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-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-151593
    dBRD4-BD1 2839318-19-1 98.02%
    dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1.
    dBRD4-BD1
  • HY-173011
    RJS308
    RJS308 is the PROTAC degrader for cyclosporin A (CypA) with a DC50 of 284 nM. RJS308 exhibits antiviral activcity through inhibition of HIV-1 and HCV replication. (Pink: ligand for target protein CypA ligand-2 (HY-173012); Black: linker (HY-W123015); Blue: ligand for E3 ligase VHL (S,R,S)-AHPC-Me (HY-112078))
    RJS308
  • HY-156744
    DBr-1 98.87%
    DBr-1 is a potent BRD9 PROTAC degrader (KD: 13 nM). DBr-1 can overcome intrinsic resistance to VHL-degrader. Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BRD9/BRD7 bromodomains inhibitor (HY-100352).
    DBr-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-115568
    BETd-246 2140289-17-2 98.34%
    BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.
    BETd-246
  • HY-111593
    Homo-PROTAC pVHL30 degrader 1 2244684-49-7 99.40%
    Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC, consists of two ligands of von Hippel-Lindau.
    Homo-PROTAC pVHL30 degrader 1
  • HY-135382A
    PROTAC IRAK4 degrader-3 2374122-43-5
    PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau.
    PROTAC IRAK4 degrader-3
  • 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-112377
    MZP-55 2010159-48-3 99.94%
    MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 8 nM for Brd4BD2.
    MZP-55
  • HY-130714
    TD-165 2305936-56-3 98.01%
    TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a?cereblon (CRBN)?ligand binding group, a linker and an?von Hippel-Landau (VHL)?binding group.
    TD-165
  • HY-133120A
    INY-03-041 trihydrochloride 98.44%
    INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively.
    INY-03-041 trihydrochloride
  • HY-112375
    AT6 2098836-50-9 99.93%
    AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 with highly selectivity to bromodomain (Brd4).
    AT6
  • HY-122830
    DD-03-171 2366132-45-6 98.72%
    DD-03-171 is a PROTAC BTK degrader. DD-03-171 inhibits mantle cell lymphoma (MCL) cell proliferation (IC50 = 5.1 nM) and prolongs the survival of mice bearing a lymphoma PDX model by degrading BTK, IKFZ1, and IKFZ3. DD-03-171 also inhibits platelet function and thrombosis. (Pink: BTK ligand 9 (HY-168292); Black: linker (HY-28875); Blue: Thalidomide-NH-CH2-COOH (HY-131717)).
    DD-03-171
  • 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. (Pink: BI 7271: HY-123616, Blue: 5-Aminothalidomide: HY-W023573, Blue + Black: Thalidomide-5-piperazine: HY-W834174, Black: N,N'-Dimethylpiperazine: HY-W539783).
    PROTAC BRD9 Degrader-7
  • HY-141877B
    MS4322 (isomer) 2601727-80-2 99.22%
    MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
    MS4322 (isomer)
  • HY-153598
    LD4172 2782022-40-4 98.12%
    LD4172 is a PROTAC degrader for RIP kinase (RIPK1) with DC50 in nanomolare levels. LD4172 induces apoptosis in cell B16F10 with combination of TNF-α. LD4172 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-170613); Black: linker (HY-W012241); Blue: ligand for E3 ligase VHL (HY-112078))
    LD4172
  • HY-149428
    AD4 2918262-09-4 98.01%
    AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy.
    AD4
  • HY-143275
    HL-8 2766352-64-9 99.17%
    HL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277); Blue: E3 ligase VHL ligand (HY-138678); Black: linker (HY-W002042)).
    HL-8
  • HY-152263
    HEMTAC CDK4/6 degrader 1 2821803-61-4 98.18%
    HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer. HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HEMTAC CDK4/6 degrader 1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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