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-168455
    RNAse L RIBOTAC
    RNAse L RIBOTAC (compound C64) is an RNA-degrading chimera which binds to a four-way RNA helix called SL5 in the 5’ UTR of the SARS-CoV-2 RNA genome and inhibits the virus replication in lung epithelial carcinoma cells. (Blue: RNA ligand (HY-168456); Black: linker (HY-130591); Pink: Rnase L ligand (HY-168457))
    RNAse L RIBOTAC
  • HY-162748
    PROTAC SMARCA2/4-degrader-30 2568276-44-6
    PROTAC SMARCA2/4-degrader-30 (Compound I-291) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-30 degrades SMARCA2 in A549 and in MV411 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: ligand for target protein (HY-163926); Black: linker (HY-159684); Blue: ligand for E3 ligase (HY-W382038)).
    PROTAC SMARCA2/4-degrader-30
  • HY-169367
    ERD-1233
    ERD-1233 is a potent and orally active estrogen receptor PROTAC degrader, with the DC50 of 0.9 nM. ERD-1233 plays an important role in ER+ breast cancer research (Pink: ligand for target protein (HY-201580); Black: linker (HY-W889109); Blue: E3 ligase ligand (HY-W1009348)).
    ERD-1233
  • HY-157805
    PROTAC SARS-CoV-2 Mpro degrader-2 3057294-32-0
    PROTAC SARS-CoV-2 Mpro degrader-2 (Compound 6) is a potent PROTAC degrader of SARS-CoV-2 Mpro. PROTAC SARS-CoV-2 Mpro degrader-2 has broad-spectrum antiviral activity against CoVs, including SARS-CoV-2 (EC50 = 10.8 μM), HCoV-OC43 (EC50 = 1.6 μM) and HCoV-229E (EC50 = 6.5 μM). PROTAC SARS-CoV-2 Mpro degrader-2 exhibits potent activity against SARS-CoV-2 in Calu-3 cells, with an EC50 of 0.89 μM.
    PROTAC SARS-CoV-2 Mpro degrader-2
  • HY-177730
    PROTAC BRD4 Degrader-40
    PROTAC BRD4 Degrader-40 is a Bromodomain protein 4 (BRD4) PROTAC degrader. PROTAC BRD4 Degrader-40 can induce BRD4 degradation in cancer cells. PROTAC BRD4 Degrader-40 can be used for the research of cancer, such as leukemia. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-163927))
    PROTAC BRD4 Degrader-40
  • HY-153938A
    PROTAC PTPN2 degrader-2 TFA 2912307-39-0
    PROTAC PTPN2 degrader-2 (example 187B) TFA is a potent PTPN2 degrader with potential for studying cancer or metabolic diseases.
    PROTAC PTPN2 degrader-2 TFA
  • HY-115718B
    PZ703b hydrochloride 99.18%
    PZ703b hydrochloride is a Bcl-xl PROTAC degrader that induces apoptosis and inhibits cancer cell proliferation. PZ703b hydrochloride can be used for the research of bladder cancer research.
    PZ703b hydrochloride
  • HY-177041
    PROTAC BRD4 Degrader-35 2503035-53-6
    PROTAC BRD4 Degrader-35 (Compound 17) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-35 can be studied in anticancer research. (Pink: BRD4 ligand (HY-78695); Black: linker; Blue: ligase).
    PROTAC BRD4 Degrader-35
  • HY-147196
    KB03-SLF 2384184-42-1
    KB03-SLF (compound 6) is an electrophilic PROTAC degrader that binds to DCAF16 to degrade the nuclear protein FKBP12. KB03-SLF can be used in cancer research. (Pink: Ligand for target protein SLF (HY-114872); Black: Linker (HY-W040168); Blue: Ligand for E3 ligase (HY-169968)).
