Search Result
Results for "
CRBN Degrader
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-128845
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PROTACs
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Cancer
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PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader .
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- HY-130714
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TD-165
1 Publications Verification
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PROTACs
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Cancer
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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 .
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- HY-132857A
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PROTACs
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Neurological Disease
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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 .
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- HY-130800
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- HY-132288
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-162014
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PROTACs
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Cancer
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WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1 .
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- HY-169077
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Molecular Glues
IKZF Family
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Cancer
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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 .
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- HY-163757
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PROTACs
PD-1/PD-L1
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Inflammation/Immunology
Cancer
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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)) .
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- HY-151886
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PROTACs
Indoleamine 2,3-Dioxygenase (IDO)
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Neurological Disease
Cancer
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NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd 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) .
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- HY-126534
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- HY-122725A
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-129775
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Target Protein Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-129776
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Target Protein Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-130991
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Target Protein Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-153341
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PROTACs
Raf
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Cancer
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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 .
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- HY-136262
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PROTACs
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Cancer
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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 .
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- HY-132857
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PROTACs
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Neurological Disease
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ZXH-4-130 is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC) .
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- HY-132862
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PROTACs
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Cancer
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ZXH-4-137 is a potent and selective CRBN degrader (PROTAC).
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- HY-157426
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- HY-160531
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Molecular Glues
IKZF Family
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Cancer
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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 .
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- HY-111594
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PROTACs
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Cancer
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Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3 .
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- HY-158325
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PROTACs
FLT3
Apoptosis
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Cancer
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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) .
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- HY-143435
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Apoptosis
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Cancer
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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 .
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- HY-156591
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PROTACs
Mixed Lineage Kinase
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Others
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PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC degrader of MLKL, with a Dmax >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.
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- HY-114406
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Ligands for E3 Ligase
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Cancer
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TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .
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- HY-158381
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PROTACs
Phosphatase
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Metabolic Disease
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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) .
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- HY-139186
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PROTACs
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Cancer
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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 .
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- HY-164891
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Molecular Glues
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Others
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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 .
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- HY-163168
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CFT-4531
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PROTACs
DNA/RNA Synthesis
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Cancer
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aTAG 4531 (CFT-4531) is a potent, selective, and onmechanism tool degrader of MTH1 with DC50 value of 0.28 nM and Ki 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) .
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- HY-151902
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PROTACs
JAK
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Cancer
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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) .
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- HY-133144
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Ligands for E3 Ligase
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Cancer
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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) .
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- HY-161536
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PROTACs
EGFR
Apoptosis
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Cancer
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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 Kd 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)) .
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- HY-161696
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Apoptosis
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Cancer
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AN5777 is a GSPT1 degrader. AN5777 significantly reduces GSPT1 through the ubiquitin-proteasome system. AN5777 induces G1 block and Apoptosis. AN5777 has antitumor activity .
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- HY-169235
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- HY-153803
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PROTACs
Molecular Glues
Btk
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Cancer
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GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1. GBD-9 effectively inhibits cancer cell growth .
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- HY-131318
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Ligands for E3 Ligase
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Cancer
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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) .
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- HY-43722
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Ligands for E3 Ligase
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Cancer
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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) .
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- HY-161633
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PROTACs
EGFR
FAK
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Cancer
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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 Ki 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.
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- HY-163851
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PROTACs
HIV
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Infection
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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-1IIIB). Blue: CRBN ligand (HY-10984); Black: linker; Pink: HIV-1 inhibitor(HY-163852) .
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- HY-146237
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CC-99282
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Ligands for E3 Ligase
Molecular Glues
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Cancer
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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) .
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- HY-101488
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- HY-159098
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Molecular Glues
Histone Acetyltransferase
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Others
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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) .
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- HY-150839
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Ligands for E3 Ligase
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Cancer
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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) .
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- HY-158045
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PROTACs
PARP
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Inflammation/Immunology
Cancer
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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) .
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- HY-161632
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PROTACs
EGFR
FAK
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Cancer
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PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM .
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- HY-112811
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PROTACs
CDK
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Cancer
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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 .
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- HY-145776
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- HY-141481
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PROTACs
EGFR
PARP
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Cancer
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DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP .
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-
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- HY-141486
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Target Protein Ligand-Linker Conjugates
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Cancer
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(Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP .
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- HY-125876
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PROTACs
Bcl-2 Family
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Cancer
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PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker;Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
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- HY-153321
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BTK-IN-24
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Btk
PROTACs
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Inflammation/Immunology
Cancer
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NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
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- HY-163938
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PROTACs
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Cancer
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PROTAC erf3a Degrader-1 (Compound C63) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-1 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-1 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: CRBN ligand (HY-41547)) .
