .

HY-156828

MMH2

Others Others

MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4_BD2) .
HY-156827

MMH1

Others Others

MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4_BD2) .
HY-143340

LEB-03-145

Wee1 Cancer

LEB-03-145 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C5 alkyl linker .

MMH2	Others	Others
MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4_BD2) .

MMH1	Others	Others
MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4_BD2) .

LEB-03-145	Wee1	Cancer
LEB-03-145 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C5 alkyl linker .

HY-23095

Thalidomide-5-OH	Ligands for E3 Ligase	Cancer
Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs .

HY-W076696

Lenalidomide-4-OH	Ligands for E3 Ligase	Cancer
Lenalidomide-4-OH is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-OH can be connected to the ligand for protein by a linker to form PROTAC.

HY-139539

Thalidomide-5-COOH	Ligands for E3 Ligase	Cancer
Thalidomide-5-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-COOH can be connected to the ligand for protein by a linker to form PROTACs .

HY-123109

(S,R,S)-AHPC-Boc VH032-Boc	Ligands for E3 Ligase	Cancer
(S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology .

Cat. No.	Product Name

HY-L024

Histone Modification Research Compound Library

614 compounds

A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.

MCE owns a unique collection of 614 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

HY-L129

Target Protein Ligand Library

39 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. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 39 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

HY-L128

E3 Ligase Ligand Library

88 compounds

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 88 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-P1682A

Balixafortide TFA 1 Publications Verification POL6326 TFA	CXCR Arrestin	Cancer
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC₅₀ < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC₅₀s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .

HY-P2197

ELA-11(human)	Apelin Receptor (APJ) Arrestin	Inflammation/Immunology
ELA-11(human), a peptide, is a full agonist of human apelin receptor, with a pK_i of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment .

HY-P1099

Ac2-12 1 Publications Verification	Peptides	Inflammation/Immunology
Ac2-12, an annexin/lipocortin 1 (LC1)-mimetic peptide, inhibit neutrophil extravasation. Ac2-12 has antimigratory action and inhibits recruitment of neutrophils in experimental inflammation models .

HY-P1682

Balixafortide POL6326	CXCR Arrestin	Cancer
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC₅₀ < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC₅₀s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .

HY-P4272

Tetraproline	Peptides	Others
Tetraproline is a fragment sequence in tristetraprolin (TTP). Recruitment of the 4EHP-GYF2 cap-binding complex to tetraproline motifs of tristetraprolin promotes repression and degradation of mRNAs with AU-rich elements .

HY-P1099A

Ac2-12 TFA	Peptides	Inflammation/Immunology
Ac2-12 TFA, an annexin/lipocortin 1 (LC1)-mimetic peptide, inhibit neutrophil extravasation. Ac2-12 TFA has antimigratory action and inhibits recruitment of neutrophils in experimental inflammation models .

HY-P2249

ELA-21 (human)	Arrestin Apelin Receptor (APJ)	Cardiovascular Disease
ELA-21 (human) is an apelin receptor agonist with a pK_i of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .

HY-P10114

STAT3-IN-24, cell-permeable PpYLKTK-mts; STAT3 PI	STAT	Cancer
STAT3-IN-24, cell-permeable (PpYLKTK-mts) is a STAT3 peptide inhibitor. STAT3-IN-24, cell-permeable inhibits recruitment of STAT3 to Jak2 and phosphorylation of Y705, thus preventing the dimerization and the nuclear translocation of STAT3 .

HY-108742

Abaloparatide 1 Publications Verification BA 058; BIM 44058	Thyroid Hormone Receptor Arrestin	Metabolic Disease
Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis .

HY-138951

AY77	Protease Activated Receptor (PAR)	Inflammation/Immunology Cancer
AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC₅₀ of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca ²⁺ release .

HY-P1102

TC14012 2 Publications Verification	CXCR HIV	Infection Cancer
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC₅₀ of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC₅₀ of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .

HY-P2197A

ELA-11(human) TFA	Apelin Receptor (APJ)	Inflammation/Immunology
ELA-11(human) TFA is a high affinity apelin receptor agonist (K_i=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.

HY-126327

UNC4976	Histone Methyltransferase	Cancer
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

HY-108742A

Abaloparatide TFA 1 Publications Verification BA 058 TFA; BIM 44058 TFA	Thyroid Hormone Receptor Arrestin	Metabolic Disease Endocrinology
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis .

