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CRBN Degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (4) Androgen Receptor (5) Apoptosis (25) ATM/ATR (1) Autophagy (2) AUTOTACs (1) Bcl-2 Family (3) BCL6 (1) Btk (6) c-Fms (1) c-Kit (1) c-Met/HGFR (2) c-Myc (2) Casein Kinase (2) Caspase (1) CDK (10) DNA/RNA Synthesis (3) E1/E2/E3 Enzyme (4) E3 Ligase Ligand-Linker Conjugates (14) EGFR (7) Epigenetic Reader Domain (13) Estrogen Receptor/ERR (1) Eukaryotic Initiation Factor (eIF) (1) FAK (3) FGFR (3) FKBP (2) FLT3 (4) Fluorescent Dye (1) GSK-3 (2) HDAC (2) Hexokinase (1) Histone Acetyltransferase (3) Histone Demethylase (1) Histone Methyltransferase (3) HIV (1) HSP (1) IKK (1) IKZF Family (8) Indoleamine 2,3-Dioxygenase (IDO) (1) Interleukin Related (2) IRAK (6) Isotope-Labeled Compounds (3) JAK (3) JNK (1) Ligands for E3 Ligase (20) Ligands for Target Protein for PROTAC (9) MALT1 (1) MDM-2/p53 (1) MEK (1) Mixed Lineage Kinase (1) MNK (1) Molecular Glues (25) mTOR (1) NEKs (1) NF-κB (3) PARP (4) PD-1/PD-L1 (1) PDGFR (1) PDK-1 (1) Phosphatase (1) PIN1 (1) PROTAC Linkers (1) PROTACs (117) Raf (1) Ras (2) Reactive Oxygen Species (1) RET (1) ROR (1) SF3B1 (1) Small Interfering RNA (siRNA) (1) SOS1 (1) STAT (2) STING (4) Target Protein Ligand-Linker Conjugates (8) TNF Receptor (1) Trk Receptor (1) VEGFR (1) WDR5 (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (166) Infection (2) Inflammation/Immunology (22) Metabolic Disease (1) Neurological Disease (6)
Click Chemistry:	PROTAC Synthesis (1) Azide (1) Alkynes (2)

189

Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-128845

*PROTAC CRBN* Degrader-1**	PROTACs E1/E2/E3 Enzyme	Cancer
PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other . (Blue: VHL ligand (S,R,S)-AHPC (HY-125845); Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846); Black: Linker (HY-128847))

HY-162014

WDR5 degrader-1	PROTACs WDR5	Cancer
WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1 .

HY-130714

TD-165 1 Publications Verification	PROTACs	Cancer
TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a?cereblon (CRBN)?ligand binding group, a linker and an?von Hippel-Landau (VHL)?binding group .

HY-132857A

ZXH-4-130 TFA 1 Publications Verification	PROTACs	Neurological Disease
ZXH-4-130 TFA is a highly potent and selective degrader of *CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). ZXH-4-130 TFA induces ~80% CRBN* degradation at 10 nM in MM1.S cells .

HY-126534

Abemaciclib metabolite M18 1 Publications Verification LSN3106729	Ligands for Target Protein for PROTAC CDK	Cancer
Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .

HY-130800

Eragidomide 2 Publications Verification CC-90009	Ligands for E3 Ligase Molecular Glues Apoptosis	Inflammation/Immunology Cancer
Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4 ^CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation .

HY-169077

IKZF3 degrader 1	Molecular Glues IKZF Family	Cancer
IKZF3 degrader 1 (compound 19a) is a molecular glue degrader of IKZF3 (EC₅₀=0.012 μM). IKZF3 degrader 1 promotes the binding of IKZF3 to Cereblon (CRBN), leading to the ubiquitination and degradation of IKZF3 .

HY-172827

PROTAC BRD4 Degrader-30	PROTACs Epigenetic Reader Domain
PROTAC BRD4 degrader-30 is an ISOX-DUAL-Based PROTAC degrader selectively targeting BRD4 (IC₅₀ = 65 nM). PROTAC BRD4 degrader-30 can be used for research of c-Myc oncoprotein and cancer cell pathophysiology. (Pink: BRD4 ligand (HY-172828); Blue: CRBN ligand (HY-103596); Black: linker (HY-Y0139); CRBN ligand+linker: HY-138847) .