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- HY-155072
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PROTACs
Btk
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Cancer
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PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research (Blue: E3 ligand (HY-W440230), Black: linker HY-168297;Pink:BKT inhibitor (HY-150898)) 1.
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- HY-145226
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PROTACs
Epigenetic Reader Domain
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Cancer
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XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4BD1L94V degrader. XY-06-007 shows a DC50, 6 h of 10 nM against BRD4BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies .
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- HY-115881
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PROTACs
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Cancer
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SR-1114 is a first-in-class PROTAC ENL degrader. SR-1114 elicits rapid, CRBN-dependent degradation of ENL with DC50s of 150 nM, 311 nM, and 1.65 μM in MV4;11 , MOLM-13, and OCI/AML-2 cells, respectively .
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- HY-123937
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PROTACs
CDK
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Cancer
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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) .
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- HY-41547
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Cereblon ligand 4; E3 ligase Ligand 4
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Ligands for E3 Ligase
Autophagy
Apoptosis
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Cancer
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Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966) .
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- HY-130707
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Target Protein Ligand-Linker Conjugates
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Cancer
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K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
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- HY-130822
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Target Protein Ligand-Linker Conjugates
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Cancer
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K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
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- HY-130823
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Target Protein Ligand-Linker Conjugates
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Cancer
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K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
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- HY-168274
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PROTACs
Apoptosis
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Cancer
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PROTAC TRIB2 degrader-1 (Compound 5k) is an effective TRIB2 degrader that selectively induces TRIB2 degradation through the CRBN-dependent ubiquitin-proteasome pathway. PROTAC TRIB2 degrader-1 can inhibit cell proliferation and induce cell apoptosis, and can be used in cancer research. (Target protein ligand (Pink): HY-168275; linker (black): HY-168276; E3 Ligase Ligand-Linker Conjugates: HY-168277; E3 ligase (Blue): HY-W023573) .
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- HY-139344
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FAK
PROTACs
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Cancer
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FC-11 is a PROTAC FAK degrader (DC90: 1 nM) . FC-11 contains CRBN ligand Pomalidomide (HY-10984), linker and FAK ligand PF562271 (HY-10459) .
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- HY-149845
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GSK-3
PROTACs
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Neurological Disease
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PROTAC GSK-3β Degrader-1 (compound 1) is a degrader targets GSK-3β degradation with an IC50 value of 833 nM. PROTAC GSK-3β Degrader-1 contains SB-216763 (a GSK-3β inhibitor), a PEG linker and a CRBN (E3 ligase liand). PROTAC GSK-3β Degrader-1 reduces the neurotoxicity induced by Aβ25-35 peptide and CuSO4. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease .
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- HY-161675
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-5-bromopentanamide is an E3 ligase ligand-linker conjugate in PROTAC ATR degrader-2 (HY-161615), and consists of a CRBN ligand Lenalidomide (HY-A0003) and a linker 5-Bromopentanoyl chloride (HY-43538). Lenalidomide-5-bromopentanamidecan be used for synthesis of PROTACs .
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- HY-114421
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dTAG-13
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PROTACs
FKBP
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Cancer
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FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12 F36V and CRBN, thereby selectively degrading FKBP12 F36V .
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- HY-144998
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Molecular Glues
IKZF Family
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Inflammation/Immunology
Cancer
|
NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2 .
|
-
- HY-155008
-
|
PROTACs
Hexokinase
|
Cancer
|
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .
|
-
- HY-115997
-
|
PROTACs
HSP
|
Cancer
|
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-130713
-
-
- HY-168614
-
|
IKZF Family
|
Cancer
|
MGD-4 is an orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=67.2 nM), IKZF2 (DC50=918.2 nM), and IKZF3 (DC50=95.8 nM) in a dose-dependent manner. MGD-4 effectively inhibits the growth of multiple myeloma .
|
-
- HY-133137
-
|
PROTACs
Btk
|
Cancer
|
SJF620 is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .
|
-
- HY-133137A
-
|
PROTACs
Btk
|
Cancer
|
SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .
|
-
- HY-157767
-
|
PROTACs
ATM/ATR
|
Cancer
|
Abd110 (compound 42i) is a Lenalidomide-based PROTAC ATR kinase degrader. Abd110 selectively decreases ATR and phospho-ATR without affecting related kinases ATM and DNA-PKcs .