HY-P1102A

TC14012 TFA	CXCR HIV	Infection Cancer
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC₅₀ of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC₅₀ of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .

HY-126327A

UNC4976 TFA	Histone Methyltransferase	Cancer
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

Cat. No.	Product Name	Target	Research Area

HY-P99394

Talquetamab JNJ-64407564	CD3	Cancer
Talquetamab (JNJ-64407564) is a humanized bispecific antibody that binds to GPRC5D (member of G protein-coupled receptor family C5 group D) and CD3 to induce T cell-mediated killing of GPRC5D-expressing MM cells through T cell recruitment and activation. Talquetamab (JNJ-64407564) has antitumor activity .

HY-P99746

Murlentamab 3C23K; GM102	Inhibitory Antibodies	Inflammation/Immunology Cancer
Murlentamab (3C23K; GM102) is a humanized anti-AMHRII antibody. AMHRII is the anti-Müllerian hormone receptor. Murlentama significantly promotes macrophage-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Murlentama stimulates pro-inflammatory and anti-tumor internal environment, recruits and activates T cells. Murlentama suppresses tumors growth by inducing naïve macrophage orientation and promoting tumor-associated macrophage (TAM) reprogramming .

HY-P99361

Enavatuzumab PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)	TNF Receptor	Cancer
Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .

HY-P99776

Plamotamab XmAb-13676	CD20 CD3	Cancer
Plamotamab (XmAb-13676) is a human bispecific antibody (bsAb) that binds CD3 and CD20. Plamotamab recruits cytotoxic T cells to kill CD20 ⁺ expressing tumor cells. Plamotamab induces a mild hematologic reaction (MR), and results in tumor regression in vivo .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N3196

Neotuberostemonine	Alkaloids Structural Classification Classification of Application Fields Stemonaceae Source classification Plants Inflammation/Immunology Disease Research Fields Stemona tuberosa Lour. Indole Alkaloids	Bacterial
Neotuberostemonine, one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, attenuates bleomycin-induced pulmonary fibrosis by suppressing the recruitment and activation of macrophages .

HY-W020790

Sialyl-Lewis X sLeX	Structural Classification Polysaccharides Classification of Application Fields Source classification Endogenous metabolite Inflammation/Immunology Disease Research Fields Saccharides	Endogenous Metabolite
Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin) . Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation .

Cat. No.	Product Name	Chemical Structure

HY-128423AS

Tylvalosin-d9
Tylvalosin-d₉ (Acetylisovaleryltylo?sin-d₉)is the deuterium labeledTylvalosin(HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .

Cat. No.	Product Name		Classification

HY-157182

DNP-PEG2-NHCO-C2-DBCO		DBCO
DNP-PEG2-NHCO-C2-DBCO is a clickable hapten that bears a dinitrophenyl (DNP) moiety as the antibody‐recruiting motif at one end, a polyethylene glycol chain as a spacer and a dibenzocyclooctene at the other end for the SPAAC chemistry .

HY-161134

Lenalidomide 4'-PEG2-azide		Azide
Lenalidomide 4'-PEG2-azide is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide 4'-PEG2-azide can be connected to the ligand for protein by a linker to form PROTAC .

HY-139332

Pomalidomide 4'-PEG6-azide		Azide
Pomalidomide 4'-PEG6-azide (compound 33e) is the E3 ligase ligand-linker conjugate used in the recruitment of CRBN protein. Pomalidomide 4'-alkylC3-acid can be used to synthesize PROTACs .

HY-139333

Pomalidomide 4'-PEG5-azide		Azide
Pomalidomide 4'-PEG5-azide is the Pomalidomide (HY-123324)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide 4'-PEG5-azide can be connected to the ligand for protein by a linker to form PROTAC .

HY-139339

Pomalidomide 4'-alkylC6-azide		Azide
Pomalidomide 4'-alkylC6-azide is the Pomalidomide (HY-123324)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide 4'-alkylC6-azide can be connected to the ligand for protein by a linker to form PROTAC .

HY-157514

Thalidomide 4'-ether-PEG1-azide		Azide
Thalidomide 4'-ether-PEG1-azide is the Thalidomide (HY-14658)-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4'-ether-PEG1-azide can be connected to the ligand for protein by a linker to form PROTACs .

HY-126457

Thalidomide-propargyl		Alkynes
Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs . Thalidomide-propargyl 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-147858

PROTAC EGFR degrader 7		Alkynes
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR ^L858R/T790M degrader, with a DC₅₀ of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC₅₀ of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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