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-170808
    PROTAC BRD4 Degrader-28
    PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-28 is promising for research of cancers (Pink: target protein ligand JQ-1 (carboxylic acid) (HY-78695); Black+ Blue: E3 ubiquitin ligase ligand-Linker conjugate Thalidomide-O-amido-C3-NH2 (HY-115560)).
    PROTAC BRD4 Degrader-28
  • HY-155685
    SA-VA
    SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase.
    SA-VA
  • HY-162875
    PROTAC BRD4 Degrader-27 2407163-44-2
    PROTAC BRD4 Degrader-27 (compound 6b) is a PROTAC that selectively targets BRD4 (rather than BRD2/BRD3) and can also inhibit the expression of KLF5 transcription factor and exert anti-cancer activity. PROTAC BRD4 Degrader-27 is composed of E3 ubiquitinase ligand Thalidomide-4-OH (HY-103596) (red part), PROTAC Linker γ-Aminobutyric acid (HY-N0067) (black part) and PROTAC target protein ligand PROTAC BRD4 ligand-3 (HY-162876) (blue part), of which the active control of the target protein ligand is Mivebresib (HY-100015), and the conjugate of E3 ubiquitin ligase ligand + Linker is Pomalidomide 4'-alkylC3-acid (HY-131875)[1].
    PROTAC BRD4 Degrader-27
  • HY-168453
    dBAZ2B 3104449-58-0
    dBAZ2B is a BAZ2B PROTAC degrader, with a DC50 of 19 nM. (Pink: BAZ2A/B ligand (HY-168449); Black: linker (HY-168450); Blue: VHL Ligand (HY-125905))
    dBAZ2B
  • HY-162281
    PROTAC SOS1 degrader-6 3032282-51-9
    PROTAC SOS1 degrader-6 (compound 23) is an effective SOS1 PROTACs degrader that synergizes with KRASG12C inhibitors. PROTAC SOS1 degrader-6 consists of the target protein ligand (red part) SOS1 Ligand intermediate-7 (HY-169371), E3 ubiquitin ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and PROTAC linker (black part) 5-Bromopentanoic acid (HY-W016456). Among them, the E3 ubiquitin ligase ligand + linker can form (S,R,S)-AHPC-CO-C4-bromine (HY-169372).
    PROTAC SOS1 degrader-6
  • HY-147654
    PROTAC Hemagglutinin Degrader-1 3031330-66-9
    PROTAC Hemagglutinin Degrader-1 (Compound V3) is a potent PROTAC influenza hemagglutinin (HA) degrader with a median degradation concentration of 1.44 μM. PROTAC Hemagglutinin Degrader-1 shows broad-spectrum anti-influenza virus activity.
    PROTAC Hemagglutinin Degrader-1
  • HY-161750
    PROTAC ALK degrader-2
    PROTAC ALK degrader-2 (B1-PEG) is an ALK degrader based on PROTACs, with the DC50 of 45 nM in H3122 EML4-ALK DC50 (GSH+). PROTAC ALK degrader-2, through PEGylation, is engineered to self-organize into micelles in water and releases its active form in response to the tumor-specific high GSH environment.
    PROTAC ALK degrader-2
  • HY-146397
    TD-802 2760703-21-5
    TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research.
    TD-802
  • HY-149917
    ITK degrader 1
    ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 consists of target protein ligand (red part) ITK ligand 1 (HY-168387), PROTAC linker (black part) Piperidine-C2-piperazine-Boc (HY-168388) and E3 ubiquitinase ligand (blue part) Thalidomide 5-fluoride (HY-W087383). E3 ubiquitinase and PROTAC linker can form Thalidomide-piperidine-C2-piperazine-Boc (HY-168389).
    ITK degrader 1
  • HY-168225
    PROTAC SMARCA2/4-degrader-35 2933253-85-9
    PROTAC SMARCA2/4-degrader-35 (Ex.43) is a SMARCA2/4 degrader with a DC50 <2.5 nM. (Target ligand: HY-W874018; E3 ligand: HY-168226; linker: HY-168227; E3 ligand+linker: HY-168228)
    PROTAC SMARCA2/4-degrader-35
  • HY-157426
    GSPT1 degrader-3
    GSPT1 degrader-3 (Pro-2) is a CRBN-based PROTAC degrader for BRD, with a DC50 of 21.1 nM (4h).
