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-147219A
    SIAIS164018 hydrochloride 98.06%
    SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857).
    SIAIS164018 hydrochloride
  • HY-114404
    SJFα 2254609-27-1 99.61%
    SJFα is a selective p38α PROTAC degrader with a DC50 of 7.16   nM and Dmax of 97.4%. SJFα is far less effective at degrading p38δ (DC50 = 299 nM). SJFαcan be used for the research of cancer, such as breast cancer. (Structure Note: Pink: p38α ligand (HY-45124); Blue: VHL ligand (HY-125845))
    SJFα
  • HY-172113
    H122 98.04%
    H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM, and exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki of 2.0, 3.6 and 1.6 nM. H122 downregulates the expression of Myc. H122 inhibits the cell growth of MSTO-211H and NCI-H226 with IC50 of 21.3 nM and 0.6 nM, and exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-151525); Black: linker (HY-W573128); Blue: ligand for E3 ligase Cereblon (HY-W087383))
    H122
  • HY-145159
    SHP2 protein degrader-1 2624181-69-5 98.94%
    SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases.
    SHP2 protein degrader-1
  • HY-157581
    MS39 2675490-92-1 99.89%
    MS39 (compound 6) is a PROTAC targeting EGFR. MS39 is composed of PROTAC target protein ligand N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-(piperazin-1-yl)propoxy)quinazolin-4-amine (HY-W109039) (red part), E3 ligase ligand (S,R,S)-AHPC (HY-125845) (blue part) and PROTAC Linker Undecanedioic acid (HY-W014125) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC-CO-C9-acid (HY-139345). MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells.
    MS39
  • HY-171139
    PROTAC HDAC6 degrader 2 99.80%
    PROTAC HDAC6 degrader 2 (Compound 1) is a HDAC6 PROTAC degrader, with IC50 of 0.643 μM. PROTAC HDAC6 degrader 2 promotes ubiquitination and degradation of HDAC6. PROTAC HDAC6 degrader 2 can be used for the research of haematological and solid cancers (Pink: HDAC6 ligand (HY-171141); Blue: E3 ligase CRBN ligand (HY-10984)).
    PROTAC HDAC6 degrader 2
  • HY-148290
    KTX-951 2573298-36-7 98.00%
    KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader (Kd = 3.5 nM). KTX-951 has DC50s of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. KTX-951 has IC50 of 35 nM for OCl-Ly10 CTG. KTX-951 has antitumor activity.(Pink: IRAK4 ligand-12 (HY-48932); Black: Linker (HY-W382009); Blue: CRBN Ligand Pomalidomide (HY-10984)).
    KTX-951
  • HY-145815A
    JPS014 TFA 98.40%
    JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
    JPS014 TFA
  • HY-139185
    PROTAC ERRα Degrader-3 2306388-65-6 98.82%
    PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
    PROTAC ERRα Degrader-3
  • HY-158342
    PROTAC TEAD degrader-1 3061498-57-2 99.82%
    PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293T cells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383))
    PROTAC TEAD degrader-1
  • HY-158764
    PROTAC BET Degrader-12 98.10%
    PROTAC BET Degrader-12 (Compound 8b) is a PROTAC degrader for bromodomain and extra-terminal domain (BET)-containing proteins, which degrades the BRD3 and BRD4 in a DCAF11-dependent manner. PROTAC BET Degrader-12 inhibits cell viability of KBM7 with a DC50 of 305.2 nM. (Pink: ligand for target protein (+)-JQ-1 (HY-13030); Black: linker (HY-159077); Blue: ligand for E3 ligase (HY-159076))
    PROTAC BET Degrader-12
  • HY-139682A
    Dovitinib-RIBOTAC TFA 2759351-69-2 98.35%
    Dovitinib RIBOTAC TFA is an RNA-targeting RIBOTAC degrader that can specifically bind to and degrade pre-miR-21. Dovitinib RIBOTAC TFA can inhibit the metastasis of breast cancer and has anti-tumor activity.
    Dovitinib-RIBOTAC TFA
  • HY-162706
    BSJ-5-63 2519823-37-9 99.97%
    BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer (Pink: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078)).
    BSJ-5-63
  • HY-112557
    PROTAC TBK1 degrader-2 2052306-13-3 98.20%
    PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM).
    PROTAC TBK1 degrader-2
  • HY-145703
    SHP2-D26 isomer-1 2740582-16-3 99.76%
    SHP2-D26 isomer-1 is an isoform of SHP2-D26 (HY-145162). SHP2-D26 is a PROTAC SHP2 degrader. (Pink: SHP2 ligand (HY-176797); Blue: Isomer control of VHL Ligand 14 (HY-150803); Black: linker).
    SHP2-D26 isomer-1
  • HY-148837
    GT19630 2883535-99-5 98.85%
    PROTAC c-Myc degrader-1 (Compound A153) is a multiple target protein degrader (PROTAC). PROTAC c-Myc degrader-1 effective degrades c-MYC, CK1α, GSPT1 and IKZF1/2/3 proteins in a variety of tumor cells. PROTAC c-Myc degrader-1 can be used for c-Myc high expression related disease research, such as cancer, cardiovascular and cerebrovascular diseases, and viral infection (Pink: c-Myc ligand (HY-168685); Blue: E3 ligase ligand (HY-W093472); Black: linker (HY-W015808)).
    GT19630
  • HY-131865
    SJF-1521 2230821-40-4 99.65%
    SJF-1521 is a selective EGFR PROTAC degrader. SJF-1521 is capable of inducing EGFR degradation in OVCAR8 cells. SJF-1521 can be used for tumor research. (Pink: EGFR ligand (HY-177379); Black: Linker (HY-128804); Blue: VHL Ligand (HY-125845)).
    SJF-1521
  • HY-115881
    SR-1114 2769141-82-2 99.04%
    SR-1114 is a PROTAC degrader targeting ENL. SR-1114 degrades ENL in a CRBN-dependent manner and selectively downregulates ENL target genes. SR-1114 can promote the differentiation of acute myeloid leukemia cells. SR-1114 can be used in tumor research. (Pink: ENL ligand (HY-145409); Black: Linker; Blue: E3 Ligand (HY-14658)).
    SR-1114
  • HY-114324
    PROTAC PARP1 degrader 2369022-68-2 99.74%
    PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. PROTAC PARP1 degrader induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader consists of E3 ubiquitinase ligand MDM2 ligand (HY-128836), blue part; target protein ligand PAPR1 ligand (HY-171543), pink part; PROTAC linker N3-PEG4-C2-NH2 (HY-128834), black part.
    PROTAC PARP1 degrader
  • HY-130614
    PROTAC EED degrader-1 2639882-72-5 98.27%
    PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.
    PROTAC EED degrader-1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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