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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 (13) Ligands for E3 Ligase (19) Aldose Reductase (1) Apoptosis (15) Autophagy (5) Btk (1) CDK (2) Epigenetic Reader Domain (1) FKBP (1) FLT3 (1) IKZF Family (1) Isotope-Labeled Compounds (3) MDM-2/p53 (1) Molecular Glues (11) PROTACs (9) Reference Standards (1) Sirtuin (1) STAT (1) α-synuclein (1)
By Research Areas:	Cancer (42) Inflammation/Immunology (10) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (1) 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 ByeTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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 .

HY-131863

Pomalidomide 4'-alkylC8-acid	E3 Ligase Ligand-Linker Conjugates	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-176470

Thalidomide-N-C-piperidine-C7-Br	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-N-C-piperidine-C7-Br, an *E3 ligase* ligand-linker conjugate*, incorporates a cereblon* (CRBN) ligand for the E3 ubiquitin ligase and a linker. Thalidomide-N-C-piperidine-C7-Br can be used in the synthesis of ZS3-046 (HY-176457) .

HY-123937

THAL-SNS-032 5+ Cited Publications	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-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-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-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-174266

WB156	MDM-2/p53	Cancer
WB156 is a dual MDM2 and GSPT1 degrader. WB156 can recruit CRBN (Cereblon, a substrate receptor of the E3 ubiquitin-ligase complex) to induce the ubiquitination-proteasome pathway-mediated degradation of MDM2 and GSPT1. WB156 is promising for research of cancers, such as leukemia .

HY-155269

Pomalidomide-5-C13-NH2 hydrochloride	E3 Ligase Ligand-Linker Conjugates	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-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-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-14658

Thalidomide 15+ Cited Publications	Ligands for E3 Ligase Autophagy Apoptosis Molecular Glues	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 .

HY-123844

dBET57 3 Publications Verification	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
dBET57 is an effective and selective BRD4_BD1 degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4 ^Cereblon, showing a DC_50/5h value of 500 nM for BRD4_BD1 .

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-A0003B

Lenalidomide hemihydrate Maximum Cited Publications 45 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-A0003

Lenalidomide Maximum Cited Publications 45 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-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-14658R

Thalidomide (Standard)	Ligands for E3 Ligase Autophagy Apoptosis Reference Standards	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-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 .

HY-173630

BMS-986449	Molecular Glues IKZF Family	Cancer
BMS-986449 is a CELMoD molecular glue and an IKZF2/IKZF4 degrader. BMS-986449 targets the degradation of transcription factors Helios (IKZF2) and Eos (IKZF4) in regulatory T (Treg) cells. BMS-986449 redirects the E3 ubiquitin ligase Cereblon to induce the degradation of Helios and Eos, reprogramming Treg cells and enhancing antitumor immunity. BMS-986449 is promising for research of advanced solid tumors .

HY-157839

PROTAC α-synuclein degrader 6	α-synuclein	Neurological Disease
PROTAC α-synuclein degrader 6 (compound T3) is a PROTAC degrader of α-synuclein and tau, with EC₅₀ of 1.57 μM and 4.09 μM, respectively. PROTAC α-synuclein degrader 6 plays an important role in neurodegenerative diseases (NDs) research (Blue:ubiquitin E3 ligase cereblon ligand (HY-14658), Black: linker (HY-128803); Pink: Ligand for target protein (HY-151035)) .

HY-A0003R

Lenalidomide (Standard)	Ligands for E3 Ligase Molecular Glues Apoptosis	Inflammation/Immunology Cancer
Lenalidomide (Standard) is the analytical standard of Lenalidomide. This product is intended for research and analytical applications. 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-157213

LWY713	Apoptosis PROTACs FLT3	Cancer
LWY713 is a PROTAC-class FLT3 degrader (DC₅₀=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).

HY-A0003S2

Lenalidomide-13C5,15N CC-5013-¹³C₅,¹⁵N	Ligands for E3 Ligase Apoptosis Molecular Glues Isotope-Labeled Compounds	Inflammation/Immunology Cancer
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 CC-5013-d₄	Isotope-Labeled Compounds Apoptosis Molecular Glues Ligands for E3 Ligase	Inflammation/Immunology Cancer
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 .

HY-103636

PROTAC Sirt2 Degrader-1 1 Publications Verification	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-161131

Lenalidomide 4'-alkyl-C3-azide	E3 Ligase Ligand-Linker Conjugates	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-163609

PROTAC AKR1C3 degrader-1	PROTACs Aldose Reductase	Cancer
PROTAC AKR1C3 degrader-1 (compound 5) is a potent AKR1C3 PROTAC degrader. PROTAC AKR1C3 degrader-1 decreases the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTAC AKR1C3 degrader-1 has the potential for the research of prostate cancer. (Blue:ubiquitin E3 ligase cereblon ligand (HY-A0003), Black: linker (HY-163647); Pink: AKR1C3 inhibitor (HY-163610)) .

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.

HY-153357

NRX-0492	PROTACs Btk	Cancer
NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC₅₀ ≤ 0.2 nM, DC₉₀ ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 has antitumor effects against chronic lymphocytic leukemia.NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263).

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library

92 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 92 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	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-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 .

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