|
-
- HY-130612
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
|
-
- HY-131232
-
Desmorpholinyl ABT-263-NH-Me
|
Bcl-2 Family
Ligands for Target Protein for PROTAC
|
Cancer
|
Desmorpholinyl Navitoclax-NH-Me is a Bcl-xL inhibitor. Desmorpholinyl Navitoclax-NH-Me and a CRBN ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC BCL-XL degrader XZ739 (HY-133557) .
|
-
- HY-137206
-
|
Molecular Glues
Ligands for E3 Ligase
|
Cancer
|
ALV2 is a potent and selective Helios molecular glue degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment .
|
-
- HY-W760183
-
|
Fluorescent Dye
|
Cancer
|
EM12-SO2F is a powerful covalent inhibitor of CRBN through binding at His353. EM12-SO2F is a useful chemical probe to investigate the CRBN. EM12-SO2F inhibits the degradation of IKZF1 by lenalidomide (HY-A0003) in MOLT4 cells
|
-
- HY-W998345
-
|
PROTACs
PDK-1
Akt
|
Cancer
|
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .
|
-
- HY-130981
-
-
- HY-158239
-
|
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717) .
|
-
- HY-44148
-
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation .
|
-
- HY-126534A
-
LSN3106729 hydrochloride
|
Ligands for Target Protein for PROTAC
CDK
|
Cancer
|
Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
|
-
- HY-126534S
-
LSN3106729-d8
|
CDK
Ligands for Target Protein for PROTAC
|
Cancer
|
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[1][2].
|
-
- HY-161574
-
|
PROTACs
Histone Methyltransferase
|
Cancer
|
LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)) .
|
-
- HY-168615
-
|
IKZF Family
Casein Kinase
|
Cancer
|
MGD-28 is a potent, orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=3.8 nM), IKZF2 (DC50=56.3 nM), and IKZF3 (DC50=7.1 nM) in a dose-dependent manner. In addition, MGD-4 also degrades CK1α (DC50=7.8 nM). MGD-28 has antiproliferative activity and can be used in multiple myeloma research .
|
-
- HY-136688
-
|
PROTACs
|
Cancer
|
MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4 CRBN E3 ligase .
|
-
- HY-161654
-
|
PROTACs
Ras
|
Cancer
|
PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))
|
-
- HY-114407
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50?of?0.32?nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .
|
-
- HY-122653
-
|
PROTACs
|
Cancer
|
CCT367766 is a potent and the third generation?heterobifunctional and Cereblon-based pirin targeting protein?degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an?IC50?value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with?Kd?values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein .
|
-
- HY-122653A
-
|
PROTACs
|
Cancer
|
CCT367766 formic is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 formic exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 formic reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 formic provides a potential chemical tool to study a largely unexplored protein .
|
-
- HY-145765
-
-
- HY-169232
-
|
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-147858A
-
|
PROTACs
|
Cancer
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/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 .
|
-
- HY-148276
-
|
PROTACs
IRAK
|
Cancer
|
KTX-497 is an IRAK4 PROTAC degrader with a DC50 value of 3 nM. KTX-497 can be used for the research of oncology .(Pink:IRAK4 inhibitor (HY-150735); Black: linker; Blue: CRBN Ligand (HY-10984))
|
-
- HY-153959
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Thalidomide-O-amido-C11-COOH (compound IMiD acid 1) is an E3 ligase ligand and linker CRBN (Cereblon) conjugate. Thalidomide-O-amido-C11-COOH can be used to synthesize PROTAC that target the degradation of DOT1L .
|
-
- HY-131717A
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Thalidomide-NH-CH2-COOH TFA is a ligand-linker conjugate for the E3 ligase Cereblon (CRBN). Thalidomide-NH-CH2-COOH TFA can be conjugated to multi-targeted kinase inhibitors to transform them into selective degraders .
|
-
- HY-123941
-
dTAG-7
|
PROTACs
FKBP
Epigenetic Reader Domain
|
Cancer
|
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN .
|
-
- HY-122725B
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Lenalidomide-C5-NH2 hydrochloride 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-A0003
-
Lenalidomide
Maximum Cited Publications
39 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
-
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
-
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-148277
-
|
PROTACs
IRAK
|
Cancer
|
KTX-612 is an orally active IRAK4 PROTAC degrader with a DC50 value of 7 nM. KTX-612 can be used for the research of oncology .(Pink:IRAK4 inhibitor (HY-150735); Black: linker; Blue: CRBN Ligand (HY-10984))
|
-
- HY-153166
-
|
PROTACs
GSK-3
|
Neurological Disease
|
PT-65 is a potent and selective GSK3 PROTAC degrader with the highest degradation capacity of GSK3α (DC50= 28.3 nM) and GSK3β (DC50= 34.2 nM) in SH-SY5Y cells. PT-65 can be used in Alzheimer's disease research .(Pink: GSK3 inhibitor (HY-15761); Black: linker; Blue: CRBN Ligand (HY-10984))
|
-
- HY-147858
-
|
PROTACs
EGFR
Apoptosis
|
Cancer
|
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-160695
-
|
Ligands for E3 Ligase
Molecular Glues
|
Cancer
|
PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms .
