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-130122
    MG-277 2411085-89-5 98.66%
    MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity.
    MG-277
  • HY-161574
    LLC0424 98.42%
    LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)).
    LLC0424
  • HY-134823
    MD-222 2136246-72-3 99.81%
    MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.
    MD-222
  • HY-157844
    NUCC-0226272 3004503-12-9 99.68%
    NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research.
    NUCC-0226272
  • HY-153361
    YD23 2951015-29-3 98.92%
    YD23 is a SMARCA2 PROTAC. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. Moreover, YD23 decreases chromatin accessibility at enhancers of a number of genes including cell cycle and cell growth regulatory genes. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells mechanistically.
    YD23
  • HY-112609
    QCA570 2207569-08-0 99.95%
    QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC50 of 10 nM for BRD4 BD1 Protein.
    QCA570
  • HY-111594
    Homo-PROTAC cereblon degrader 1 2244520-98-5 99.43%
    Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.
    Homo-PROTAC cereblon degrader 1
  • HY-133557
    XZ739 2365172-19-4 99.06%
    XZ739, a Cereblon-dependent PROTAC BCL-XL (Bcl-2 family member) degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis.
    XZ739
  • HY-129610
    KB02-SLF 2384184-40-9 99.25%
    KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.
    KB02-SLF
  • HY-128842
    PROTAC MDM2 Degrader-3 2249750-23-8
    PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
    PROTAC MDM2 Degrader-3
  • HY-128756
    SIAIS178 2376047-73-1 99.36%
    SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
    SIAIS178
  • HY-133737
    PROTAC BRD4 Degrader-5 2409538-70-9 99.93%
    PROTAC BRD4 Degrader-5 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines.
    PROTAC BRD4 Degrader-5
  • HY-131183
    PROTAC PD-1/PD-L1 degrader-1 2447066-37-5 99.52%
    PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
    PROTAC PD-1/PD-L1 degrader-1
  • HY-158113
    CBPD-409
    CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker).
    CBPD-409
  • HY-P5819
    xStAx-VHLL 99.37%
    xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity.
    xStAx-VHLL
  • HY-147025
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine 2347517-69-3 99.06%
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia.
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
  • HY-163144
    DAS-5-oCRBN 98.75%
    DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase. DAS-5-oCRBN has antiproliferative activity in both c-Src-dependent cell lines.
    DAS-5-oCRBN
  • HY-163814
    CDK2 degrader 1 3036604-59-5 99.74%
    CDK2 degrader 1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers (Red: spiro[3.3]heptan-2- ylmethyl carbonochloridate; Blue: N,N-diisopropylethylamine; Black: linker).
    CDK2 degrader 1
  • HY-152154
    Nampt degrader-2 3035008-40-0 99.41%
    Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD+ and exerts potent antitumor activities.
    Nampt degrader-2
  • HY-111758
    PROTAC B-Raf degrader 1 2364367-27-9 99.78%
    PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.
    PROTAC B-Raf degrader 1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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