HY-163757

PROTAC PD-L1 degrader-1	PROTACs PD-1/PD-L1	Inflammation/Immunology Cancer
PROTAC PD-L1 degrader-1 is a *CRBN*-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC₅₀ of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745)) .

HY-151886

NU223612	PROTACs Indoleamine 2,3-Dioxygenase (IDO)	Neurological Disease Cancer
NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a K_d of 640 nM. NU223612 potently degrades the IDO1 protein through *CRBN*-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB) .

HY-132288

Pom-8PEG	E3 Ligase Ligand-Linker Conjugates	Cancer
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader .

HY-122725A

Lenalidomide-C5-NH2 TFA	E3 Ligase Ligand-Linker Conjugates	Cancer
Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader .

HY-172736

BMS-986458	PROTACs BCL6	Cancer
BMS-986458 is a highly selective and orally active BCL6 PROTAC degrader. BMS-986458 simultaneously co-opts cereblon (CRBN) and the BCL6 N-terminal BTB domain to catalyze proximity induced degradation of BCL6. BMS-986458 can be used for the study of B-cell Non-Hodgkin's lymphoma (Pink: Target protein ligand (HY-172740); Black: linker (HY-W267161); Blue: E3 ligase ligand (HY-W593794)) .

HY-129776

K-Ras ligand-Linker Conjugate 2	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 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-129775

K-Ras ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 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-153341

CFT1946	PROTACs Raf	Cancer
CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC ) degrader of BRAF ^V600E with a DC₅₀ of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF ^V600E splice variant. CFT1946 can be used in tumor research .

HY-136262

CRBN-6-5-5-VHL	PROTACs E1/E2/E3 Enzyme	Cancer
CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based *cereblon (CRBN)* degrader with a DC₅₀ value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3. (Pink: VHL ligand (HY-125845); Blue: E3 Ligase ligand (HY-10984); Black: linker (HY-403544)) .

HY-132857

ZXH-4-130	PROTACs	Neurological Disease
ZXH-4-130 is a highly potent and selective degrader of *CRBN. ZXH-4-130 is a CRBN*-VHL compound (hetero-PROTAC) .

HY-132862

ZXH-4-137	PROTACs	Cancer
ZXH-4-137 is a potent and selective CRBN degrader (PROTAC).

HY-157426

GSPT1 degrader-3	Epigenetic Reader Domain PROTACs	Cancer
GSPT1 degrader-3 (Pro-2) is a CRBN-based PROTAC degrader for BRD, with a DC₅₀ of 21.1 nM (4h) .

HY-160531

IKZF1-degrader-1	Molecular Glues IKZF Family	Cancer
IKZF1-degrader-1 (Compound 9-B) is a IKZF1 molecular glue degrader with the DC₅₀ value of 0.134 nM. IKZF1-degrader-1 can be used to degrader tumors .

HY-111594

Homo-PROTAC cereblon degrader 1 1 Publications Verification	PROTACs	Cancer
Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3 .

HY-158325

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

HY-143435

AG6033	Apoptosis	Cancer
AG6033 is a potential novel *CRBN* modulator. AG6033 suppresses various tumor cells by modulating the interactions between *CRBN* and various antitumor target proteins. AG6033 can cause GSPT1 and IKZF1 degradation. AG6033 induces *CRBN*-dependent cytotoxic effect .

HY-156591

PROTAC MLKL Degrader-1	PROTACs Mixed Lineage Kinase	Others
PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC degrader of MLKL, with a D_max ＞90%. PROTAC MLKL Degrader-1 contains modified CRBN ligands, linker and Lenalidomide (HY-A0003)-linker fragments. PROTAC MLKL Degrader-1 abrogates cell death in a TSZ model of necroptosis.

HY-114406

TD-106	Ligands for E3 Ligase	Cancer
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .

HY-147158

ZXH-1-161	Molecular Glues	Cancer
ZXH-1-161 is a potent *CRBN* modulator that selectively induces the degradation of GSPT1 in a *CRBN*-dependent manner. ZXH-1-161 can inhibit the proliferation of multiple myeloma cells and exhibits antitumor activity .