|
-
- HY-147158
-
|
Molecular Glues
Ligands for E3 Ligase
|
Cancer
|
ZXH-1-161 is a potent cereblon (CRBN) modulator with an IC50 value of 39 nM in MM1.S wild type cells. ZXH-1-161 has selective degradation activity towards GSPT1. ZXH-1-161 can be used for researching multiple myeloma .
|
-
- HY-169362
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Lenalidomide-Pip-butyn is Lenalidomide (HY-A0003)-based E3 ligase ligand-linker conjugate, and is used in the recruitment of CRBN protein. Lenalidomide-Pip-butyn can be connected to the ligand for protein to form PROTACs, such as the PROTAC STAT3 degrader SD-436 (HY-169360) .
|
-
- HY-158101
-
CC-94676
|
PROTACs
Androgen Receptor
|
Cancer
|
BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader, capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. (Blue: HY-W247437; Black: linker (HY-W126831); Pink: HY-168697) .
|
-
- HY-130504
-
|
PROTAC Linkers
|
Cancer
|
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-131295
-
|
MEK
Ligands for Target Protein for PROTAC
|
Cancer
|
PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader .
|
-
- HY-148275
-
|
PROTACs
IRAK
|
Cancer
|
KTX-955 is an antumor and effective IRAK4 degrader, with DC50 values of 5 nM and 130 nM for IRAK4 and Ikaros, respectively . KTX-955 is composed of CRBN ligand (blue part) Pomalidomide (HY-10984) and target protein ligand (red part) IRAK4-IN-20 (HY-150735).
|
-
- HY-122830
-
|
PROTACs
Btk
|
Cancer
|
DD-03-171 is a BTK PROTAC degrader, the BTK IC50 a value of 5.1 nM. DD-03-171 has an antiproliferative effect on mantle cell lymphoma (MCL) cells . (Pink: BTK inhibitor (HY-168292); Black: linker (HY-28875); Blue: CRBN Ligand (HY-131717))
|
-
- HY-A0003S
-
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-149843
-
|
FGFR
PROTACs
|
Cancer
|
LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity .
|
-
- HY-157570
-
|
PROTACs
STING
|
Infection
|
Anti-inflammatory agent 70 (N-Me-SP23) is a STING protein PROTAC degrader and inhibits the STING signaling pathway. Anti-inflammatory agent 70 has anti-inflammatory activity. (Pink: STING inhibitor (HY-47709); Black: linker (HY-W008296); Blue: CRBN Ligand (HY-W460193)) .
|
-
- HY-A0003R
-
|
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-A0003S2
-
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-129603
-
|
STAT
Ligands for Target Protein for PROTAC
|
Cancer
|
SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36 .
|
-
- HY-134582
-
dCBP-1
3 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression .
|
-
- HY-161741
-
|
AUTOTACs
Androgen Receptor
|
Cancer
|
VinclozolinM2-2204 is a androgen receptor (AR) AUTOTAC degrader, with an DC50 of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR +LC3 + autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer .(Pink: AR inhibitor (HY-168296); Black: linker (HY-128833); Blue: CRBN Ligand (HY-168293))
|
-
- HY-162702
-
|
Androgen Receptor
PROTACs
|
Cancer
|
AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker) .
|
-
- HY-145281
-
|
PROTACs
Akt
|
Cancer
|
MS98 is a potent and selective PROTAC AKT degrader. MS98 depletes cellular total AKT (T-AKT) with the DC50 value of 78 nM. MS98 binds to AKT1, AKT2, and AKT3 with Kds of 4 nM, 140 nM, and 8.1 nM, respectively .
|
-
- HY-145282
-
|
PROTACs
Akt
|
Cancer
|
MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively .
|
-
- HY-137340
-
|
PROTACs
|
Cancer
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WH-10417-099 is a CRBN-type PROTAC multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases). WH-10417-099 induces protein degradation through the ubiquitin biotinylation (E-STUB) pathway and consists of the target protein ligand (red part) PI3Kγ ligand 1 (HY-168319), the E3 ubiquitin ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547) and the PROTAC linker (black part) Amino-PEG5-C2-acid (HY-115384). The E3 ligase ligand and linker can form a conjugate Pomalidomide 4'-PEG5-acid (HY-131647).
