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-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. (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))
    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-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 (Pink: DHFR-TS ligand (HY-15676); Blue: Idasanutlin 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-162943
    P60-L3-VHL
    P60-L3-VHL is a PROTAC-class Foxp3 degrader. P60-L3-VHL reduced cell differentiation and Foxp3 expression in activated Treg cells in vitro and had anti-tumor activity (Blue: E3 ligase ligand (HY-162945); Pink: target protein ligand (HY-162946); Black: linker (HY-162947)).
    P60-L3-VHL
  • 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-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-117690A
    dBRD9 dihydrochloride 2341840-98-8
    dBRD9 dihydrochloride is a selective BRD9 PROTAC degrader. dBRD9 dihydrochloride inhibits proliferation of AML cell lines.
    dBRD9 dihydrochloride
  • HY-155371
    BT-PROTAC 3032848-64-6
    BT-PROTAC is a bioorthogonally activatable prodrug. BT-PROTAC can accurately control the activity of PROTAC.
    BT-PROTAC
  • HY-137516A
    LC-2 epimer 2502156-12-7
    LC-2 epimer is a differential isomer of LC-2. LC-2 is a mutation-selective PROTAC depressant for KRAS and contains a ligand for the von Hippel Lindau E3 ligase linked to the KRAS inhibitor MRTX849.
    LC-2 epimer
  • HY-176239
    PROTAC PI3Kδ degrader-1
    PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model. Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
    PROTAC PI3Kδ degrader-1
  • HY-132941
    CFT-2718
    CFT-2718 is a new BRD4-targeting degrader (PROTAC) with enhanced catalytic activity and in vivo properties.
    CFT-2718
  • HY-151886
    NU223612 2759420-43-2
    NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB).
    NU223612
  • HY-150251
    SD-91 2497583-03-4
    SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a Ki of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506).
    SD-91
  • HY-169275
    PROTAC SMARCA2 degrader-24 2755761-70-5
    PROTAC SMARCA2 degrader-24 (Compound 34) is a PROTAC degrader for SMARCA2 with a DC50 < 0.1 µM in HeLa. PROTAC SMARCA2 degrader-24 degrades SMARCA4 with a DC50 > 10 μM in HeLa.
    PROTAC SMARCA2 degrader-24
  • HY-174858
    dASK1-VHL
    dASK1-VHL is an orally active PROTAC degrader targeting ASK1. dASK1-VHL can effectively bind VHL and promote the selective degradation of ASK1. dASK1-VHL effectively reduces ASK1 protein levels, inhibits the activation of p38 MAPK, and reduces liver lipid content. dASK1-VHL provides new ideas for the study of Metabolic dysfunction-associated steatohepatitis (MASH) (Pink: ASK1 ligand 1 (HY-174860); Blue: E3 ligand (S,R,S)-AHPC (HY-125845); Black: Linker, (S,R,S)-AHPC-CO-C2-PEG-NHCO-C2-COOH (HY-174861).
    dASK1-VHL
  • HY-161654
    PROTAC SOS1 degrader-10 3043923-74-3
    PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))
    PROTAC SOS1 degrader-10
  • HY-162834
    PROTAC SMARCA2/4-degrader-27 2375564-54-6
    PROTAC SMARCA2/4-degrader-27 (PROTAC 2) is a PROTAC-based degrader of SMARCA2 and SMARCA4. (Blue: CRL2VHL ligand VH032-cyclopropane-F (HY-125905); Black: linker (HY-159678);Pink: a SMARCA-BD ligand 1 for PROTAC (HY-44012)).
    PROTAC SMARCA2/4-degrader-27
  • HY-175764
    FIP22 3091132-73-6
    FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis (Pink: IRAK4 ligand (HY-175765); Blue: CRBN ligand (HY-W087383); Black: Linker (HY-46871)).
    FIP22
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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