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Results for "

cereblon E3 ubiquitin ligase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (10) Ligands for E3 Ligase (17) Apoptosis (11) Autophagy (4) BCL6 (1) Btk (2) CDK (2) Epigenetic Reader Domain (1) FKBP (1) Isotope-Labeled Compounds (1) Molecular Glues (8) PROTACs (7) Sirtuin (1) STAT (1)
By Research Areas:	Cancer (35) Inflammation/Immunology (7)
Click Chemistry:	Azide (4)

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Click Chemistry

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

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-153357

NRX-0492	Btk	Cancer
NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC₅₀≤0.2 nM and DC₉₀≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex .

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 .

HY-144980

E3 ligase Ligand 21

Ligands for E3 Ligase Cancer

E3 ligase Ligand 21 (compound 2) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .

E3 ligase Ligand 21	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 21 (compound 2) is a *cereblon* binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .

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 .

HY-144985

E3 ligase Ligand 23	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 23 (compound 17-6) is a *cereblon* binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .

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-129395

Mezigdomide CC-92480	E1/E2/E3 Enzyme Molecular Glues Apoptosis	Cancer
Mezigdomide (CC-92480), a cereblon E3 ubiquitin ligase modulating agent (CELMoD), acts as a molecular glue. Mezigdomide shows high affinity to cereblon, resulting in potent antimyeloma activity .

HY-131863

Pomalidomide 4'-alkylC8-acid	Ligands for E3 Ligase Apoptosis Molecular Glues	Cancer
Pomalidomide 4'-alkylC8-acid is an *E3 ubiquitin* ligase ligand-Linker conjugate** containing Pomalidomide (HY-10984). Pomalidomide is a third-generation immunomodulator that acts like a molecular glue. Pomalidomide interacts with the E3 ligase cereblon to induce degradation of the essential Ikaros transcription factor .

HY-139336

Pomalidomide-C5-azide	E3 Ligase Ligand-Linker Conjugates	Others
Pomalidomide-C5-azide is an E3 ubiquitin ligase cereblon (CRBN) ligand-Linker conjugate. The azide group can undergo a click chemical reaction .

HY-123937

THAL-SNS-032 2 Publications Verification	PROTACs CDK	Cancer
THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase *Cereblon* (CRBN) .

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-153220A

(R)-NX-2127	Btk	Inflammation/Immunology Cancer
(R)-NX-2127 (compound 28) is an orally active Bruton’s Tyrosine Kinase (Btk) degrader. (R)-NX-2127 degrades IKZF1 and IKZF3 by molecular glue interactions with the cereblon E3 ubiquitin ligase complex .

HY-136160

Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride	E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis	Cancer
Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a linker. Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride can be used to design the PROTACs .

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-130835

FKBP12 PROTAC RC32 RC32	PROTACs FKBP	Cancer
FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an *Cereblon* E3 ubiquitin ligase (Pomalidomide; HY-10984) .

HY-157510

Thalidomide-O-C3-azide	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-O-C3-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C3-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C3-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-157511

Thalidomide-O-C5-azide	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-O-C5-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C5-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C5-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-157515

Thalidomide 4'-ether-PEG2-azide	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide 4'-ether-PEG2-azide is a click chemistry modified cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide 4'-ether-PEG2-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkynyl groups. Thalidomide 4'-ether-PEG2-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-155269

Pomalidomide-5-C13-NH2 hydrochloride	Ligands for E3 Ligase	Cancer
Pomalidomide-5-C13-NH2 hydrochloride is a Pomalidomide (HY-10984)-based E3 ubiquitin ligase cereblon (CRBN) ligand for recruiting cereblon proteins. Pomalidomide-5-C13-NH2 hydrochloride can be connected to protein ligands through a linker to form PROTAC.

HY-112811

PROTAC CDK9 degrader-2	PROTACs CDK	Cancer
PROTAC CDK9 degrader-2 (compound 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC₅₀ of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase *Cereblon* (CRBN) via a linker to form PROTAC .

