2. Signaling Pathways
  3. PROTAC
  4. PROTACs

PROTACs

PROTACs

Related Products

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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-152134
    HDAC6 degrader-3 2785404-83-1 98.12%
    HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin.
    HDAC6 degrader-3
  • HY-161410
    WH244 2941088-96-4 99.82%
    WH244 is a second generation BCL-2 and BCL-xL dual depressant (PROTAC). The primary activity of WH244 is the specific degradation of BCL-2 and BCL-xL proteins (BCL-xL: DC50=0.6 nM, BCL-2: DC50=7.4 nM). WH244 promotes their ubiquitination and subsequent proteasome degradation by targeting these proteins, thereby restoring the cell's apoptosis pathway. WH244 has good antitumor activity.
    WH244
  • HY-168641
    PROTAC HIF-1α degrader-1 98.02%
    PROTAC HIF-1α degrader-1 (compound V2) is a potent hypoxia-inducible factor-1α (HIF-1α) PROTAC degrader with an IC50 value of 7.54 µM. PROTAC HIF-1α degrader-1 shows anti-proliferative activity. PROTAC HIF-1α degrader-1 decreases the HIF-1α protein expression. PROTAC HIF-1α degrader-1 induces apoptosis.
    PROTAC HIF-1α degrader-1
  • HY-146324
    PROTAC eEF2K degrader-1 2458170-54-0 98.64%
    PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells. PROTAC eEF2K degrader-1 mediates eEF2K degradation.
    PROTAC eEF2K degrader-1
  • HY-137465
    CG428 2412055-93-5 98.26%
    CG428 is a potent and selective CRBN-dependent tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1 phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). CG428 can be used for the research of colorectal carcinoma.
    CG428
  • HY-153415
    PROTAC BCR-ABL Degrader-1 3079412-59-9 98.73%
    PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. PROTAC BCR-ABL Degrader-1 induces Bcr-Abl degradation in a ubiquitinproteasom-dependent manner. PROTAC BCR-ABL Degrader-1 exhibits antiproliferative activity against K562 cells, and has the potential to study cancer.
    PROTAC BCR-ABL Degrader-1
  • HY-147942
    MS9449 2772612-96-9 98.95%
    MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer.
    MS9449
  • HY-171830
    MS105 2408339-39-7 98.27%
    MS105 (YX39-105) is an orally active and selective protein tyrosine kinase 6 (PTK6) (BRK) PROTAC degrader. MS105 recruits VHL E3 ligase via a VHL ligand moiety, promotes PTK6 ubiquitination and proteasomal degradation, inhibits the proliferation and migration of breast cancer cells, and induces apoptosis. MS105 shows potential for use in breast cancer research.
    MS105
  • HY-159147
    SIA​​IS039 2570251-69-1 99.68%
    SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker).
    SIA​​IS039
  • HY-133737
    GAL-02-221 2409538-70-9 99.87%
    GAL-02-221 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GAL-02-221 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines.
    GAL-02-221
  • HY-161882
    PROTAC SMARCA2 degrader-8 2669027-50-1 99.54%
    PROTAC SMARCA2 degrader-8 (compound 1) is a potent SMARCA2 degrader with a DC50 of 28nM in A375 cells.
    PROTAC SMARCA2 degrader-8
  • HY-168518
    PROTAC CDK9 degrader-9 3117192-80-7 99.25%
    PROTAC CDK9 degrader-9 (compound 29) is a highly selective and efficient CDK9 degrader based on PROTAC technology. PROTAC CDK9 degrader-9 can be used in anti-cancer research.
    PROTAC CDK9 degrader-9
  • HY-158345
    PROTAC ATM degrader-1 2821804-13-9 98.01%
    PROTAC ATM degrader-1 is a ATM PROTAC degrader with a KD value of 1.17 nM. PROTAC ATM degrader-1 triggers DNA damage response, cell cycle arrest, and apoptosis in cancer cells via the ubiquitin-proteasome-dependent degradation pathway. PROTAC ATM degrader-1 can be used for research on colorectal cancer.
    PROTAC ATM degrader-1
  • HY-155361
    PROTAC BRD9 Degrader-7 3056013-04-5 99.29%
    PROTAC BRD9 Degrader-7 is an orally active, selective BRD9 PROTAC degrader (DC50 = 1.02 nM). PROTAC BRD9 Degrader-7 mediates BRD9 degradation via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-7 exhibits proliferation inhibitory activity in the MV4-11 cells. PROTAC BRD9 Degrader-7 can be used in the research of acute myeloid leukemia and other related malignancies.
    PROTAC BRD9 Degrader-7
  • HY-135312
    AZ'6421 2361115-35-5 98.13%
    AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer.
    AZ'6421
  • HY-153901
    PROTAC EGFR degrader 8 2925923-46-0 98.90%
    PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader. PROTAC EGFR degrader 8 degrades EGFR in HCC827 cell with a DC50 of 15.56 nM. PROTAC EGFR degrader 8 inhibits H1975, PC-9, HCC827 cell growth with IC50s of 7.72 nM, 121.9 nM, 14.21 nM. PROTAC EGFR degrader 8 can be used for research of cancer, especially NSCLC.
    PROTAC EGFR degrader 8
  • HY-161177
    PROTAC SARS-CoV-2 3CLPro degrader 2 98.59%
    PROTAC KRAS G12D degrader 2 is a peptidomimetic PROTAC specifically targeting the dimeric SARS-CoV-2 3CLPro protein. PROTAC KRAS G12D degrader 2 inhibits SARS-CoV-2 3CLPro with an IC50 of 21.2 μM. PROTAC KRAS G12D degrader 2 specifically binds to the active site of SARS-CoV-2 3CLPro. PROTAC KRAS G12D degrader 2 reduces protein levels of SARS-CoV-2 3CLPro without affecting cell viability. PROTAC KRAS G12D degrader 2 can be used for the study of viral infections in Coronavirus genera.
    PROTAC SARS-CoV-2 3CLPro degrader 2
  • HY-178861
    dCDK9-202 99.25%
    dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015)).
    dCDK9-202
  • HY-149324
    SP27 3034805-75-6 98.87%
    SP27 is a PROTAC that can selective degrades PLK4, with a DC50 of 19.5 nM. SP27 can be used for the research of breast cancer.
    SP27
  • HY-174444A
    PROTAC HDAC degrader-2 TFA
    PROTAC HDAC degrader-2 TFA is the trifluoroacetate salt of PROTAC HDAC degrader-2. PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs. ( Pink: HDAC ligand : (HY-174471), Blue: E3 ligase CRBN Ligand (HY-131717), E3 ligase ligand-linker conjugate (HY-174473)).
    PROTAC HDAC degrader-2 TFA
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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