    KB03-SLF
  • HY-172359
    PROTAC HDAC6 degrader 4
    PROTAC HDAC6 degrader 4 (Compound 17c) is the PROTAC degrader for HDAC6 with a DC50 of 14 nM. PROTAC HDAC6 degrader 4 exhibits inhibitory activit against HDAC1, HDAC2, HDAC3 and HDAC6 with IC50s of 2.2, 2.37, 0.61 and 0.295 μM, respectively. (Pink: ligand for target protein HDAC6 ligand-3 (HY-172360); Black: linker (HY-138387); Blue: ligand for cereblon E3 ligase (HY-W093272))
    PROTAC HDAC6 degrader 4
  • HY-175767
    PROTAC BRD4 Degrader-39
    PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC50 value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))
    PROTAC BRD4 Degrader-39
  • HY-174445
    C199
    C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker).
    C199
  • HY-175397
    Dth
    Dth is a RNA aptamer-based PROTAC degrader. Dth can degrade a range of endogenous proteins (such as mCherry, p50, p65 and E2F1) by simply replacing the 3′ module on the RNA scaffold with the corresponding RNA aptamer of target protein (target aptamer). Pink: Target aptamer ligand (HY-176801); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-79577).
    Dth
  • HY-175320
    PROTAC c-Met degrader-5
    PROTAC c-Met degrader-5 (Compound D19) is an orally active c-Met PROTAC degrader with DC50s of 0.42 and 0.32 nM in EBC-1 and Hs746T cells, respectively. PROTAC c-Met degrader-5 significantly induces cell apoptosis, G1 cell cycle arrest, and inhibits cell migration and invasion. PROTAC c-Met degrader-5 has potent antiproliferative and degradation efficacy against c-Met-addicted cancer cells and Tepotinib (HY-14721)-resistant cancer cells. Pink: c-Met ligand (HY-W425461); Blue: CRBN ligase ligand (HY-14658); Black: linker
    PROTAC c-Met degrader-5
  • HY-159450
    PROTAC SMARCA2 degrader-6 2568523-72-6
    PROTAC SMARCA2 degrader-6 (compound I-427) 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-6
  • HY-169135
    PROTAC 20S proteasome subunit β5 degrader 2
    PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader for 20S proteasome subunit β5, with a DC50 of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 inhibits the proliferation of cancer cell FaDu with IC50 of 0.23 μM. PROTAC 20S proteasome subunit β5 degrader 2 exhibits antitumor efficacy in mice models. (Pink: Ligand for target protein (HY-10227); Blue: Ligand for E3 ligase (HY-103596); Black: Linker (HY-Y1760))
    PROTAC 20S proteasome subunit β5 degrader 2
  • HY-162538
    LC-MI-3
    LC-MI-3 is an orally active and potent interleukin-1 receptor-associated kinase 4 (IRAK4) PROTAC degrader, with a DC50 of 47.3 nM. LC-MI-3 effectively inhibits the activation of downstream NF-κB signaling. LC-MI-3 can be used for the research of acute and chronic inflammatory skin. (Blue: VHL ligand, Black: linker, Pink: CRBN ligand (HY-14658)).
    LC-MI-3
  • HY-147235
    RIPK2-IN-2 2143956-20-9
    RIPK2-IN-2 (example 25) is a RIP2 kinase PROTAC inhibitor. RIPK2-IN-2 can block RIP2-dependent proinflammatory signaling, regulated RIP2 kinase activity in auto inflammatory diseases.
    RIPK2-IN-2
  • HY-175448
    GNE-1567
    GNE-1567 is a potent ERα PROTAC degrader and a selective XIAP antagonist with a Kd value of 0.03 μM. GNE-1567 is indicated for breast cancer research. (Pink: ligand for target protein (HY-18719); Black: linker; Blue: ligand for E3 ligase (HY-175449)).
    GNE-1567
  • HY-155397
    PRO-HD2
    PRO-HD2 is a cell-specific, PROTAC-based HDAC6 degrader.
    PRO-HD2
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