HY-123844

dBET57 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
dBET57 is a potent and selective degrader of BRD4_BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4 ^Cereblon E3 ubiquitin ligase, with a DC_50/5h of 500 nM for BRD4_BD1, and is inactive on BRD4_BD2 .

HY-14658

Thalidomide 10+ Cited Publications	E3 Ligase Ligand-Linker Conjugates 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-163210

Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride	Ligands for E3 Ligase	Cancer
Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride (ZJT1) is an E3 ubiquitin ligase cereblon based on Pomalidomide (HY-10984) (CRBN) ligand for recruitment of cereblon protein. Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride can be linked to protein ligand by linker to form PROTAC .

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-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 .

HY-A0003

Lenalidomide Maximum Cited Publications 32 Publications Verification 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 .

HY-A0003B

Lenalidomide hemihydrate Maximum Cited Publications 32 Publications Verification 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 .

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 .

HY-A0003S

Lenalidomide-d5 CC-5013-d₅	Isotope-Labeled Compounds Ligands for E3 Ligase Molecular Glues Apoptosis	Inflammation/Immunology Cancer
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][2].

HY-103636

PROTAC Sirt2 Degrader-1	Sirtuin PROTACs	Cancer
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide *Cereblon* ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC₅₀ of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC₅₀s>100 μM) .

HY-130683

Lenalidomide-propargyl-C2-NH2 hydrochloride	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) . 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-130682

Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312) . Lenalidomide-propargyl-C2-amido-Ph-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-158105

ARV-393	PROTACs BCL6	Cancer
ARV-393 is an orally active PROTAC that utilizes the ubiquitin-proteasome system to target the degradation of BCL6. ARV-393 consists of ligand conjugates targeting BCL6 and the E3 ligase cereblon, respectively. ARV-393 has DC₅₀ and GI₅₀ values of <1 nM in multiple cell lines of diffuse large B-cell lymphoma (DLBCL) and Burkitt lymphoma (BL). ARV-393 also demonstrated considerable tumor suppressor activity in tumor xenograft models. ARV-393 is being studied to inhibit non-Hodgkin lymphoma.

HY-161131

Lenalidomide 4'-alkyl-C3-azide	Ligands for E3 Ligase Apoptosis Molecular Glues	Inflammation/Immunology
Lenalidomide 4'-alkyl-C3-azide (compound 4a) is a click chemical modified Lenalidomide (HY-A0003) that can be used to synthesize PROTACs. Lenalidomide is an orally active immunomodulator and a ligand for the ubiquitin E3 ligase cereblon (CRBN). Lenalidomide 4'-alkyl-C3-azide contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition reactions (SPAAC) can also occur with molecules containing DBCO or BCN groups .

HY-129602

SD-36 5 Publications Verification	PROTACs STAT Apoptosis	Cancer
SD-36 is a potent and efficacious STAT3 PROTAC degrader (K_d=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC₅₀=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of *Cereblon* ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

E3 Ligase Ligand Library	88 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 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.

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].

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][2].

Cat. No.	Product Name		Classification

HY-157510

Thalidomide-O-C3-azide		Azide
Thalidomide-O-C3-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C3-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C3-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-157511

Thalidomide-O-C5-azide		Azide
Thalidomide-O-C5-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C5-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C5-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-157515

Thalidomide 4'-ether-PEG2-azide		Azide
Thalidomide 4'-ether-PEG2-azide is a click chemistry modified cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide 4'-ether-PEG2-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkynyl groups. Thalidomide 4'-ether-PEG2-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-161131

Lenalidomide 4'-alkyl-C3-azide		Azide
Lenalidomide 4'-alkyl-C3-azide (compound 4a) is a click chemical modified Lenalidomide (HY-A0003) that can be used to synthesize PROTACs. Lenalidomide is an orally active immunomodulator and a ligand for the ubiquitin E3 ligase cereblon (CRBN). Lenalidomide 4'-alkyl-C3-azide contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition reactions (SPAAC) can also occur with molecules containing DBCO or BCN groups .

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