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CRBN Degrader

" in MedChemExpress (MCE) Product Catalog:

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研究分野別:	Cancer (337) Cardiovascular Disease (8) Endocrinology (1) Infection (7) Inflammation/Immunology (50) Metabolic Disease (4) Neurological Disease (23)
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Oligonucleotides:	Pegylated Lipids (1)

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製品番号	製品名	Target	研究分野	構造式

HY-130800

Eragidomide 5+ Cited Publications 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-175742

BMS-986470	Molecular Glues Ligands for E3 Ligase Histone Acetyltransferase	Cardiovascular Disease
BMS-986470, a HbF-activating CRBN E3 ligase modulator (CELMoD), is an orally active dual molecular glue degrader targeting ZBTB7A and WIZ. BMS-986470 has potent γ-globin induction activity. BMS-986470 can be used for sickle cell disease (SCD) research .

HY-153341

Tagarafdeg CFT1946	PROTACs Raf	Cancer
Tagarafdeg (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. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF ^V600E splice variant. Tagarafdeg can be used in tumor research .

HY-163814

CDK2 degrader 1	Molecular Glues CDK	Cancer
CDK2 degrader 1 (Compound 3) is a selective CDK2 molecular glue degrader with a D_max (CDK2) of > 80% and a K_i (CRBN) > 1 μM. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers .

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-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-169912

CDK2 degrader 5	Molecular Glues CDK	Cancer
CDK2 degrader 5 is a CRBN-binding CDK2 molecular glue degrader. CDK2 degrader 5 induces ubiquitination and subsequent proteasomal degradation of CDK2. CDK2 degrader 5 can be used for the research of cancer .

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-176134

RP03707	PROTACs Ras	Cancer
RP03707 is a PROTAC degrader of KRAS ^G12D. RP03707 forms a ternary complex with KRAS ^G12D and the *CRBN* E3 ligase, promoting the ubiquitination and proteasomal degradation of KRAS ^G12D. RP03707 inhibits the growth of KRAS ^G12D-positive tumor cells .

HY-136262

CRBN-6-5-5-VHL 1 Publications Verification	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-139186

PROTAC KRAS G12C degrader-1	PROTACs Ras	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-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-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-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-132857A

ZXH-4-130 TFA 2 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 2 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-W453397

Aberrant tau ligand 1	Ligands for Target Protein for PROTAC Tau Protein	Cardiovascular Disease Neurological Disease
Aberrant tau ligand 1 is a tau protein ligand. Aberrant tau ligand 1 engages tau and *CRBN* to trigger proteasomal degradation. Aberrant tau ligand 1 can be used for synthesis PROTACs, such as QC-01–175 (HY-134850) .

HY-158342

PROTAC TEAD degrader-1	PROTACs YAP	Cancer
PROTAC TEAD degrader-1 is a TEAD2 degrader and antiproliferative agent with selective activity toward TEAD2 relative to other TEAD family members. PROTAC TEAD degrader-1 relies on *CRBN* and the proteasome system for TEAD2 degradation; disruption of *CRBN* binding attenuates this activity. PROTAC TEAD degrader-1 decreases expression of YAP target genes CYR61 and CTGF. PROTAC TEAD degrader-1 can be used for the research of NF2-deficient cancer .

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-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-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-142662A

PROTAC IRAK3 degrade-1 formic	PROTACs IRAK	Others
PROTAC IRAK3 degrader-1 formic is a potent and selective IRAK3 degrader with a DC₅₀ of 0.002 μM. PROTAC IRAK3 degrader-1 formic induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and *CRBN. PROTAC IRAK3 degrader*-1 formic can be used for cancer research .

HY-163502

PROTAC STAT3 degrader-3	PROTACs STAT	Cancer
PROTAC STAT3 degrader-3 is a STAT3 PROTAC degrader. PROTAC STAT3 degrader-3 recruits the E3 ubiquitin ligase *CRBN* and induces the degradation of STAT3 protein. PROTAC STAT3 degrader-3 inhibits the proliferation of malignant tumor cells. PROTAC STAT3 degrader-3 can be used for the research of non-small cell lung cancer and liver cancer .

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-168135

PROTAC c-Met degrader-1	PROTACs c-Met/HGFR	Cancer
PROTAC c-Met degrader-1 is a selective and orally active c-Met PROTAC degrader with a DC₅₀ of 6.21 nM against c-Met. PROTAC c-Met degrader-1 induces CRBN-dependent ubiquitination and proteasomal degradation of c-Met. PROTAC c-Met degrader-1 induces G0/G1 phase arrest in c-Met-dependent cancer cells. PROTAC c-Met degrader-1 kills c-Met-dependent cancer cells. PROTAC c-Met degrader-1 inhibits tumor growth in animal models. PROTAC c-Met degrader-1 can be used for the research of gastric cancer .

