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-176134
    RP03707 3030493-05-8
    RP03707 is a PROTAC based KRASG12D degrader (Red: KRASG12D inhibitor (HY-134813), black: linker, Blue: E3 ligase ligand).
    RP03707
  • HY-173357
    TYD-68 99.54%
    TYD-68 is a highly efficient and selective CRBN-recruited TYK2 PROTAC degrader with a DC50 value of 0.42 nM. TYD-68 significantly inhibits IL-12 and IFN-α-induced STAT4 and STAT1 phosphorylation, thereby blocking TYK2-dependent signaling pathways. TYD-68 can be used in the study of psoriasis. (Pink: Target protein ligand (HY-173359); Black: Linker (HY-W007732B); Blue: E3 ligase ligand (HY-14658); E3 ligase ligand + Linker (HY-173358)).
    TYD-68
  • HY-158432
    GT-653 99.84%
    GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
    GT-653
  • HY-160924
    MS147 98.03%
    MS147 is a VHL-based PROTAC degrader of PRC1 (Polycomb Repressive Complex 1). The dissociation constants (Kd) of MS147 for EED (Embryonic Ectoderm Development) and VHL (Von Hippel-Lindau) are 3.0 μM and 450 nM, respectively. MS147 specifically binds to the EED protein through its EED-binding moiety; EED is a core component of PRC2 (Polycomb Repressive Complex 2) and interacts with the core components of PRC1, BMI1 (B-lymphoma Mo-MLV insertion region 1 homolog) and RING1B (Ring Finger Protein 1B). By this binding, MS147 is able to recruit BMI1 and RING1B near to VHL. Through the degradation of BMI1 and RING1B, MS147 reduces the level of H2AK119ub (histone H2A lysine 119 ubiquitination), affecting the proliferation of cancer cells. (Blue: VHL ligand (HY-125845), Black: linker ; Pink: PRC1 ligand (HY-158771)).
    MS147
  • HY-144304
    PROTAC EGFR degrader 2 3031336-58-7
    PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC.
    PROTAC EGFR degrader 2
  • HY-137342
    SB1-G-187 2769753-18-4 98.70%
    SB1-G-187 is a GNF-7-based multi-kinase PROTAC degrader that induces potent degradation of YES1, IRAK1, LYN, etc. SB1-G-187 mediates kinase degradation in a partially p97/VCP-dependent manner. SB1-G-187 can be utilized to develop new strategies for treating difficult diseases (Pink: multi-kinase ligand (HY-125142); Blue: CRBN ligand (HY-A0003)).
    SB1-G-187
  • HY-164995
    L1BC8 2417370-68-2 99.20%
    L1BC8 (compound 13a) is a BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments. (Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845); Black: linker (HY-171663)).
    L1BC8
  • HY-161989
    DZ-837
    DZ-837 (compound 3d) is a PROTAC targeting BCL6 with a DC50 of approximately 600 nM. DZ-837 can induce cell cycle arrest and exert synergistic anticancer effects with Ibrutinib (HY-10997). DZ-837 is composed of PROTAC target protein ligand BCL6 ligand-2 (HY-161990) (red part), E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), and PROTAC Linker (HY-W245803) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione (HY-W924949)[1].
    DZ-837
  • HY-148117
    MD13 2758431-97-7 99.96%
    MD13 is a macrophage migration inhibitory factor (MIF)-directed PROTAC with a Ki of 71 nM. MD13 can be used for cancer research.
    MD13
  • HY-173414
    PROTAC STING degrader-3 98.04%
    PROTAC STING degrader-3 (Compound ST9) is a STING PROTAC degrader (DC50: 0.62 μM). PROTAC STING degrader-3 induces STING degradation via the ubiquitin-proteasome pathway. PROTAC STING degrader-3 exerts anti-inflammatory effects by inhibiting STING/TBK1/NF-κB signaling. PROTAC STING degrader-3 has renal protective effects and can be used in the study of acute kidney injury (AKI) (Pink: STING ligand (HY-47709); Blue: E3 ligase CRBN ligand (HY-41547); Black: linker).
    PROTAC STING degrader-3
  • HY-149678
    PROTAC eDHFR Degrader-1 2849442-92-6 98.09%
    PROTAC eDHFR Degrader-1 is a PROTAC that is effective degradation of eDHFR-YFP, various POIs-including YFP and Luciferase.
    PROTAC eDHFR Degrader-1
  • HY-171767
    SK2188 3038446-94-2
    SK2188 is a highly efficient and selective PROTAC degrader targeting AURKA (DC50 = 3.9 nM). SK2188 induces DNA damage and cell apoptosis. SK2188 indirectly degrades MYCN, inhibits tumor cell proliferation, and provides insights into the study of MYCN-amplified neuroblastoma (Pink: AURKA ligand: MK-5108 (HY-13252); Blue: Thalidomide (HY-14658); Black: Linker: Amino-PEG4-alcohol (HY-W008005)).
    SK2188
  • HY-147858
    PROTAC EGFR degrader 7 99.99%
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research. PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC EGFR degrader 7
  • HY-155150
    JH-XII-03-02 2415900-86-4 99.41%
    JH-XII-03-02 is a potent and selective LRRK2 PROTAC degrader. JH-XII-03-02 can be used for parkinson's Disease (PD) research.
    JH-XII-03-02
  • HY-148739
    dBRD 9-A 2170679-42-0 99.50%
    dBRD 9-A is a PROTAC which can selective degrade BRD9. dBRD 9-A improves the bromine domain binding profile and reduces the binding activity of the whole BET family.
    dBRD 9-A
  • 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-159147
    SIA​​IS039 2570251-69-1 99.68%
    SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker).
    SIA​​IS039
  • HY-128840
    PROTAC MDM2 Degrader-1 2249944-98-5 98.11%
    PROTAC MDM2 Degrader-1 (Compound 15a) is a MDM2 PROTAC degrader. The structures of both Linker ends of PROTAC MDM2 Degrader-1 are MDM2 ligands. PROTAC MDM2 Degrader-1 can not only block the binding of p53-MDM2, but also degrade the target MDM2 protein by utilizing the function of the E3 ligase of MDM2 itself, thus exerting an anti-tumor effect. (Pink: MDM2 ligand 2 (HY-128836); Black: Linker (HY-128844); Blue: E3 ligase Ligand 15 (HY-128836))
    PROTAC MDM2 Degrader-1
  • HY-145264
    OARV-771 2683008-37-7 98.77%
    OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively.
    OARV-771
  • HY-112376
    MZP-54 2010159-47-2 98.03%
    MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 4 nM for Brd4BD2.
    MZP-54
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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