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-176786
    MCB-36
    MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)).
    MCB-36
  • HY-150403
    XF067-68 2407452-79-1 99.56%
    XF067-68 (example 132) is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5). XF067-68 can be usde for the study of WDR5-mediated diseases. (Pink: target protein ligand (HY-141799); Blue: E3 ligase ligand (HY-173627); Black: linker (HY-Y0966); E3 ligase ligand + linker: HY-176517).
    XF067-68
  • HY-146231
    SS47 2636072-62-1
    SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy.
    SS47
  • HY-165298
    DGY-09-192 2504949-52-2
    DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM). DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN). DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers. (Pink: FGFR1/2 ligand (HY-160013), Blue: VHL Ligand (HY-112078), Black: Linker (HY-W020017)).
    DGY-09-192
  • HY-168037
    PROTAC PIN1 degrader-1 3038591-59-9
    PROTAC PIN1 degrader-1 (compound D4) is a PROTAC targeting PIN1, with a DC50=1.8 nM. The GI50 of PROTAC PIN1 degrader-1 to MDA-MB-468 is >30 μM. PROTAC PIN1 degrader-1 is composed of target protein ligand PIN1 ligand-1 (HY-168038) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part), and PROTAC linker (black part)[1].
    PROTAC PIN1 degrader-1
  • HY-175266
    MI1013
    MI1013 is a PROTAC PXR degrader (DC50 = 89 nM, Dmax = 82%). MI1013 degrades PXR in human hepatocellular carcinoma RG cells (HepaRG). MI1013 specifically and safely regulates CYP3A4 promoter activity through PXR degradation. MI1013 affects several key genes involved in sulfate conjugation (e.g., SULT1E1), bile acid synthesis (CYP7A1), gluconeogenesis (PCK1), ketone synthesis (HMGCS20), and hepatocyte proliferation (MKI67). (Pink: PXR ligand 3: HY-175267, Blue: Pomalidomide-propargyl ligand: HY-W410002, Pink + Black: PXR ligand-Linker Conjugate 1: HY-175268).
    MI1013
  • HY-168669
    PROTAC K-Ras Degrader-5 3052745-16-8
    pan-KRAS degrader 4 (compound 69) is a potent cereblon-based KRAS PROTAC degrader, with a DC50 of <100 nM. pan-KRAS degrader 4 shows anticancer effects. (Pink: ligand for target protein (HY-168671); Black: linker (HY-168670); Blue: E3 ligase ligand (HY-W733895)).
    PROTAC K-Ras Degrader-5
  • HY-171860
    FC-14369 3066894-28-5
    FC-14369 is a PROTAC degrader targeting HIV-1 Nef protein with a DC50 value of 160 nM. FC-14369 binds to both Nef and Cereblon E3 ubiquitin ligase via its bifunctional structure, inducing Nef ubiquitination and proteasomal degradation to restore cell-surface CD4 and MHC-I expression and inhibit HIV-1 replication. FC-14369 can be used in research on HIV infection and AIDS. (Pink: Nef ligand-2 (HY-171862); Black: Ethylenediamine (HY-Y0275); Blue: Thalidomide (HY-14658))
    FC-14369
  • HY-168201
    MJP6412
    MJP6412 is a potent degrader histone acetyltransferases p300/CBP, with DC50 of 1.6 and 1.2 nM for p300 and CBP, respectively. MJP6412 plays an important role in cancer research.
    MJP6412
  • HY-115718A
    PZ703b TFA 98.62%
    PZ703b TFA is a Bcl-xl PROTAC degradation agent that induces apoptosis and inhibits cancer cell proliferation for bladder cancer research.
    PZ703b TFA
  • HY-139340
    Photo-lenalidomide-acid 2363154-39-4
    Photo-lenalidomide-acid (compound 3) is a photacts consist of a ligand for an E3 ligase, a photoswitch, and a ligand for a protein of interest and enable optical control of protein degradation.
    Photo-lenalidomide-acid
  • HY-164977
    JCS-1 3093519-24-2 99.38%
    JCS-1 is a potent DcpS PROTAC degrader. JCS-1 non-covalently binds DcpS with a RG3039-based warhead and recruits the E3 ligase VHL. JCS-1 promotes ubiquitination and degradation of DcpS at nanomolar concentrations (DC50 in MOLM-14 cells: 87 nM). JCS-1 can be used for the research of AML and other DcpS-dependent genetic disorders (Pink: DcpS ligand (HY-102020); Blue: E3 ligase VHL ligand (HY-151227); Black: linker (HY-141230)).
    JCS-1
  • HY-174873
    AF151
    AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875)).
    AF151
  • HY-175839
    PROTAC EGFR degrader 15
    PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)).
    PROTAC EGFR degrader 15
  • HY-175252
    PROTAC EGFR degrader 14
    PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFRC797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFRWT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)).
    PROTAC EGFR degrader 14
  • HY-160415
    WD6305 98.06%
    WD6305 is a potent and selective METTL3-METTL14 PROTAC degrader. WD6305 has DC50 values of 140 nM and 194 nM for METTL3 and METTL14, respectively. WD6305 inhibits m6A modification and proliferation of AML cells, and induces apoptosis. WD6305 has antitumor activity.(Pink: UZH2 (HY-115717); Black: Linker; Blue: VHL ligand (HY-150803))
    WD6305
  • HY-139997
    DDC-01-163 2140806-84-2
    DDC-01-163 is a mutant-selective allosteric PROTAC-based EGFR degrader, with an IC50 of 45 nM (Pink: EGFR ligand (HY-151048); Black: linker (HY-W008005); Blue: CRBN ligand (HY-14658)).
    DDC-01-163
  • HY-169481
    AP-1 3027918-96-0
    AP-1 is a PROTAC targeting anaplastic lymphoma kinase (ALK). AP-1 is composed of PROTAC target protein ligand CS-1243648 (HY-169482) (red part), E3 ligase ligand Pomalidomide (HY-10984) (blue part) and PROTAC Linker 2-(Tert-Butoxy)-2-oxoacetic acid (HY-W687662) (black part).
    AP-1
  • HY-133136
    PROTAC BRD4 Degrader-2 2185795-53-1
    PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 14.2 nM against BRD4 BD1.
    PROTAC BRD4 Degrader-2
  • HY-128839
    PROTAC ERRα Degrader-2 2306388-85-0
    PROTAC ERRα Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.
    PROTAC ERRα Degrader-2
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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