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-163502
    PROTAC STAT3 degrader-3 3033746-17-4 99.75%
    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.
    PROTAC STAT3 degrader-3
  • HY-W998345
    SMART1 99.87%
    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)) .
    SMART1
  • HY-168546
    CFT-1297 2154353-03-2 98.82%
    CFT-1297 is a BET PROTAC degrader that can degrade BRD4.
    CFT-1297
  • HY-178472
    AurAP14 3106831-75-5 99.42%
    AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker).
    AurAP14
  • HY-158381
    PROTAC PTP1B degrader 1 2924835-22-1 99.37%
    PROTAC PTP1B degrader 1 is a CRBN-based PTP1B PROTAC degrader, with DC50 values of 0.2 μM (48 h) and 0.05 μM (72 h).
    PROTAC PTP1B degrader 1
  • HY-178825A
    LD-110 triTFA 99.56%
    LD-110 triTFA is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 triTFA promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 triTFA inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 triTFA can be used for the study of esophagus squamous cancer.
    LD-110 triTFA
  • HY-176184
    PROTAC DDR1 degrader-1 3081612-73-6 98.69%
    PROTAC DDR1 degrader-1 is a potent and selective DDR1-targeting PROTAC degrader. PROTAC DDR1 degrader-1 selectively induces full-length DDR1 degradation via the ubiquitin proteasome system, blocking downstream signaling pathways. PROTAC DDR1 degrader-1 inhibits tumor cell migration and invasion. PROTAC DDR1 degrader-1 exhibits anti-tumor activity in mice. PROTAC DDR1 degrader-1 can be used for the research of DDR1-driven cancers.
    PROTAC DDR1 degrader-1
  • HY-176166
    PD-M6 3058330-82-5 98.17%
    PD-M6 is a mTOR PROTAC degrader (DC50: 4.8 μM). PD-M6 promotes ubiquitination and degradation of mTOR. PD-M6 downregulates MAPKAP1 and CASTOR1, and induces Autophagy. PD-M6 inhibits the proliferation of cervical cancer, breast cancer and liver cancer cell lines. PD-M6 can be used for the research of cervical cancer, breast cancer and liver cancer.
    PD-M6
  • HY-153932
    NR-7h 2550399-06-7
    NR-7h is a potent and selective p38α and p38β degrader with DC50 values of 24 nM and 27.2 nM for p38α in T47D, MB-MDA-231 cells, respectively.
    NR-7h
  • HY-157767
    Abd110 3021581-79-0 98.67%
    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.
    Abd110
  • HY-161346A
    (Rac)-EBET-1055 3031540-65-2
    (Rac)-EBET-1055 is the racemate of EBET-1055 (HY-161346). EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures.
    (Rac)-EBET-1055
  • HY-168574
    SZU-B6 3059333-98-8 98.78%
    SZU-B6 is a PROTAC degrader for SIRT6 with DC50 of 45 nM and 154 nM in cell SK-HEP-1 and Huh-7. SZU-B6 inhibits the proliferation of cell SK-HEP-1 with an IC50 of 1.51 μM, inhibits the colony formation of SK-HEP-1 and Huh-7, induces apoptosis and arrests the cell cycle at G2/M phase in SK-HEP-1. SZU-B6 exhibits antitumor efficacy in mouse model. (Pink: ligand for target protein (HY-16605); Black: linker (HY-W012935); BLue: ligand for E3 ligase (HY-W453548)
    SZU-B6
  • HY-179055
    PROTAC DAPK1 Degrader-1 3063030-38-3
    PROTAC DAPK1 Degrader-1 (Compound CP1) is a DAPK1 PROTAC degrader with a DC50 of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increased the MDM2 protein level. PROTAC DAPK1 Degrader-1 significantly reduced the levels of cleaved caspase-3 and cleaved PARP in a cell apoptosis model induced by the neurotoxin ceramide, indicating that it effectively inhibits neuronal apoptosis by degrading DAPK1. PROTAC DAPK1 Degrader-1 can be used to study neurological diseases such as cerebral ischemia and traumatic brain injury (pink: DAPK1 ligand (HY-179071); blue: CRBN ligand (HY-10984); black: linker (HY-40171)).
    PROTAC DAPK1 Degrader-1
  • HY-168936
    DP-15 3033837-71-4 99.06%
    DP-15 is the degrader for GSPT1 and BRD4 with DC50s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC50 of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models. (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))
    DP-15
  • HY-176528
    PROTAC ERK5 degrader-1 2919963-24-7 99.58%
    PROTAC ERK5 degrader-1 (compound 2) is a bifunctional ERK5 PROTAC degrader. PROTAC ERK5 degrader-1 induces ERK5 degradation via VHL-mediated proteasome pathway in MOLT-4 cells. PROTAC ERK5 degrader-1 can be used for the study of a disease or disorder characterized by aberrant ERK5 activity, such as acute lymphoblastic leukemia.
    PROTAC ERK5 degrader-1
  • HY-155102
    PROTAC TG2 degrader-2 3033465-51-6 99.15%
    PROTAC TG2 degrader-2 (compound 7) is a selective, competitive degrader targeting Transglutaminase 2 (TG2), with Kd > 100 μM. PROTAC TG2 degrader-2 inhibits the cell migration and decreases the level of TG2 in ovarian cancer cells. PROTAC TG2 degrader-2 can be used for ovarian cancer study.
    PROTAC TG2 degrader-2
  • HY-143904
    PROTAC TTK degrader-1 2953426-43-0 98.01%
    PROTAC TTK degrader-1 is a potent Mps1/TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells.
    PROTAC TTK degrader-1
  • HY-149760
    PVD-06 3032975-48-4 98.30%
    PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM (selectivity index >60-fold over PTP1B). PVD-06 induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity. PVD-06 can be used to further investigate PTPN2 in diseases such as leukemia and melanoma.
    PVD-06
  • HY-168135
    PROTAC c-Met degrader-1 3056647-52-7 98.48%
    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.
    PROTAC c-Met degrader-1
  • HY-176180
    PROTAC STING degrader-4 98.25%
    PROTAC STING degrader-4 is a nitro-free covalent STING PROTAC degrader with a DC50 of 3.23 μM. PROTAC STING degrader-4 effectively inhibits STING as well as its downstream signaling, such as p-TBK1 and p-NF-κB (p-P65), and immune-inflammatory cytokines. PROTAC STING degrader-4 mitigates kidney and blood inflammation in Cisplatin (HY-17394)-induced acute kidney injury (AKI) mice model. Pink: STING ligand (HY-176183); Blue: CRBN ligase ligand (HY-103596); Black: linker (HY-176182); CRBN ligase ligand + linker: HY-176181
    PROTAC STING degrader-4
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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