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-173250
    YN14-H
    YN14-H is a PROTAC degrader targeting KRASG12C. YN14-H inhibits cell growth in NCI-H358 and MIA PaCa-2 cells (IC50 values of 0.042, 0.021 μM, DC50 values of 28.9, 18.1 nM, respectively). YN14-H significantly induces apoptosis and inhibits migration. YN14-H demonstrates favorable pharmacokinetic properties and excellent antitumor activity in vivo.
    YN14-H
  • HY-168242
    PROTAC BRM/BRG1 degrader-1 2724268-88-4
    PROTAC BRM/BRG1 degrader-1 (Example 253) is a PROTAC BRM/BRG1 degrader, with DC50 of 10-100 nM for BRM, > 1 μM for BRG1. PROTAC BRM/BRG1 degrader-1 can be used for cancer research.
    PROTAC BRM/BRG1 degrader-1
  • HY-180970
    TD-004 2162120-55-8
    TD-004 is a potent ALK PROTAC degrader. TD-004 exhibits anti-ALK inhibitory activity with an IC50 of 0.11 µM and selectively inhibits the proliferation of SU-DHL-1 and H3122 cells (ALK-positive cancer cells) with IC50s of 0.058 µM and 0.28 µM, respectively. TD-004 induces degradation of ALK fusion proteins (NPM-ALK and EML4-ALK) via recruitment of the VHL E3 ligase and the proteasome pathway. TD-004 demonstrates significant tumor growth inhibition with a favorable safety profile in vivo. TD-004 can be used for the research of anaplastic large cell lymphoma and non-small cell lung cancer.
    TD-004
  • HY-159728
    PROTAC PRMT3 degrader 1
    PROTAC PRMT3 degrader 1 is a selective PRMT3 PROTAC degrader with a DC50 of 2.566 μM. PROTAC PRMT3 degrader 1 forms a ternary complex with MDM2 E3 ubiquitin ligase to induce proteasomal and neddylation-dependent degradation of PRMT3. PROTAC PRMT3 degrader 1 activates intrinsic apoptosis, endoplasmic reticulum stress signaling pathways. PROTAC PRMT3 degrader 1 downregulates E2F, MYC, oxidative phosphorylation pathways. PROTAC PRMT3 degrader 1 reduces cellular asymmetric dimethylarginine (ADMA) levels. PROTAC PRMT3 degrader 1 inhibits acute leukemia cell growth. PROTAC PRMT3 degrader 1 acts with glycolysis inhibitor 2-DG to reduce ATP production, induce intrinsic apoptosis, drive synergistic antiproliferative effects. PROTAC PRMT3 degrader 1 can be used for the research of acute leukemia.
    PROTAC PRMT3 degrader 1
  • HY-168274
    PROTAC TRIB2 degrader-1 3100306-42-8
    PROTAC TRIB2 degrader-1 (Compound 5k) is an effective TRIB2 degrader that selectively induces TRIB2 degradation through the CRBN-dependent ubiquitin-proteasome pathway. PROTAC TRIB2 degrader-1 can inhibit cell proliferation and induce cell apoptosis, and can be used in cancer research.
    PROTAC TRIB2 degrader-1
  • HY-144657
    (4S)-PROTAC SOS1 degrader-1 2913176-81-3
    (4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo.
    (4S)-PROTAC SOS1 degrader-1
  • HY-179424
    PROTAC HIF-1α degrader-2 3095636-64-6
    PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer.
    PROTAC HIF-1α degrader-2
  • HY-131188
    PROTAC Bcl-xL degrader-1 2450351-07-0
    PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively.
    PROTAC Bcl-xL degrader-1
  • HY-129937
    (S)-GNE-987 2738533-33-8
    (S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).
