2. Signaling Pathways
  3. PROTAC
  4. PROTACs

PROTACs

PROTACs

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PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.

PROTACs Isoform Specific Products:

PROTACs Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-181011
    PROTAC Cdc25 degrader-1
    PROTAC Cdc25 degrader-1 (Compound D3) is an efficient Cdc25 PROTAC degrader. Its DC50 values for Cdc25A, Cdc25B, and Cdc25C are 0.97, 2.02, and 4.67 μM respectively. PROTAC Cdc25 degrader-1 induces cell cycle arrest and apoptosis in cancer cells and inhibits cell migration ability. PROTAC Cdc25 degrader-1 significantly increases the ROS level. PROTAC Cdc25 degrader-1 can be used for the study of colorectal adenocarcinoma.
    PROTAC Cdc25 degrader-1
  • HY-169264
    SJYHJ-026
    SJYHJ-026 (compound 37) is a pregnane X receptor (PXR) PROTAC degrader with the DC50 of 86.6 nM and maximal degradation of 66.4%. SJYHJ-026 shows cell cytotoxic aganist SNU-C4 HiBiT-PXR KI cells with the IC50 values of 97.4 μM (24 h) and 99.5 μM (72 h).
    SJYHJ-026
  • HY-142662
    PROTAC IRAK3 degrader-1 2712600-00-3
    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.
    PROTAC IRAK3 degrader-1
  • HY-181413
    PROTAC EZH2 Degrader-44 3093642-25-9
    PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer.
    PROTAC EZH2 Degrader-44
  • HY-162098
    PROTAC tubulin-Degrader-1
    PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)).
    PROTAC tubulin-Degrader-1
  • HY-111842
    PROTAC CRABP-II Degrader-3 1225383-41-4
    PROTAC CRABP-II Degrader-3 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand.
    PROTAC CRABP-II Degrader-3
  • HY-150400
    XF056-132 free base 2407450-73-9
    XF056-132 free base is a potent WDR5 (WD40 repeat domain protein 5) PROTAC degrader.
    XF056-132 free base
  • HY-173467
    PROTAC MTP3 degrader-1
    PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader (Red: MYC inhibitor (HY-173469), black: linker (HY-W008296), Blue: E3 ligase ligand (HY-14658)).
    PROTAC MTP3 degrader-1
  • HY-178215
    PROTAC SMARCA2/4 degrader-40 3099581-65-1
    BRM/BRG1 ligand 4 (Compound 6) is a SMARCA2/4 PROTAC degrader. BRM/BRG1 ligand 4 exhibits potent degradation activity against both SMARCA2 and SMARCA4 in HeLa cells, with DC50 less than 0.1 nM. BRM/BRG1 ligand 4 can be used for the study of cancers associated with SMARCA2/SMARCA4 abnormalities or SWI/SNF mutations.
    PROTAC SMARCA2/4 degrader-40
  • HY-170855A
    YW-N-7 TFA
    YW-N-7 (TFA) is a PROTAC that targets both the inhibition and degradation of RET kinase, with a DC50 of 88 nM. YW-N-7 (TFA) exhibits antitumor activity in a KIF5B-RET-driven xenograft mouse tumor model and can be used in the area of cancer (Structure: red part represents the target protein ligand: HY-170856; blue part represents the E3 ligase ligand: HY-1708557; black part represents the linker; E3 ligase ligand + linker: HY-170858).
    YW-N-7 TFA
  • HY-178797
    PROTAC LRRK2 Degrader-3 3080678-98-1
    PROTAC LRRK2 Degrader-3 (compound 6) is a PROTAC LRRK2 degrader with a DC50 of 0.17 nM. PROTAC LRRK2 Degrader-3 can be used for research in Parkinson’s disease and inflammation.
    PROTAC LRRK2 Degrader-3
  • HY-139315
    PROTAC IRAK4 degrader-4 2360528-45-4
    PROTAC IRAK4 degrader-4 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127.
    PROTAC IRAK4 degrader-4
  • HY-181660
    PROTAC IKKβ degrader-1
    PROTAC IKKβ degrader-1 is a IKKβ PROTAC degrader (DC50 = 7.15 μM). PROTAC IKKβ degrader-1 induces apoptosis (Apoptosis) in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 induces G1 phase cell cycle arrest in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 exhibits antiproliferative activity against a variety of cells. PROTAC IKKβ degrader-1 is applicable for research related to cancers such as triple-negative breast cancer, colon cancer, liver cancer, pancreatic cancer.
    PROTAC IKKβ degrader-1
  • HY-177758
    PROTAC HDAC6 degrader 8
    HDAC6 degrader-6 (Compound 11b) is a potent and selective HDAC6 PROTAC degrader with a DC50 of 1.9 nM. HDAC6 degrader-6 has no effect on the protein levels of other HDAC family members and does not degrade IKZF1, IKZF3, and GSPT1. HDAC6 degrader-6 can be used to study multiple myeloma (Pink: HDAC6 ligand (HY-177776); Blue: CRBN ligand (HY-W998281); Black: Linker).
    PROTAC HDAC6 degrader 8
  • HY-175867
    PROTAC SMARCA2 degrader-34
    PROTAC SMARCA2 degrader-34 (compound 52) is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: < 0.1 μM for SMARCA2, > 1 μM for SMARCA4). PROTAC SMARCA2 degrader-34 can be used for study of cancer. (Pink: SMARCA2 ligand (HY-178414) ; Blue: E3 ligand (HY-168055) ; Black: linker).
    PROTAC SMARCA2 degrader-34
  • HY-180793
    PROTAC USP7 Degrader-2 3056612-67-7
    PROTAC USP7 Degrader-2 (Compound D16) is an efficient and selective USP7 PROTAC degrader with a DC50 of 1.91 μM (in TE-12 cells). PROTAC USP7 Degrader-2 inhibits the migration of upper gastrointestinal tract (UGI) cancer cells and shows relatively weak anti-proliferative activity. PROTAC USP7 Degrader-2 can be used in the research of metastatic upper gastrointestinal cancer.
    PROTAC USP7 Degrader-2
  • HY-180909
    TMU454
    TMU454 is a prototype GalNAc-PROTAC conjugate. TMU454 binds to ASGPR on the membrane of cells, and then is internalized via ASGPR-mediated endocytosis. TMU454 selectively degrades BRD4. TMU454 exhibits anticancer activity against hepatocellular carcinoma.
    TMU454
  • HY-160151
    TP1L
    TP1L is a potent and selective T-cell protein tyrosine phosphatase (TC-PTP) PROTAC degrader, with a DC50 value of 35.8 nM. TP1L elevates the phosphorylation level of TC-PTP substrates including pSTAT1 and pJAK1. TP1L selectively enhances IFN-γ signaling and increases MHC-I expression. TP1L activates TCR signaling through increases phosphorylation of LCK. TP1L enhances CAR-T cell mediated tumor killing efficacy through activation of the CAR-T cells. TP1L can be used for the study of cancer. (Pink: TC-PTP ligand: (HY-138964), Blue: E3 ligase CRBN Ligand (HY-A0003), Black: Linker: (HY-140002)).
    TP1L
  • HY-158062
    LC-1-40
    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).
    LC-1-40
  • HY-153674
    PROTAC SOS1 degrader-4
    PROTAC SOS1 degrader-4 (compound 10) is a potent SOS1 degrader. PROTAC SOS1 degrader-4 shows antiproliferative activity.
    PROTAC SOS1 degrader-4
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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