HY-132857

ZXH-4-130 2 Publications Verification	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-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-142662

PROTAC IRAK3 degrader-1	PROTACs IRAK	Cancer
PROTAC IRAK3 degrader-1 is a potent and selective IRAK3 degrader with a DC₅₀ of 0.002 μM. PROTAC IRAK3 degrader-1 induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and *CRBN. PROTAC IRAK3 degrader*-1 can be used for cancer research .

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-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-175600

MI-2-80	IKZF Family Casein Kinase Molecular Glues	Cancer
MI-2-80 is a molecular glue degrader. MI-2-80 induces proteins (such as IKZF1/3 and CSNK1A1) to bind to CRBN, promoting their ubiquitination and degradation .

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-178497

ZJK-807	PROTACs Ras p38 MAPK TNF Receptor	Inflammation/Immunology Cancer
ZJK-807 is a highly effective and selective PROTAC degrader targeting KRAS^G12D (DC₅₀ = 79.5 nM in AsPC-1 cells). ZJK-807 shows minimal impact on wild-type KRAS or other mutants (G12C/S/V, G13D), inducing mutant-specific cytotoxicity. ZJK-807 suppresses RAS/MAPK signaling and uniquely modulates TNF signaling and eukaryotic ribosome biogenesis. ZJK-807 can be used for the study of KRAS-driven pancreatic cancer. Yellow: KRAS^G12D ligand (HY-W087383); Green: E3 ligase CRBN ligand (HY-178507); Black: Linker (HY-178506) .

HY-W245311

E3 ligase Ligand 51	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 51 is the ligand for E3 ligase CRBN that can be used for synthesis of PROTAC BTK Degrader-12 (HY-170413) .

HY-141481

DP-C-4	PROTACs EGFR PARP	Cancer
DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP .

HY-173631

(S)-dHTC1	PROTACs	Cancer
(S)-dHTC1 is a molecular glue degrader targeting the transcriptional co-activator ENL. (S)-dHTC1 binds the ligase with high affinity only after forming the ENL:dHTC1 complex with an IC₅₀ value of 93 nM. (S)-dHTC1 degrades ENL in MV4;11 cells with a DC₅₀ value of 26 nM. (S)-dHTC1 can be used for acute myeloid leukemia study .

HY-170413

PROTAC BTK Degrader-12	PROTACs Btk	Cancer
PROTAC BTK Degrader-12 (EXAMPLE 19) is a PROTAC-based BTK degrader (Pink & black: BTK ligand & linker (HY-170414); Black: linker (HY-30105); Blue: CRBN ligand ( HY-W245311)) .

HY-177725

MG degrader 2	Molecular Glues PI4K	Cancer
MG degrader 2 (Compound CM-2) is a CRBN-dependent molecular glue degrader. MG degrader 2 induces ZFP91, FIZ1 and PI4KB degradation. MG degrader 2 has anti-proliferative activity against MM.1S cells (IC₅₀ = 162 nM). MG degrader 2 can be used for the research of cancer, such as multiple myeloma .

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-178518

Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine	E3 Ligase Ligand-Linker Conjugates E1/E2/E3 Enzyme	Cancer
Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine is an E3 ligase ligand-linker conjugate containing a cereblon (CRBN) ligand for E3 ubiquitin ligase and a linker. Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine can be used to synthesize PROTAC CDK4/6/9 degrader 2 (HY-178516) .

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-177724

GSPT1 degrader-11	Molecular Glues	Cancer
GSPT1 degrader-11 is a CRBN-dependent G1 to S phase transition 1 (GSPT1) molecular glue degrader (DC₅₀ = 67.7 nM, D_max = 97%). GSPT1 degrader-11 can inhibit MDA-MB-231 CRBN-WT cells proliferation (IC₅₀ = 2.07 μM). GSPT1 degrader-11 can be used for the research of cancer .

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-177928

Adavosertib acid AZD1775 acid; MK-1775 acid	Drug Intermediate Drug Derivative	Cancer
Adavosertib (AZD1775; MK-1775) acid (Compound 9) is a derivative of AZD1775 (HY-10993) and can be used for the synthesis of PROTAC .

HY-W1128213

IKZF2-degrader 2	Molecular Glues IKZF Family	Inflammation/Immunology Cancer
IKZF2-degrader 2 is a selective and orally active IKZF2 molecular glue degrader with DC₅₀ values of 0.5 nM and 1.8 nM in HiBit and FACS. The IKZF2-degrader 2 mediates the ubiquitination and degradation of target proteins by recruiting the CRL4-CRBN E3 ubiquitin ligase. IKZF2-degrader 2 displays moderate degradation against SALL4 with a DC₅₀ of 9 nM but does not induce any significant degradation towards IKZF1, IKZF3, CK1α and GSPT1. IKZF2-degrader 2 can be used for the study of cancer immunology .

