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  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. Nom du produit CAS No. Pureté Chemical Structure
  • HY-123844
    dBET57 1883863-52-2 99.94%
    dBET57 is an effective and selective BRD4BD1 degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4Cereblon, showing a DC50/5h value of 500 nM for BRD4BD1.
    dBET57
  • HY-111866
    PROTAC RIPK degrader-2 1801547-16-9 99.89%
    PROTAC RIPK degraders -2 is a non-peptide PROTAC based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes.
    PROTAC RIPK degrader-2
  • HY-168016
    PROTAC YAP degrader-1 3058483-58-9 99.77%
    PROTAC YAP degrader-1 is a VHL-recruiting PROTAC degrader (DC50=8.2 μM) and antiproliferative agent that targets YAP. PROTAC YAP degrader-1 recruits the E3 ligase VHL and binds to VHL to form a ternary complex containing YAP. PROTAC YAP degrader-1 inhibits the nuclear localization of YAP in cancer cells, reduces YAP/TEAD-mediated transcription, and induces TAZ protein degradation. PROTAC YAP degrader-1 reduces the oncogenic activity of YAP and exerts antiproliferative effects in the Huh7 xenograft mouse model. PROTAC YAP degrader-1 can be used for the research of hepatocellular carcinoma and mesothelioma.
    PROTAC YAP degrader-1
  • HY-136262
    CRBN-6-5-5-VHL 2362575-45-7 99.45%
    CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3.
    CRBN-6-5-5-VHL
  • HY-169093
    MS41 2768610-97-3 98.97%
    MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078).
    MS41
  • HY-156568
    SMD-3040 3033109-92-8 99.91%
    SMD-3040 is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 can be used in the study of tumors such as melanoma.
    SMD-3040
  • HY-125877
    PROTAC Mcl1 degrader-1 2163793-38-0 98.13%
    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM.
    PROTAC Mcl1 degrader-1
  • HY-130835
    FKBP12 PROTAC RC32 2375555-66-9
    FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an Cereblon E3 ubiquitin ligase (Pomalidomide; HY-10984).
    FKBP12 PROTAC RC32
  • HY-129523
    PROTAC K-Ras Degrader-1 2378258-52-5 99.90%
    PROTAC K-Ras Degrader-1 (Compound 518) is a PROTAC. PROTAC K-Ras Degrader-1 can effectively degrades K-Ras based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells.
    PROTAC K-Ras Degrader-1
  • HY-137487
    PROTAC BRAF-V600E degrader-1 2417296-84-3 98.04%
    PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS) and inhibits the growth of melanoma cells.
    PROTAC BRAF-V600E degrader-1
  • HY-154984
    JET-209 3033714-58-5
    JET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia.
    JET-209
  • HY-159779
    NR-V04 2766608-52-8 99.90%
    NR-V04 is a selective NR4A1 PROTAC degrader. NR-V04 forms a ternary complex with NR4A1 and the VHL E3 ligase, mediates proteasome-dependent degradation of NR4A1. NR-V04 induces tumor-infiltrating B cells and effector memory CD8+ T cells and reduces monocytic myeloid-derived suppressor cells in tumor microenvironments. NR-V04 can be used for the research of melanoma and colon cancer.
    NR-V04
  • HY-173523
    KI-CDK9d-32 3054009-82-1 99.03%
    KI-CDK9d-32 is a highly selective and potent CDK9 PROTAC degrader (DC50: 0.89 nM). KI-CDK9d-32 promotes the ubiquitination and degradation of CDK9. KI-CDK9d-32 inhibits the MYC pathway and disrupts nucleolar homeostasis. KI-CDK9d-32 exhibits anticancer activity against acute lymphoblastic leukemia and pancreatic cancer. (Pink: CDK9 ligand (HY-153718); Blue: E3 ligase CRBN ligand (HY-163233); Black: Linker (HY-W011657); E3 ligase CRBN ligand-linker conjugate (HY-173525)).
    KI-CDK9d-32
  • HY-131864
    SJF-1528 2230821-38-0 98.90%
    SJF-1528 (PROTAC 1) 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 also degrades HER2. SJF-1528 promotes ubiquitination and degradation of EGFR and can be used in breast cancer research.
    SJF-1528
  • HY-176786
    MCB-36 3104382-00-2 98.43%
    MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)).
    MCB-36
  • HY-130644
    iRucaparib-AP6 2410557-00-3 99.03%
    iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1.
    iRucaparib-AP6
  • HY-141640
    MS154 2550393-21-8 99.71%
    MS154 is a first-in-class E3 ligase cereblon-recruited EGFR degrader with Kd values of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand (HY-103596); black: linker (HY-W096167); pink: EGFR ligand (HY-168305)).
    MS154
  • HY-141438
    SIM1 2719051-84-8 99.47%
    SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity.
    SIM1
  • HY-152036A
    SIAIS100 TFA 99.75%
    SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 TFA can be used to research chronic myeloid leukemia (CML).
    SIAIS100 TFA
  • HY-168664
    CPD-39 3055472-38-0 98.06%
    CPD-39 is a potent and orally active CCND1 and CDK4 heterobifunctional PROTAC degrader. CPD-39 shows anti-proliferation. (Pink: ligand for target protein (HY-50767); black: linker (HY-20240); Blue: E3 ligase ligand (HY-168667)).
    CPD-39
Cat. No. Nom du produit / Synonyms Application Reactivity
PROTACs Isoform Comparison

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