    (S)-GNE-987
  • HY-179732
    PROTAC ALK degrader-4
    PROTAC ALK degrader-4 (Compound B8) is an ALK PROTAC degrader with a DC50 of 445.25 nM. PROTAC ALK degrader-4 exhibits excellent anti-proliferative activity against NCI-H2228 and NCI-H3122. PROTAC ALK degrader-4 leads to a significant downregulation of 390 proteins, including IGF-1R and its downstream proteins such as ERK1/2 and STAT3. PROTAC ALK degrader-4 can be used for research on lung adenocarcinoma. (Pink: ALK ligand (HY-15656); Blue: CRBN ligand (HY-179733); Black: linker).
    PROTAC ALK degrader-4
  • HY-186015
    Arg-TERRα 2408832-28-8
    Arg-TERRα is a mini-PROTAC targeting ERRα. Arg-TERRα induces ERRα degradation via the N-end rule pathway, thereby in inhibiting the proliferation and migration of MCF7 breast cancer cells. Arg-TERRα can be used for breast cancer research.
    Arg-TERRα
  • HY-178066
    PROTAC BCL-xL/BCL-w Degrader 1
    PROTAC BCL-xL/BCL-w Degrader 1 (Compound 44) is a BCL-xL/BCL-w PROTAC degrader. PROTAC BCL-xL/BCL-w Degrader 1 has significant anticancer activity with reduced on-target platelet toxicity . Pink: BCL-xL/BCL-w ligand (HY-10087); Blue: CRBN ligase ligand (HY-163233); Black: linker (HY-Y1230)
    PROTAC BCL-xL/BCL-w Degrader 1
  • HY-158048
    UNC9036 3094059-54-5
    UNC9036 is a PROTAC-based STING degrader, with a DC50 of 227 nM. UNC9036-mediated STING degradation is proteasome and VHL dependent (Structure Note: Red, STING agonist diABZI (HY-112921A); Blue, VHL ligand VH032 (HY-120217); Black, linker).
    UNC9036
  • HY-168678
    PROTAC K-Ras Degrader-6 3052745-46-4
    PROTAC K-Ras Degrader-6 (compound 102) is a potent cereblon-based KRAS PROTAC degrader, with a DC50 of ≤100 nM. PROTAC K-Ras Degrader-6 shows anticancer effects.
    PROTAC K-Ras Degrader-6
  • HY-156401
    BRD9 Degrader-1
    BRD9 c-1 (Compound 13-7) is a PROTAC BRD9 degrader. BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062).
    BRD9 Degrader-1
  • HY-145400
    PROTAC BRD9 Degrader-3 2633632-05-8
    PROTAC BRD9 Degrader-3 is a BRD9 bifunctional degrader for researching cancer.
    PROTAC BRD9 Degrader-3
  • HY-153322
    ITK degrader 2 2858738-65-3
    ITK degrader 2 is an orally active ITK PROTAC degrader with a DC50 < 0.001 nM. ITK degrader 2 degrades ITK via the ubiquitin-proteasome pathway. ITK degrader 2 can be used in the research of cancer, autoimmune diseases and inflammatory diseases.
    ITK degrader 2
  • HY-174135
    PROTAC HPK1 Degrader-4
    PROTAC HPK1 Degrader-4 (compound E3) is a selective and orally active PROTAC HPK1 degrader with a DC50 of 3.16 nM. PROTAC HPK1 Degrader-4 demonstrates >1000-fold selectivity over GLK. PROTAC HPK1 Degrader-4 promotes immune activation. PROTAC HPK1 Degrader-4 can be used for the study of colon cancer and lymphoma (Pink: ligand for target protein (HY-174355); Blue: ligand for E3 ligase CRBN (HY-45808); Black: Linker (HY-174356); Target protein ligand-linker Conjugate (HY-174357)).
    PROTAC HPK1 Degrader-4
  • HY-162651
    PROTAC BRD9 Degrader-8 3081180-48-2
    PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma.
    PROTAC BRD9 Degrader-8
  • HY-169151
    PROTAC BRD4-DCAF1 degrader-1 3036944-87-0
    PROTAC BRD4-DCAF1 degrader-1 (I-907) is a BRD4-DCAF1 PROTAC degrader, DC50 is 10~100 nM. .
    PROTAC BRD4-DCAF1 degrader-1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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