1. Signaling Pathways
  2. PROTAC
  3. PROTACs

PROTACs

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.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-182577
    CFT-743 2154350-81-7
    CFT-743, a PROTAC-based heterobifunctional degrader and BET inhibtor, is a degrader of BRD4 bromodomain 1 (BD1) with a DC50 of 4.3 nM. CFT-743's antitumor activitiy is dependent on BET degradation and can be attenuated by Pomalidomide (HY-10984), which is a CRBN binding molecule. CFT-743 induces ubiquitination of BRD4 BD1. CFT-743 can be used for cancer research.
    CFT-743
  • HY-185009
    GSK702 2260944-69-0
    GSK702, a PROTAC, is a the less active cis-(S,S)-enantiomer of GSK983 (P300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) PROTAC). GSK702 induces only a small decrease of PCAF protein levels. GSK702 binds to CRBN and causes a reduction of IL-1β in macrophages. GSK702 can be used for the study of inflammatory mediators.
    GSK702
  • HY-175036
    YTHu78
    YTHu78 is a KDM5B PROTAC-type degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 exhibits significant antiproliferative activity against a variety of hematological cancer cell lines and can be used to study hematological cancers. (Pink: KDM5B ligand: (HY-116761); Blue: Thalidomide ligand: (HY-14658), Black + Pink: KDM5B ligand + linker: (HY-175145)).
    YTHu78
  • HY-115873
    Folate-MS432 2769735-56-8
    Folate-MS432, a PROTAC, is capable of degrading MEKs in a folate receptor-dependent manner in cancer cells.
    Folate-MS432
  • HY-111840
    PROTAC CRABP-II Degrader-1 1225383-40-3
    PROTAC CRABP-II Degrader-1 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand.
    PROTAC CRABP-II Degrader-1
  • HY-184225
    PROTAC TEAD degrader-3 3120075-62-6
    PROTAC TEAD degrader-3 is a TEAD PROTAC degrader with an IC50 of < 5 nM against TEAD1, TEAD2, TEAD3 and TEAD4. PROTAC TEAD degrader-3 promotes ubiquitination and degradation of TEAD1/2/3/4. PROTAC TEAD degrader-3 can be used in cancer research.
    PROTAC TEAD degrader-3
  • HY-180959
    NEP168 3031840-37-3
    NEP168 is an ERα PROTAC degrader designed based on the GID4 E3 ligase. NEP168 can be used for the study of breast cancer.
    NEP168
  • HY-159458
    PROTAC SMARCA2/4-degrader-7 2568277-89-2
    SMARCA2/4-degrader-7 (compound I-439) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment.
    PROTAC SMARCA2/4-degrader-7
  • HY-139294
    PROTAC BRD4 Degrader-15 2417370-67-1
    PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
    PROTAC BRD4 Degrader-15
  • HY-184233
    C9S
    C9S is an As (III)-PROTAC and arsenic-binding protein PROTAC degrader. C9S promotes the ubiquitination and degradation of arsenic-binding proteins such as Glutathione reductase. C9S binds to metallothionein. C9S exhibits anticancer activity against lung cancer. C9S can be used in lung cancer-related research.
    C9S
  • HY-183768
    PROTAC FAK degrader 5
    PROTAC FAK degrader 5 is a potent PROTAC degrader targeting FAK, with a DC50 of 11.65 nM. PROTAC FAK degrader 5 induces FAK protein degradation, selectively inhibits colony formation of human colorectal cancer HCT116 cells, and blocks the proliferation of human umbilical vein endothelial HUVEC cells, exhibiting anti-angiogenic activity. PROTAC FAK degrader 5 can be used in the research of colorectal cancer and angiogenesis.
    PROTAC FAK degrader 5
  • HY-174247
    CPS-021
    CPS-021 is a selective PAK4 PROTAC degrader with a DC50 of 50 nM. CPS-021 has potent antimigratory and invasive activity and significantly suppresses the invasion and metastasis of tumor cells in A549-luc lung metastasis mice model. Pink: PAK4 ligand (HY-174822); Blue: CRBN ligase ligand (HY-10984); Black: linker
    CPS-021
  • HY-155075
    NC-R17 3049087-34-2
    NC-R17 is a PROTAC-class, non-covalent GPX4 degrader based on RSL3, involved in ferroptosis. NC-R17 has antitumor activity and is used for non-covalent GPX4 PROTAC design. NC-R17 consists of a target protein ligand (red part) Demethyl-RSL3 (HY-135832); an E3 ubiquitin ligase ligand (blue part) Lenalidomide (HY-A0003) and a PROTAC linker (black part) (HY-169376). E3 ubiquitin ligase and linker can form Lenalidomide-C13-piperazine-Boc (HY-169377).
    NC-R17
  • HY-172124
    PROTAC BRD4 Degrader-29
    PROTAC BRD4 Degrader-29 (compound 7a) is a potent PROTACs degrader of BRD4, with the DC50 of 89.4 nM. PROTAC BRD4 Degrader-29 plays an important role in cancer research (Pink: ligand for target protein (HY-13030); Black: linker (HY-172125); Blue: E3 ligase ligand (HY-103597)).
    PROTAC BRD4 Degrader-29
  • HY-163875
    PROTAC SMARCA2/4-degrader-22 2568277-48-3
    SMARCA2 degrader-14 (compound I-408) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment.
    PROTAC SMARCA2/4-degrader-22
  • HY-149679
    PROTAC eDHFR Degrader-2 2849442-91-5
    PROTAC eDHFR Degrader-2 (compound 7b) is a potent degrader targeting Escherichia coli dihydrofolate reductase (eDHFR), enabling robust degradation of eDHFR-tagged proteins.
    PROTAC eDHFR Degrader-2
  • HY-176035
    MS479
    MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695); Blue: GLP ligand (HY-176036); Black: linker (HY-176037); GLP ligand+linker: HY-176038).
    MS479
  • HY-159947
    PROTAC BTK Degrader-11 2736508-94-2
    PROTAC BTK Degrader-11 is a PROTAC degrader that can break down BTK, with a DC50 of 1.7 nM. PROTAC BTK Degrader-11 can be used in cancer research.
    PROTAC BTK Degrader-11
  • HY-162835
    PROTAC SMARCA2/4-degrader-28 2409844-88-6
    PROTAC SMARCA2/4-degrader-28 (PROTAC 1) is a PROTAC-based partial degrader of SMARCA2 and SMARCA4(Bliue: CRL2VHL ligand (S,R,S)-AHPC (HY-125845); Black: linker (HY-159680); Pink: a SMARCA-BD ligand (+)-JQ-1 (HY-13030)).
    PROTAC SMARCA2/4-degrader-28
  • HY-181296
    PROTAC EZH2 Degrader-16 3093642-22-6
    PROTAC EZH2 Degrader-16 (compound 51) is a PROTAC protein degrader targeting EZH2 with an IC50 of 13.74 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-16 exerts antiproliferative activity against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-16 can be used for the research of diffuse large B-cell lymphoma.
    PROTAC EZH2 Degrader-16
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