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-173066
    NU227326 3048196-52-4
    NU227326 is the PROTAC degrader for Indoleamine 2,3-dioxygenase 1 (IDO1) with DC50 of 4.5 nM. NU227326 degrades IDO1 in cell U87 and GBM43 with DC50 of 7.1 nM and 11.8 nM. NU227326 exhibits good pharmacokinetic properties with a plasma half-life of 5.7 hours and a brain tissue half-life of 11.8 hours.(Pink: ligand for target protein IDO1 ligand-1 (HY-173067); Black: linker (HY-173068); Blue: ligand for E3 ligase Cereblon (HY-W087383))
    NU227326
  • HY-161368
    BRD-SF2 3050690-26-8
    BRD-SF2 is a BRD4-targeted PROTAC degrader (DC50: 17.2 μM) (Blue: VHL ligand, black: linker, pink: BRD4 ligand).
    BRD-SF2
  • HY-147373
    DA-PROTAC 2488660-12-2
    DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research.
    DA-PROTAC
  • HY-170852
    QZ2135
    QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854).
    QZ2135
  • HY-132997
    PROTAC Bcl-xL degrader-3 2471970-60-0
    PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader (WO2020163823A2, compound 44).
    PROTAC Bcl-xL degrader-3
  • HY-170347
    PROTAC SMARCA2/4 degrader-36 3033588-00-7
    PROTAC SMARCA2/4 degrader-36 (Compound 29) is an effective dual degrader of SMARCA2/4,with DC50 values of 0.22 nM and 0.85 nM for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2/4 degrader-36 has anti-cell proliferation activity (Pink: Target Protein Ligand (HY-170354); Black: Linker (HY-W895794); Blue: E3 Ligase Ligand (HY-170353); E3 Ligase Ligand-Linker Conjugate (HY-170356)).
    PROTAC SMARCA2/4 degrader-36
  • HY-169276
    PROTAC SMARCA2 degrader-25 2770571-17-8
    PROTAC SMARCA2 degrader-25 (example 86) is a potent PROTAC SMARCA2 degrader with the DC50 of ＜0.01 μM (Pink: ligand for target protein (HY-169487); Black: linker (HY-W052601); Blue: E3 ligase ligand (HY-W087383)).
    PROTAC SMARCA2 degrader-25
  • HY-168586
    PROTAC IRAK4 degrader-12 2919995-09-6
    PROTAC IRAK4 degrader-12 is a PROTAC based on Cereblon ligand, inducing a maximum degradation rate of IRAK4 of 108.46% in K562 cells with an IC50 value of 4.87 nM ( Structure Note: Pink, IRAK4 inhibitor (HY-168611); Blue, E3 (HY-W733885); Black, linker (HY-168613)).
    PROTAC IRAK4 degrader-12
  • HY-164924
    ERD-12310A
    ERD-12310A is a PROTAC targeting Estrogen Receptor α (ERα) with a ED50 value of 47 pM. ERD-12310A has oral activity. ERD-12310A is composed of PROTAC target protein ligand ER ligand-4 (HY-164925) (red part), E3 ligase ligand (S)-Deoxy-thalidomide (HY-168055) (blue part).
    ERD-12310A
  • HY-148521
    PROTAC FLT3/CDK9 degrader-1
    PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML.
    PROTAC FLT3/CDK9 degrader-1
  • HY-170824
    SMD-3236 3033586-31-8
    SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827).
    SMD-3236
  • HY-153880
    KRAS degrader-1 2795275-59-9
    KRAS degrader-1 (compound 1) is a potent KRAS degrader. KRAS degrader-1 target specific proteins for degradation through the autophagy-lysosomal degradation pathway.
    KRAS degrader-1
  • HY-168910
    PROTAC c-Met degrader-3
    PROTAC c-Met degrader-3 (Compound 22b) is a c-Met PROTAC degrader. PROTAC c-Met degrader-3 promotes ubiquitination and degradation of c-Met (DC50 of 0.59 nM in EBC-1 cells). PROTAC c-Met degrader-3 can be used for the research of lung cancer (Pink: c-Met ligand (HY-14721); Blue: E3 ligase CRBN ligand (HY-W249500); linker + E3 ligase ligand (HY-168911)).
    PROTAC c-Met degrader-3
  • HY-163851
    PROTAC Vif degrader-1
    PROTAC Vif degrader-1 (Compound L15) is a Vif PROTAC degrader. PROTAC Vif degrader-1 has antiviral activity against HIV-1 (EC50: 33.35 μM against HIV-1IIIB). Blue: CRBN ligand (HY-10984); Black: linker; Pink: HIV-1 inhibitor(HY-163852).
    PROTAC Vif degrader-1
  • HY-163870
    PROTAC SMARCA2/4-degrader-17 2568276-88-8
    PROTAC SMARCA2/4-degrader-17 (Compound I-345) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-17 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-W053507); Blue: Ligand for E3 Ligase (HY-125845))
    PROTAC SMARCA2/4-degrader-17
  • HY-162813
    PROTAC SMARCA2/4-degrader-25
    PROTAC SMARCA2/4-degrader-25 (compound 7d) is a PROTAC targeting SMARCA2/4. PROTAC SMARCA2/4-degrader-25 is composed of E3 ligase (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (HY-W998248) (blue part), PROTAC Linker (S)-2-Amino-3,3-dimethylbutanoic acid (HY-59140) (black part), and target protein ligand SMARCA2/4-ligand-3 (HY-162814) (red part). The conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC (HY-125845)[1].
    PROTAC SMARCA2/4-degrader-25
  • HY-178225
    PROTAC SMARCA2/4 degrader-39 3099581-74-2
    PROTAC SMARCA2/4 degrader-39 (Compound 7) is a selective degrader of SMARCA2 (BRM) and SMARCA4 (BRG1) PROTAC. PROTAC SMARCA2/4 degrader-39 is promising for research of oncology, such as non-small cell lung cancer and colorectal cancer. (Pink: BRM/BRG1 ligand 5 (HY-178886); Black: Linker Piperazine (HY-B0912); Blue: (S)-Deoxy-thalidomide (HY-168055))
    PROTAC SMARCA2/4 degrader-39
  • HY-168634
    SJ46421
    SJ46421 is a (+)-JQ-1 (HY-13030) based KLHDC2-BRD3 PROTAC protein degrader. SJ46421 induces cooperative ternary complexes with KLHDC2 and BRD3BD2, with an IC50 of 7.8 nM. SJ46421 selectively inhibits KLHDC2 substrate ubiquitylation. SJ46421 promotes polyubiquitylation of the BD2 domain from BRD2, BRD3, or BRD4. SJ46421 possesses poor cell permeability. (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-168536)).
    SJ46421
  • HY-170598
    HP211206
    HP211206 is a SARS-CoV-2 main protease (Mpro) PROTAC degrader. HP211206 effectively degrades SARS-CoV-2 Mpro and its drug-resistant mutants. HP211206 has an IC50 of 181.9 nM and a DC50 of 621 nM for Mpro. HP211206 has antiviral activity. (Pink: H117 (HY-170599); Black: linker (HY-B0236); Blue: E3 ligase ligand (HY-41547)).
    HP211206
  • HY-137344
    dAURK-4 2705844-81-9
    dAURK-4, an Alisertib (HY-10971) derivative, is a potent and selective AURKA (Aurora A) degrader. dAURK-4 has anticancer effects.
    dAURK-4
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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