HY-172770

KMG-1068	Molecular Glues	Cancer
KMG-1068 (Compound 4a), a molecular glue, is a GSPT1/2 degrader. KMG-1068 effectively induces the CRBN-dependent degradation of GSPT1/2 by binding to the IMiD binding site on CRBN, facilitating the formation of a ternary complex with GSPT1/2. KMG-1068 is promising for research of cancers .

HY-158381

PROTAC PTP1B degrader 1	PROTACs Phosphatase	Metabolic Disease
PROTAC PTP1B degrader 1 (compound 75) is a CRBN-based PTP1B PROTAC degrader, with DC₅₀ values of 0.2 μM (48 h) and 0.05 μM (72 h) (Red: PTP1B ligand Oleanolic acid (HY-N0156); Black: linker; Blue: CRBN ligand) .

HY-170449

E3 ligase Ligand 48	Ligands for E3 Ligase	Others
E3 ligase Ligand 48 is a *CRBN* ligand for PROTAC AR Degrader-9 (HY-170448). PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC₅₀ of 262.38 nM .

HY-139186

PROTAC KRAS G12C degrader-1	PROTACs	Cancer
PROTAC KRAS G12C degrader-1 is a Cereblon-based KRAS ^G12C PROTAC degrader. PROTAC KRAS G12C degrader-1 induces CRBN/ KRAS ^G12C dimerization and degrades GFP- KRAS ^G12C in reporter cells .

HY-164891

EM12-FS	Molecular Glues	Others
EM12-FS is a cereblon (CRBN) ligand that binds CRBN at His353 and a molecular glue degrader of NTAQ1. EM12-FS has a human plasma half-life of 196 min .

HY-163168

aTAG 4531 CFT-4531	PROTACs DNA/RNA Synthesis	Cancer
aTAG 4531 (CFT-4531) is a potent, selective, and onmechanism tool degrader of MTH1 with DC₅₀ value of 0.28 nM and K_i value of 1.8 nM. The degradation activity is due to the intricate formation of the ternary complex between the MTH1 aTAG, CRBN E3 ligase, and aTAG tool degrader. Red: MTH1 aTAG inhibitor (HY-134725), Blue: CRBN ligand (HY-126457), Black: linker (HY-108374) .

HY-151902

SJ988497	PROTACs JAK	Cancer
SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL) .

HY-133144

Lenalidomide-OH	Ligands for E3 Ligase	Cancer
Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137) .

HY-161536

PROTAC EGFR degrader 9	PROTACs EGFR Apoptosis	Cancer
PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC₅₀ of 10.2 nM and a K_d of 240.2 nM against EGFR ^{L858R/T790M/C797S}. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)) .

HY-176180

PROTAC STING degrader-4	PROTACs STING NF-κB IKK	Inflammation/Immunology
PROTAC STING degrader-4 is a nitro-free covalent STING PROTAC degrader with a DC₅₀ of 3.23 μM. PROTAC STING degrader-4 effectively inhibits STING as well as its downstream signaling, such as p-TBK1 and p-NF-κB (p-P65), and immune-inflammatory cytokines. PROTAC STING degrader-4 mitigates kidney and blood inflammation in Cisplatin (HY-17394)-induced acute kidney injury (AKI) mice model . Pink: STING ligand (HY-176183); Blue: CRBN ligase ligand (HY-103596); Black: linker (HY-176182); CRBN ligase ligand + linker: HY-176181

HY-169235

DHHC3 degrader 1	Ligands for Target Protein for PROTAC	Cancer
DHHC3 degrader 1 is a PROTAC target protein ligand that is used to synthesize PCC16 chloride (HY-169232) .

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-131318

Lenalidomide-I	Ligands for E3 Ligase	Cancer
Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609) .

HY-176428

PROTAC MNK1 degrader-1	PROTACs MNK Apoptosis Eukaryotic Initiation Factor (eIF)	Cancer
PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC₅₀ of 11.92 nM, and a D_max > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC₅₀: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety . Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430

HY-163851

PROTAC Vif degrader-1	PROTACs HIV	Infection
PROTAC Vif degrader-1 (Compound L15) is a Vif PROTAC degrader. PROTAC Vif degrader-1 has antiviral activity against HIV-1 (EC₅₀: 33.35 μM against HIV-1_IIIB). Blue: CRBN ligand (HY-10984); Black: linker; Pink: HIV-1 inhibitor(HY-163852) .

