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-141512
    JB170 2705844-82-0 98.97%
    JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.
    JB170
  • HY-138669
    C004019 2417159-57-8 99.37%
    C004019 is a BBB-penatrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases. (Pink: Ligand for target protein (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))
    C004019
  • HY-169179
    AK-1690 2984505-88-4
    AK-1690 is a potent and selective STAT6 PROTAC degrader. AK-1690 reduces the levels of STAT6 protein in cells (DC50=1 nM) and depletes STAT6 protein in mouse tissues. AK-1690 can be used for the research of cancer. (Pink: ligand for target protein STAT6 (HY-169182); Black: linker (HY-W459522); Blue: ligand for E3 ligase (HY-131318).
    AK-1690
  • HY-125835
    CP-10 2366268-80-4 98.41%
    CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6.
    CP-10
  • HY-125878
    PROTAC SGK3 degrader-1 2381320-35-8 99.89%
    PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate).
    PROTAC SGK3 degrader-1
  • HY-117690
    dBRD9 2170679-45-3 99.89%
    dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family.
    dBRD9
  • HY-154984
    JET-209 98.07%
    JET-209 is a potent PROTAC CBP/p300 degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 contains Lenalidomide (HY-A0003) (the cereblon ligand), a linker and GNE-207 (HY-120028) (bromodomain Inhibitor). JET-209 is used for cancer research.
    JET-209
  • HY-151902
    SJ988497 2595365-41-4 98.05%
    SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL).
    SJ988497
  • HY-103628
    PROTAC CDK9 Degrader-1 2118356-96-8 98.03%
    PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.
    PROTAC CDK9 Degrader-1
  • HY-130602
    MS432 2672512-44-4 99.78%
    MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
    MS432
  • HY-145696
    SJ10542 2789678-92-6 99.92%
    SJ10542 is a potent and selective JAK2/3 directing phenyl glutarimide (PG)-PROTAC with DC50s of 14, 11, and 24 nM for JAK2, JAK3, and JAK2-fusion ALL, respectively. SJ10542 utilizes a PG ligand as the cereblon (CRBN) recruiter.
    SJ10542
  • HY-153713
    MYC-RIBOTAC 98.05%
    MYC-RIBOTAC is a nucleic acid-targeting degrader (ribonuclease-targeting chimera, RIBOTAC) that targets the MYC internal ribosome entry site (IRES). MYC-RIBOTAC contains a MYC mRNA binding component and a small molecule that recruits and locally activates RNAse L1. MYC-RIBOTAC reduces MYC mRNA and protein expression levels, induces cell apoptosis, and can be used for antitumor research. MYC-RIBOTAC consists of pre-miR-155 binder Anticancer agent 167 (HY-156839), RNA binder NCI-B16 (HY-156215), and Linker Amino-PEG4-alcohol (HY-W008005).
    MYC-RIBOTAC
  • HY-145816A
    JPS016 TFA 98.70%
    JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
    JPS016 TFA
  • HY-155994
    PIK5-12d 99.90%
    PIK5-12d is a PROTAC PIKfyve degrader (DC50: 1.48 nM). PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d has anti-tumor activity.
    PIK5-12d
  • HY-162723
    FOSL1 degrader 1 99.47%
    FOSL1 degrader 1 (4) is a T-5224-PROTAC, potently degrade FOSL1 (AP-1) to suppress cancer stemness gene expression in HNSCC. FOSL1 degrader 1 (4) effectively eliminate HNSCC cancer stem cells to inhibit tumor growth through degrading FOSL1. FOSL1 degrader 1 (4) displays around 30- to 100-fold increased potency over T-5224 (Pink: T-5224 (HY-12270); Black: Linker (HY-130200); Blue: Pomalidomide (HY-10984)).
    FOSL1 degrader 1
  • HY-111866
    PROTAC RIPK degrader-2 1801547-16-9 99.48%
    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-130644
    iRucaparib-AP6 2410557-00-3 99.27%
    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-137487
    PROTAC BRAF-V600E degrader-1 2417296-84-3 98.02%
    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. (In the molecular structure, target protein ligand: BI-882370 (HY-107779), red part; E3 ubiquitin enzyme ligand: Pomalidomide (HY-10984), blue part; PROTAC linker: G007-LK (HY-12438), black part.
    PROTAC BRAF-V600E degrader-1
  • HY-151110A
    PROTAC CDK12/13 Degrader-1 TFA 98.37%
    PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research.
    PROTAC CDK12/13 Degrader-1 TFA
  • HY-151101
    MS159 3031353-59-7 98.28%
    MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease.
    MS159
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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