    GSPT1 degrader-3
  • HY-175849
    ALK degrader 1
    ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research.
    ALK degrader 1
  • HY-132857
    ZXH-4-130 2711006-66-3
    ZXH-4-130 is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC).
    ZXH-4-130
  • HY-175225
    PROTAC BRD4 Degrader-37
    PROTAC BRD4 Degrader-37 (Compound TrimTAC-2) is a PROTAC BRD4 degrader. PROTAC BRD4 Degrader-37 has a DC50 of 36.4 nM and a Dmax of 73% in PANC-1 cells. PROTAC BRD4 Degrader-37 exhibits cytotoxicity against PANC-1 cells (GI50: 0.282 μM). PROTAC BRD4 Degrader-37 can be used in the research of tumors. (Pink: PROTAC BRD4 ligand-4 (HY-175242); Blue + Black: E3 ligase ligand + linker (HY-175241)).
    PROTAC BRD4 Degrader-37
  • HY-175547
    PROTAC HPK1 Degrader-5
    PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy (Pink: Target protein ligand (HY-175549); Blue: E3 ligand (HY-W023573); Black: Linker; E3 ligand + Linker (HY-175551)).
    PROTAC HPK1 Degrader-5
  • HY-175370
    PROTAC RIPK1 Degrader-1
    PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma. (Pink: RIPK1-ligand-2: HY-175371, Blue: (S,R,S)-AHPC-Me: HY-112078, Pink + Black: RIPK1 ligand-Linker Conjugate-1: HY-175374, Black: Bispiperidin-piperazin-acetater: HY-175373).
    PROTAC RIPK1 Degrader-1
  • HY-178360
    NP1192 2966791-41-1
    NP1192 is a potent, selective PROTAC NAT10 degrader that depletes NAT10 protein and inhibits ac4C modification in cancer cells. NP1192 demonstrates dual inhibition of hypoxia-driven glycolysis and immunosuppression via NAT10/HIF-1α/PD-L1 axis disruption, achieving superior antitumor efficacy and synergizing with anti-PD-L1 both in vitro and in vivo. NP1192 can be used for ovarian, cervical, and glioblastoma cancer research. (Blue: CRBN ligand (HY-148834); Black: linker; Pink: NAT10 ligand (HY-16706)).
    NP1192
  • HY-168234
    PROTAC SMARCA2 degrader-31 2380274-45-1
    PROTAC SMARCA2-degrader-36 (compound 38) is a SMARCA2 degrader and can reach the the degradation rate of 99 % at the 100 nM in H929 cells. PROTAC SMARCA2-degrader-36 shows anti-proliferative activity and can be used for study of cancer(Structure Note: PINK SMARCA2 ligand HY-44012; Blue, VHL ligand (HY-112078); Black, linker HY-W014125).
    PROTAC SMARCA2 degrader-31
  • HY-168190
    PROTAC TBL1X degrader-1
    PROTAC TBL1X degrader-1 (Compound TD11) is a PROTAC degrader for Transducin β-like protein 1 X-linked (TBL1X), and exhibits cytotoxicity in lymphoma cell Riva, Pfeiffer and Granta-519 with IC50 of 0.795, 0.397 and 0.522 μM, respectively. (Pink: ligand for target protein: TBL1X ligand 1 (HY-168191); Black: linker (HY-168193); Blue: ligand for E3 ligase: Thalidomide 4-fluoride (HY-41547))
    PROTAC TBL1X degrader-1
  • HY-176449
    PROTAC BRD4 Degrader-32
    PROTAC BRD4 Degrader-32 (Compound 22) is a BRD4 PROTAC degrader (DC50: 0.20 nM). PROTAC BRD4 Degrader-32 connects the BRD4-binding domain and CRBN-binding domain through a unique carbon-carbon linked linker to form a ternary complex, inducing ubiquitination of BRD4 for proteasomal degradation. PROTAC BRD4 Degrader-32 is promising for research of BRD4-related cancers (such as hematological malignancies). (Pink: GSK1324726A (HY-13960); Black: linker (HY-176450); Blue: Lenalidomide-5-Br (HY-W072954)).
    PROTAC BRD4 Degrader-32
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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