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- HY-162538
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NF-κB
IRAK
PROTACs
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Inflammation/Immunology
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LC-MI-3 is an orally active and potent interleukin-1 receptor-associated kinase 4 (IRAK4) PROTAC degrader, with a DC50 of 47.3 nM. LC-MI-3 effectively inhibits the activation of downstream NF-κB signaling. LC-MI-3 can be used for the research of acute and chronic inflammatory skin. (Blue: VHL ligand, Black: linker, Pink: CRBN ligand (HY-14658)) .
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- HY-143286
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PROTACs
FLT3
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Cancer
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PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia .
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- HY-148290
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PROTACs
IRAK
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Cancer
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KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader. KTX-951 has DC50 of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. TX-951 has antitumor activity.(Pink: IRAK4 ligand-12 (HY-48932); Black: Linker (HY-W382009); Blue: CRBN Ligand Pomalidomide (HY-10984))
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- HY-158062
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PROTACs
DNA/RNA Synthesis
Apoptosis
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Cancer
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LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research . (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).
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- HY-162704
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PROTACs
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Cancer
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JMV7048 is an effective PROTAC degrader targeting PXR (Pregnane X Receptor) with a DC50 of 379 nM. JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome. JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein in these cells, thereby significantly delaying cancer recurrence in vivo. JMV7048 is composed of the PXR agonist JMV6944 (HY-162738), linker (HY-162736), and Thalidomide 5-fluoride (HY-W087383) (Red: JMV6944; Blue: Thalidomide 5-fluoride ligand; Black: linker) .
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- HY-141881
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PROTACs
Apoptosis
SF3B1
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Cancer
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PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells .
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- HY-143286A
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PROTACs
FLT3
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Cancer
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PF15 TFA is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 TFA is a high selective FLT3-ITD degrader,with a DC50 of 76.7 nM. PF15 TFA significantly inhibits the proliferation of FLT3-ITD-positive cells,can down-regulate the phosphorylation of FLT3 and STAT5. PF15 TFA also inhibits tumor growth in mouse models and can be used in study of leukemia .
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- HY-148333
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MS177
1 Publications Verification
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PROTACs
Histone Methyltransferase
Apoptosis
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Cancer
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MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12?nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest .
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- HY-158113
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Histone Acetyltransferase
PROTACs
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Cancer
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CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
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- HY-133557
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PROTACs
Bcl-2 Family
Apoptosis
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Cancer
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XZ739, a Cereblon-dependent PROTAC BCL-XL (Bcl-2 family member) degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis .
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- HY-139996
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PROTACs
Apoptosis
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
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Cancer
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Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD + acute myeloid leukemia .
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- HY-161250
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PROTACs
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Cancer
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Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (compound 22 (dCE-1)) is a CBP/EP300 degrader, which contains a CRBN ligands Pomalidomide, a 24-atom linker with 6 PEG units and a HAT inhibitor CPI-1612. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 exhibits antiproliferative effects in cells multiple myeloma cells LP1 (with a DC50 of 1.2 μM), MM1S and various cancer cell lines, especially the leukemia cells .
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- HY-137465
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PROTACs
Trk Receptor
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Cancer
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CG428 is a potent and selective tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC50 = 2.9 nM) .(Pink: TRK inhibitor (HY-118271); Black: linker (HY-W067489); Blue: CRBN Ligand (HY-41547))
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- HY-145925C
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PROTACs
Epigenetic Reader Domain
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Cancer
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(S,R)-CFT8634 (compound 176) is a selective and orally active PROTAC-class BRD9 protein degrader. (S,R)-CFT8634 has the potential to study BRD9-mediated diseases, including but not limited to abnormal cell proliferation. (S,R)-CFT8634 consists of a target protein ligand (red part) BRD9 ligand-5 (HY-169988), an E3 ligase ligand (blue part) CRBN ligand-11 (HY-169989), and a PROTAC linker (black part) 1-(3,3-Difluoro-4-piperidinyl)piperazine (HY-169991). E3 ligase ligand and linker can form E3 Ligase Ligand-linker Conjugate 142 (HY-169990) .
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HY-L128
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54 compounds
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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 54 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.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-169235
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- HY-169232
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PROTACs
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Cancer
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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) .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-126534S
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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[1][2].
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- HY-A0003S
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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].
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- HY-A0003S2
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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 .
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Cat. No. |
Product Name |
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Classification |
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- HY-147858
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Alkynes
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PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-130504
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PROTAC Synthesis
Alkynes
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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.
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