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-143905
    PROTAC TTK degrader-2 2953426-48-5
    PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells.
    PROTAC TTK degrader-2
  • HY-178176
    PROTAC CB1R Degrader-1
    PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)).
    PROTAC CB1R Degrader-1
  • HY-159016
    SIAIS630121-NC
    SIAIS630121-NC is a negative control for NAMPT (nicotinamide phosphoribosyltransferase) degrader SIAIS630121(Sturcture Note:(Blue: Cereblon ligand Thalidomide (HY-14658) analogue (HY-138793), Black: linker；Pink: Nampt inhibitor FK866 (HY-50876)).
    SIAIS630121-NC
  • HY-163920
    PROTAC HDAC8 Degrader-1
    Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC50 of 0.27 nM in A549 cells.
    PROTAC HDAC8 Degrader-1
  • HY-162745
    SMARCA2 degrader-20 2568273-85-6
    SMARCA2 degrader-20 is a PROTAC SMARCA2 degrader with a DC50 less than 100 nM in A549 cells.
    SMARCA2 degrader-20
  • 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-173372
    PROTAC AR Degrader-10
    PROTAC AR Degrader-10 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-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-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. (Pink: ERα Ligand (HY-12864); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W040168))
    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-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-175381
    DeFer-2 3058911-16-0
    DeFer-2 is a ferritin PROTAC degrader (Kd = 17.1 μM). DeFer-2 induces ferritin degradation, triggering caspase 3-GSDME-mediated pyroptosis in cancer cells through free iron accumulation and elevated ROS. DeFer-2 significantly inhibits tumor growth and prolongs survival in mice bearing B16F10 subcutaneous tumors. DeFer-2 can be used to study melanoma. (Pink: Oleic acid: HY-N1446, Blue: (S,R,S)-AHPC: HY-125845, Black: γ-Aminobutyric acid: HY-N0067, Blue + Black: (S,R,S)-AHPC-C3-NH2: HY-130711).
    DeFer-2
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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