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-175599

Z6466608628	Molecular Glues	Cardiovascular Disease Neurological Disease
Z6466608628 is a selective PPIL4 molecular glue degrader with human PPIL4 EC₅₀ values of 0.34 µM. Z6466608628 functionally recruits PPIL4 to *CRBN, induces CRL4 ^CRBN-mediated ubiquitylation and degradation* of PPIL4. Z6466608628 can be used for the research of intracranial aneurysms .

HY-177728

MG degrader 3	Molecular Glues E1/E2/E3 Enzyme	Cancer
MG degrader 3 (Compound CM-3) is a molecular glucose degrading agent that targets the *CRBN* protein. MG degrader 3 has certain anti proliferative activity in MM.1S cells (IC₅₀ = 8.7 nM). MG degrader 3 can be used for cancer research .

製品番号	製品名

HY-L934

CRBN Ligand Library

125 compounds

CRBN, namely cereblon, is the substrate recognition subunit of the E3 ubiquitin ligase complex in the ubiquitin-proteasome system. A CRBN ligand library refers to a collection of numerous fragments that can specifically bind to the CRBN protein.

These ligands are mostly designed based on validated CRBN-binding warheads and modified through AI-driven molecular generation optimization systems. They not only include classic lenalidomide-derived structures but also cover novel non-lenalidomide scaffolds. After drug-likeness filtering, these ligands exhibit structural diversity and favorable druggable properties. They can be further optimized and modified to facilitate the development of novel molecular glue degraders, accelerate the discovery of molecular glues that induce interactions between CRBN and new substrate proteins, and enable the exploration of novel CRBN substrates for identifying previously unknown CRBN-binding proteins.

MCE compiles 125 fragments that can specifically bind to the CRBN protein, with molecular weights ranging from 200 to 500. Compounds developed based on the library ligands target multiple disease targets such as cancer and autoimmune diseases, further advancing the development of Molecular Glues and PROTACs therapeutic agents.

HY-L918

Molecular Glue-like Compound Library

317 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 317 molecular glue analogs, and these compounds serve as powerful tools for the research of molecular glues.

HY-L128

E3 Ligase Ligand Library

174 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 174 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.

製品番号	製品名	Target	研究分野

HY-122542B

PPACK TFA 2 Publications Verification	Ligands for E3 Ligase Molecular Glues IKZF Family	Cardiovascular Disease
PPACK TFA is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK TFA binds to *CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (T_reg) into effector-like T cells, enhances CD8 ⁺ T cell responses, and modulates the T_eff:T_reg balance. PPACK TFA also increases the production of the inflammatory cytokine IL-2* and reduces the suppressive activity of T_reg. PPACK TFA can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1 .

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) .

HY-169235

DHHC3 ligand 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) .

製品番号	製品名	構造式

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 .

製品番号	製品名		Classification

HY-147858

PROTAC EGFR degrader 7		PROTAC Synthesis 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-115997

PROTAC HSP90 degrader BP3		PROTAC Synthesis
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a *CRBN*-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC₅₀=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 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-137342

SB1-G-187		PROTAC Synthesis
SB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with *CRBN* and specific functional kinases. SB1-G-187 can be used in tumor-related research. (Pink: multi-target kinase ligand (HY-125142); Blue: CRBN ligand (HY-A0003); Black: linker) .

HY-101460

Tz-Thalidomide		Tetrazine
Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research .

HY-130504

Propargyl-PEG1-acid 1 Publications Verification		Alkynes PROTAC Synthesis
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-178118

PROTAC PDIA1 degrader 1		Alkynes
PROTAC PDIA1 degrader 1 (Compound H4) is a PDIA1 PROTAC degrader with a DC₅₀ of 29.71 μM. PROTAC PDIA1 degrader 1 has potent anticancer activity and significantly inhibits cancer cell proliferation . Pink: PDIA1 ligand (HY-100433); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W015088)

HY-181043

CRBN ligand-895-PEG2-N3		Azide
CRBN ligand-895-PEG2-N3 (Compound 15) is a synthetic E3 ligase linker conjugate that can be used for the synthesis of PROTACs, such as PROTAC HDAC8 Degrader-4 (HY-181024) .

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))

製品番号	製品名		Classification

HY-174863

Pomalidomide-C2-PEG-NHCO-C2-COOH		Pegylated Lipids
Pomalidomide-C2-PEG-NHCO-C2-COOH is a conjugate of the CRBN ligand (HY-10984) and the linker (E3 Ligase Ligand-Linker Conjugate). Pomalidomide-C2-PEG-NHCO-C2-COOH can be used for synthesizing PROTAC ASK1 degrader dASK1 (HY-174862) .

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