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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
Art. -Nr. Produktname CAS. Nr. Reinheit Chemische Struktur
  • HY-138642A
    (Rac)-Vepdegestrant 2229711-08-2
    (Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
    (Rac)-Vepdegestrant
  • HY-180889
    PROTAC BRD3 degrader-1 2257497-15-5
    PROTAC BRD3 degrader-1 (compound D072) is a potent and selective PROTAC BRD3 degrader. PROTAC BRD3 degrader-1 selectively degrades BRD3 in mice, leading to the downregulation of H3K18ac without affecting BRD2 or BRD4. PROTAC BRD3 degrader-1 reduces intraocular inflammation in the experimental autoimmune uveitis (EAU) mouse mode and inhibits proinflammatory microglia in both uveitis retina and LPS (HY-D1056) treated mouse microglia cell line BV2. PROTAC BRD3 degrader-1 can be used for uveitis research.
    PROTAC BRD3 degrader-1
  • HY-173372
    PROTAC AR Degrader-10
    PROTAC AR Degrader-10 (GT19) is a protein degrader targeting the androgen receptor (AR) with a DC50 value ≤100 nM. PROTAC AR Degrader-10 can be used for prostate cancer study. (Structure Note: Pink: target protein ligand (HY-173373); Blue: E3 ligase ligand (HY-138793); Black: linker) .
    PROTAC AR Degrader-10
  • HY-182083
    PROTAC PI3Kα/δ degrader-1
    PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer.
    PROTAC PI3Kα/δ degrader-1
  • HY-161930
    PROTAC GPX4 degrader-3
    PROTAC GPX4 degrader-3 is a potent PROTAC GPX4 degrader with a DC50 (24h) of 0.019 μM and an IC50 of 0.024 μM in HT1080 cell.
    PROTAC GPX4 degrader-3
  • HY-182370
    TKP-5 3076612-97-7
    TKP-5 is a PROTAC protein degrader targeting BRD4. TKP-5 can binds to BRD2, BRD3, BRD4 and BRDT, with Kd values of 150 nM, 100 nM and 150 nM for the first three proteins respectively. TKP-5 inhibits the production of thymic stromal lymphopoietin and suppresses the expression of IL-33 mRNA. TKP-5 is applicable to studies related to tape-stripping induced skin injury.
    TKP-5
  • HY-180925
    Leu-PEG1-Dasa 3037776-72-7
    Leu-PEG1-Dasa is a potent BCR-ABL PROTAC degrader with a DC50 of 0.48 nM. Leu-PEG1-Dasa uses a single amino acid as the E3 ligand and belongs to a mini-PROTAC, functioning through the N-terminal canonical pathway. Leu-PEG1-Dasa exhibits potent anti-proliferative activity against K562 cells. Leu-PEG1-Dasa can be used for the study of chronic myeloid leukemia (CML).
    Leu-PEG1-Dasa
  • HY-173125
    FDU73
    FDU73 is a highly effective and selective BTK PROTAC degrader with a DC50 of 2.9 nM (in JeKo-1 cells). FDU73 can inhibit the proliferation of tumor cells and exhibits anti-tumor activity. (Pink: BTK ligand-14 (HY-173126); Black: Linker (HY-168297); Blue: E3 ligase ligand 59 (HY-173378); E3 ligase ligand+Linker (HY-173127))
    FDU73
  • HY-145395
    PROTAC BRD9 Degrader-2 2633631-78-2
    PROTAC BRD9 Degrader-2 is a BRD9 bifunctional degrader for researching cancer.
    PROTAC BRD9 Degrader-2
  • HY-178961
    PROTAC ERα Degrader-13
    PROTAC ERα Degrader-13 is an orally active PROTAC molecule that efficiently and selectively degrades ERα (DC50 = 3.78 nM). PROTAC ERα Degrader-13 has the characteristics of strong anti proliferation (IC50 = 0.6 nM), induction of apoptosis, and overcoming drug resistance in MCF-7 cells. PROTAC ERα Degrader-13 has good safety and no significant organ toxicity. PROTAC ERα Degrader-13 can be used for cancer research.
    PROTAC ERα Degrader-13
  • HY-139316
    PROTAC IRAK4 degrader-5 2360530-61-4
    PROTAC IRAK4 degrader-5 is a Cereblon-based IRAK4 degrader extracted from patent US20190192668A1, compound I-171.
    PROTAC IRAK4 degrader-5
  • HY-143286
    PF15 2892631-70-6
    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.
    PF15
  • HY-158313
    PROTAC EGFR degrader 13 2861227-35-0
    PROTAC EGFR degrader 13 (compound 106) is an EGFR PROTAC degrader with a DC50 of <0.1 μM. PROTAC EGFR degrader 13 has proliferation inhibitory activity on cell Ba/F3-TEL-EGFR-T790M-L858R-C797S with an IC50 of 15.6 nM. PROTAC EGFR degrader 13 can be used for the study of EGFR-related diseases such as cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-14658); Black: linker (HY-W262798); E3 ligand + linker: HY-W998306).
    PROTAC EGFR degrader 13
  • HY-174415
    ZSH-2117
    ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFRL858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFRL858R/T790M/C797S xenograft mice model. Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker
    ZSH-2117
  • HY-169272
    PROTAC SMARCA2 degrader-21 2891464-61-0
    PROTAC SMARCA2 degrader-21 (Compound I-5) is a PROTAC degrader for SMARCA, that degrades SMARCA2 with a DC50 of 10-50 nM in A549 cell, and degrades SMARCA2 and SMARCA4 in MV411 with DC50 of <1 nM and >100 nM, respectively.
    PROTAC SMARCA2 degrader-21
  • HY-179112
    PROTAC IKKβ/NR4A1 degrader-1 2826215-20-5
    PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577).
    PROTAC IKKβ/NR4A1 degrader-1
  • HY-162747
    PROTAC SMARCA2 degrader-17 2568276-43-5
    PROTAC SMARCA2 degrader-17 (compound I-290) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment.
    PROTAC SMARCA2 degrader-17
  • HY-181147
    PROTAC HSP70 Degrader-1
    PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 PROTAC degrader that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia.
    PROTAC HSP70 Degrader-1
  • HY-173257
    Cath-L-dBET1
    Cath-L-dBET1 is a PROTAC degrader targeting BRD4. Cath-L-dBET1 has an IC50 value of 2.8 μM in MDA-MB-231 cells. Cath-L-dBET1 can be activated by cathepsin L (Cath-L) and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.
    Cath-L-dBET1
  • HY-173327
    BRD4 degrader-6 3055207-38-7
    BRD4 degrader-6 is a dimeric BDR4 PROTAC degrader (DC50: < 0.1 μM). BRD4 degrader-6 promotes the ubiquitination and degradation of BDR4 and has anticancer activity.
    BRD4 degrader-6
Art. -Nr. Produktname / Synonyms Application Reactivity
PROTACs Isoform Comparison

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