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-182343
    PROTAC MLKL Degrader-3
    PROTAC MLKL Degrader-3 is a MLKL PROTAC degrader with DC50 values of 248.9 nM (Hepa1-6) and 271.3 nM (HepG2), respectively. PROTAC MLKL Degrader-3 induces proteasome- and cereblon-dependent MLKL degradation via ubiquitination. PROTAC MLKL Degrader-3 reduces intratumoral MLKL levels and inhibits tumor growth in mice. PROTAC MLKL Degrader-3 can be used in the research of hepatocellular carcinoma.
    PROTAC MLKL Degrader-3
  • HY-163152
    PROTAC BRM degrader-1 2378051-80-8
    PROTAC BRM degrader-1 (compound 17) is a PROTAC-based BRM and BRG1 degrader, with DC50 values of 93 pM and 4.9 nM, respectively.
    PROTAC BRM degrader-1
  • HY-163845
    YX862 3092219-09-2
    YX862 is a selective HDAC8 PROTAC degrader and induces the degradation of HDAC8 with maximum degradation ＞ 95% at 250 nM in MDA-MB-231 cells.
    YX862
  • HY-175541
    TQ-3959 2926610-43-5
    TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)).
    TQ-3959
  • HY-181360
    PROTAC EZH2 Degrader-31 3093642-33-9
    PROTAC EZH2 Degrader-31 is an EZH2 PROTAC degrader. PROTAC EZH2 Degrader-31 promotes the ubiquitination and degradation of EZH2. PROTAC EZH2 Degrader-31 can be used for lymphoma-related research.
    PROTAC EZH2 Degrader-31
  • HY-169008
    PROTAC ACC degrader-1
    PROTAC ACC degrader-1 (Compound 9b) is a Acetyl-CoA Carboxylase degrader. PROTAC ACC degrader-1 exhibits superior potency against Aphis craccivora (IC50 = 107.8 μg/mL). (Structure Note: Pink, Target protein ligand (HY-169009); Blue, E3 ligand (HY-10984); Black, linker (HY-W007559).
    PROTAC ACC degrader-1
  • HY-163864
    PROTAC SMARCA2/4-degrader-11 2568276-71-9
    SMARCA2 degrader-1 (compound I-321) is a PROTAC degrader of SMARCA with DC50 ＜ 100nM.
    PROTAC SMARCA2/4-degrader-11
  • HY-158047
    UNC8900
    UNC8900 is a VHL recruiting STING PROTAC degrader (DC50: 0.0.924 μM). UNC8900 can be used for research of viral or bacterial infection. (Blue: VHL ligand, black: linker; Pink: STING inhibitor).
    UNC8900
  • HY-170405
    YB-3–17 2940242-88-4
    YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC50=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC50=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC50 of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models.
    YB-3–17
  • HY-144605
    PROTAC EGFR degrader 3 2768472-28-0
    PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation.
    PROTAC EGFR degrader 3
  • HY-176792A
    (R)-ACBI-4 3097973-97-9
    (R)-ACBI-4 is an isomer of ACBI-4 (HY-176792). ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader. ACBI-4 has significant anti-proliferative effect and potently degrades multiple KRAS mutants in cancer cells, such as KRASG12R.
    (R)-ACBI-4
  • HY-178728
    BION106 3077918-44-3
    BION106 is a dihydrofolate reductasethymidylate synthase (DHFR-TS) PROTAC degrader. BION106 exhibits extremely strong anti-malarial activity with a Ki and toxicity of 2.68 nM and 0.2 μM against Plasmodium falciparum, and > 100 μM and 44.2 μM in mammalian cells. BION106 can be used for the study of antimalarial parasites (Blue: Idasanutlin ligand (HY-15676); Pink: DHFR-TS ligand (HY-153007); Black: Linker (HY-W021401)).
    BION106
  • HY-159455
    PROTAC SMARCA2/4-degrader-4 2568523-81-7
    PROTAC SMARCA2/4-degrader-4 (Compound I-434) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-4 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for target protein (HY-159472); Black: Linker (HY-159478); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-4
  • HY-158758
    PROTAC IRAK4 degrader-10 3033829-95-4
    PROTAC IRAK4 degrader-10 (compound 10) is an oral active PROTAC based on Cereblon ligand, and induces the degradation of IRAK4 with maximum degradation of 95.94% and the DC50 of 7.68 nM in HEK293 cells (Sturcture Note:(Blue: Cereblon ligand, Black: linker；Pink: IRAK4 ligand).
    PROTAC IRAK4 degrader-10
  • HY-181295
    PROTAC EZH2 Degrader-14 3093642-21-5
    PROTAC EZH2 Degrader-14 is an EZH2 PROTAC degrader, with an IC50 of 18.21 μM against diffuse large B-cell lymphoma cells, and exhibits no antiproliferative activity against non-target cells at concentrations up to 30.00 μM. PROTAC EZH2 Degrader-14 can be used in studies related to diffuse large B-cell lymphoma.
    PROTAC EZH2 Degrader-14
  • HY-163867
    PROTAC SMARCA2 degrader-15 2568276-78-6
    SMARCA2 degrader-4 (compound I-332) 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-15
  • HY-183937A
    PD-305
    PD-305 is a selective PTPN2 PROTAC degrader, with DC50 values of 0.25 nM and 5.11 nM against PTPN2 and PTPN1, respectively. PD-305 enhances IFN-γ-induced STAT1 phosphorylation, inhibits the proliferation of IFN-γ-stimulated colorectal cancer cells, promotes CD8+ T cell activation, enhances the tumor-killing activity of T cells, and suppresses tumor growth in mouse models. PD-305 can be used for the research of colorectal cancer.
    PD-305
  • HY-180964
    Lys-PEG3-BA 3057939-67-7
    Lys-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader with DC50 values of 1.32 and 19.66 μM for H3122 (EML4-ALK) and H1975 (EGFR-L858R/T790M) cells, respectively. Lys-PEG3-BA hinders proliferation via rewiring the ubiquitin- proteasome system in vitro. Lys-PEG3-BA can be used for non-small cell lung cancer research.
    Lys-PEG3-BA
  • HY-139317
    PROTAC IRAK4 degrader-6 2360530-72-7
    PROTAC IRAK4 degrader-6 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-172.
    PROTAC IRAK4 degrader-6
  • HY-156152
    CARM1 degrader-1 3032785-00-2
    CARM1 degrader-1 is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 can be used for the research of breast cancer.
    CARM1 degrader-1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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