1. Signaling Pathways
  2. PROTAC
  3. PROTACs

PROTACs

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.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-153821
    PROTAC KRAS G12C degrader-2 2378257-72-6 98.45%
    PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS.
    PROTAC KRAS G12C degrader-2
  • HY-156084
    LL-K9-3 2809353-52-2 99.2%
    LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs.
    LL-K9-3
  • HY-131864A
    SJF-1528 hemihydrate 98.90%
    SJF-1528 (PROTAC 1) hemihydrate is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutant EGFR in HeLa cells. SJF-1528 hemihydrate also degrades HER2. SJF-1528 hemihydrate promotes ubiquitination and degradation of EGFR and can be used in breast cancer research (Pink: ligand for target protein (HY-159047); Black: linker Tos-PEG2-CH2-Boc (HY-130532); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845)).
    SJF-1528 hemihydrate
  • 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-146231A
    SS47 TFA 99.88%
    SS47 TFA, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies. SS47 (TFA) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SS47 TFA
  • HY-149964
    PROTAC CDK9 degrader-7 2935587-90-7 99.62%
    PROTAC CDK9 degrader-7 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-7 mediates CDK9 degradation via the proteasome.
    PROTAC CDK9 degrader-7
  • HY-137343
    DB-0646 2769753-59-3 98.0%
    DB-0646, a PROTAC, is a multi-kinase degrader.
    DB-0646
  • HY-155102
    PROTAC TG2 degrader-2 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-157765
    PROTAC ERα Degrader-6
    PROTAC ERα Degrader-6 (compound A2) is a potent PROTAC degrader of ERα, with IC50 of 0.11 μM in MCE-7 cells. PROTAC ERα Degrader-6 has anti-tumor effect. PROTAC ERα Degrader-6 is a fluorescent probes with Em of 582 nm that enable real-time visualization of ERα protein degradation.
    PROTAC ERα Degrader-6
  • HY-157764
    PROTAC ATR degrader-1 2925916-30-7 98.02%
    PROTAC ATR degrader-1 (compound ZS-7) is a potent PROTAC degrader of ataxia telangiectasia and Rad3-related (ATR), with DC50 of 0.53 μM. PROTAC ATR degrader-1 plays an importnt role in cancer research.
    PROTAC ATR degrader-1
  • HY-164807
    SARD279 1489236-55-6
    SARD279 is a potent and selective Androgen Receptor degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research.(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))
    SARD279
  • HY-162749A
    G9D-4 TFA
    G9D-4 (TFA) is a potent PROTAC degrader of G9a, with the DC50 value of 0.1 μM in PANC-1 cells and do not directly perturb GLP protein, with the DC50 of >10 μM. G9D-4 (TFA) plays an important role in pancreatic cancer research (Pink: Ligand for target protein G9a/GLP Inhibitor (HY-15273); Black: Linker; Blue: Ligand for E3 ligase (HY-10984)).
    G9D-4 TFA
  • HY-168215
    YDR1 2951015-31-7 98.03%
    YDR1 is a potent PROTAC SMARCA2 degrader, with the DC50 of 7.7 nM. YDR1 plays an important role in SMARCA4 mutant cancers(Sturcture Note:(Blue: Cereblon ligand (HY-W087383), Black: linker;Pink: SMARCA2 ligand (HY-44012B)).
    YDR1
  • HY-171658
    R1-ICR-5 3070346-91-4 98.73%
    R1-ICR-5 is a selective PROTAC degrader that targets serine/threonine-protein kinase 1 (RIPK1). R1-ICR-5 mediates the degradation of RIPK1 through VHL, thereby deregulating the TNFR1 and TLR3/4 signaling hubs, enhancing the output of NF-κB, MAPK, and IFN signaling, and simultaneously promoting the activation of RIPK3 and the induction of necroptosis. R1-ICR-5 is promising for research of cancers and inflammatory diseases. (Pink: PK68 (HY-128348); Black: linker (HY-W012241); Blue: (S,R,S)-AHPC (HY-125845).
    R1-ICR-5
  • HY-147174
    PROTAC_ERRα 1801547-15-8 99.71%
    PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker.
    PROTAC_ERRα
  • HY-151966
    TD1092 3037417-26-5 99.49%
    TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research.
    TD1092
  • HY-161633
    PROTAC EGFR degrader 11 3034244-71-5 99.20%
    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.
    PROTAC EGFR degrader 11
  • HY-161101
    MG degrader 1 99.83%
    MG degrader 1 (Compd E14) is a PROTAC degrader of IKZF3, GSPT1, and GSPT2 with an EC50 value of 1.385 nM in MM.1S cells.
    MG degrader 1
  • HY-162014
    WDR5 degrader-1 3032434-45-7 98.00%
    WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1.
    WDR5 degrader-1
  • HY-160502
    CST967 99.33%
    CST967 (Compound 17) is a USP7 PROTAC degrader, and increasing the PROTAC concentration can enhance the degradation rate of USP7. CST967 can be used in cancer research.
    CST967
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