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-137342
    SB1-G-187 2769753-18-4 98.70%
    SB1-G-187, a PROTAC, is a multi-kinase degrader. SB1-G-187 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SB1-G-187
  • HY-147330A
    SJ1008030 TFA 2863634-97-1 99.81%
    SJ1008030 (compound 8) TFA is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 TFA inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 TFA can be used for the research of leukemia.
    SJ1008030 TFA
  • HY-123961
    SJF-8240 2230821-68-6 99.33%
    SJF-8240 (PROTAC 7) is a proteolysis targeting chimera (PROTAC) degrader. SJF-8240 induces polyubiquitination of c-Met and inhibits the proliferation of GTL16 cells (IC50=66.7 nM).
    SJF-8240
  • HY-163677
    ARM165 99.75%
    ARM165 is a heterobifunctional molecule. ARM165 degrades the PIK3CG proteins, inhibits PI3Kγ-Akt signaling pathway, and thus exhibits antileukemia efficacy. ARM165 inhibits proliferations of AML cells, with IC50 <1 μM. (Pink: ligand for target protein PI3Kγ inhibitor AZ2 (HY-111570); Black: linker; Blue: ligand for E3 ligase Pomalidomide (HY-10984))
    ARM165
  • HY-148274
    KTX-582 2573298-13-0 98.65%
    KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model.
    KTX-582
  • HY-150259
    MDEG-541 98.05%
    MDEG-541 is a potent MYC-MAX degrader. MDEG-541 is a PROTAC that based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide (HY-14658). MDEG-541 shows antiproliferative activity. MDEG-541 decreases the expression of GSPT1, MYC, GSPT2, PLK1 protein.
    MDEG-541
  • HY-139659
    ARD-61 2316837-08-6 99.68%
    ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ARD-61
  • HY-145737A
    PROTAC SOS1 degrader-1 TFA 99.38%
    PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity.
    PROTAC SOS1 degrader-1 TFA
  • HY-157570
    Anti-inflammatory agent 70 2767427-87-0
    Anti-inflammatory agent 70 (N-Me-SP23) is a STING protein PROTAC degrader and inhibits the STING signaling pathway. Anti-inflammatory agent 70 has anti-inflammatory activity. (Pink: STING inhibitor (HY-47709); Black: linker (HY-W008296); Blue: CRBN Ligand (HY-W460193)).
    Anti-inflammatory agent 70
  • HY-131865
    SJF-1521 2230821-40-4 99.65%
    SJF-1521 is a selective EGFR PROTAC degrader. SJF-1521 contains the EGFR inhibitor lapatinib (HY-50898). SJF-1521 can induce EGFR degradation in OVCAR8 cells.
    SJF-1521
  • HY-112098
    PROTAC ERα Degrader-1 2417369-94-7
    PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
    PROTAC ERα Degrader-1
  • HY-145125
    SJ995973 2882065-25-8 98.84%
    SJ995973 (PROTAC) is a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins.
    SJ995973
  • HY-158239
    MS181 98.36%
    MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717).
    MS181
  • HY-114323
    PROTAC FLT-3 degrader 1 2230826-81-8 99.74%
    PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor. (Pink: FLT3 ligand (HY-168702); Black: Linker (HY-124380); Blue: VHL ligand (HY-125845)).
    PROTAC FLT-3 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-138635
    PROTAC BRD4 Degrader-12 2417370-90-0 99.85%
    PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-12 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.39 nM and 0.24 nM, respectively.
    PROTAC BRD4 Degrader-12
  • HY-162362
    MS8709 3060730-06-2 98.91%
    MS8709 (compound 10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker).
    MS8709
  • HY-168016
    PROTAC YAP degrader-1 3058483-58-9 99.77%
    PROTAC YAP degrader-1 (compound YZ-6) is a PROTAC targeting YAP and also inhibits the nuclear localization of YAP. PROTAC YAP degrader-1 is composed of PROTAC target protein ligand NSC682769 (HY-168017) (red part) and E3 ubiquitin ligase ligand + Linker conjugate (R,S,R)-AHPC-PEG2-C2-boc (HY-168019) (blue+black part), in which the PROTAC Linker used is Acid-PEG2-C2-Boc (HY-140480) and the target protein ligand activity control is Demethyl-NSC682769 (HY-168018)[1].
    PROTAC YAP degrader-1
  • HY-155815
    MS9715
    MS9715 is a potent and seletive NSD3-targeting PROTAC. MS9715 is designed by BI-9321, which binds NSD3’s PWWP1 domain, with an E3 ligase VHL ligand. MS9715 has the potental for NSD3-dependent cancer treatment research.
    MS9715
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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