HY-161633

PROTAC EGFR degrader 11	PROTACs EGFR FAK	Cancer
PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC₅₀ <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a K_i of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC₅₀ <100 nM.

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-101488

CC-885 10+ Cited Publications	Molecular Glues Ligands for E3 Ligase	Cancer
CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity. CC-885 is also a known degrader of GSPT1, inhibiting protein translation.

HY-146237

Golcadomide CC-99282	Ligands for E3 Ligase Molecular Glues	Cancer
Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL) .

HY-158045

PROTAC PARP1 degrader-1	PROTACs PARP	Inflammation/Immunology Cancer
PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) .

HY-159098

dWIZ-1	Molecular Glues Histone Acetyltransferase	Others
dWIZ-1 is a potent WIZ molecular glue degrader. dWIZ-1 recruitments WIZ(ZF7) to cereblon (CRBN) induces WIZ degradation. dWIZ-1 has the potential for the research of sickle cell disease (SCD) .

HY-150839

E3 ligase Ligand PG	Ligands for E3 Ligase	Cancer
E3 ligase Ligand PG is a E3 ligase ligand that can be used in the recruitment of *CRBN* protein. E3 ligase Ligand PG exhibits potent binding activity with CRBN (IC₅₀ of 2.191 μM). E3 ligase Ligand PG can be connected to the BMS-202 (HY-19745) by a linker to form PROTAC, PROTAC PD-L1 degrader-1 (HY-163757) .

Cat. No.	Product Name

HY-L918

Molecular Glue-like Compound Library

320 compounds

Targeted Protein Degradation (TPD) is a novel and promising approach to drug development. It shows great potential for targeting proteins traditionally considered "undruggable" due to the lack of enzymatic function and absence of binding sites by tagging them for degradation or recruiting natural degradation mechanisms.

Molecular glues are a type of small-molecule degraders that primarily induce novel interactions between E3 ubiquitin ligases and target proteins, forming ternary complexes that lead to protein ubiquitination and subsequent proteasomal degradation. Compared with PROTACs, molecular glues generally have lower molecular weights, higher cell permeability, and better drug-like properties. Additionally, the design of molecular glues is relatively simple, without the requirements for complex linkers and ligand optimization. As a result, molecular glues have gradually emerged as a promising therapeutic approach for various diseases.

Multiple types of molecular glues have been reported previously. Analysis of co-crystal complex structures reveals that CRBN-related molecular glues are more versatile. Therefore, MCE researchers select active molecules related to these targets as probes for artificial intelligence (AI) screening.Subsequently, molecular docking technology was used to verify whether the screened molecules retained the key pharmacophore features. Ultimately, we obtained 320 molecular glue analogs, and these compounds serve as powerful tools for the research of molecular glues.

HY-L128

E3 Ligase Ligand Library

87 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 87 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-169235

DHHC3 degrader 1	Ligands for Target Protein for PROTAC	Cancer
DHHC3 degrader 1 is a PROTAC target protein ligand that is used to synthesize PCC16 chloride (HY-169232) .

HY-169232

PCC16 chloride	PROTACs	Cancer
PCC16 chloride is a CRBN-based cp-PCC with an IC₅₀ value of 102 nM for the degradation of DHHC3. PCC16 chloride has antitumor activity. (Target protein ligand: HY-169235, linker: HY-169236, E3 ligase ligand: HY-10984) .

Cat. No.	Product Name	Chemical Structure

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 .

HY-126534S

Abemaciclib metabolite M18-d8
Abemaciclib metabolite M18-d₈ is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .

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 .

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 .

Cat. No.	Product Name		Classification

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.

HY-130504

Propargyl-PEG1-acid 1 Publications Verification		PROTAC Synthesis Alkynes
Propargyl-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-CRBN PROTACs Ibrutinib(HY-10997)-based PROTAC 4 and PROTAC 5. PROTAC 5 causes the degradation of BTK and induces the degradation of CSK, LYN, and LAT2 at 10 μM . Propargyl-PEG1-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-159087

RGB110		Azide
RGB110 (Compound 10d) is a PROTAC inhibitor for D-dopachrome tautomerase with an IC₅₀ of 5.9 μM. RGB110 causes no degradation of D-DT. (Pink: ligand for target protein (HY-159164); Black: linker (HY-W125017); Blue: ligand for E3 ligase CRBN (HY-10984))

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