1. Signaling Pathways
  2. PROTAC
  3. PROTACs

PROTACs

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.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-170620
    PARP1 PROTAC 180055
    PARP1 PROTAC 180055 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787)).
    PARP1 PROTAC 180055
  • HY-161749
    PROTAC ALK degrader-1 3049802-45-8
    PROTAC ALK degrader-1 (compound B1) is an ALK degrader based on PROTACs, with the DC50 of 26 nM in H3122 EML4-ALK. PROTAC ALK degrader-1 can be used to synthesis PROTAC ALK degrader-2 (HY-161750) with superior bioavailability.
    PROTAC ALK degrader-1
  • HY-155684
    SA-PA
    SA-PA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues.
    SA-PA
  • HY-170343
    PROTAC SMARCA2 degrader-32 3033586-50-1
    PROTAC SMARCA2 degrader-32 (Compound 27) is the degrader for SMARCA2 with a DC50 of 1.3 nM. PROTAC SMARCA2 degrader-32 inhibits the proliferation of lung cancer cell NCI-H838 with a GI50 of 34 nM. (Pink: ligand for target protein SMARCA2 ligand-11 (HY-170349); Black: linker (HY-W895794); Blue: ligand for E3 ligase VHL (HY-170348))
    PROTAC SMARCA2 degrader-32
  • HY-170413
    PROTAC BTK Degrader-12 2736508-65-7
    PROTAC BTK Degrader-12 (EXAMPLE 19) is a PROTAC-based BTK degrader (Pink & black: BTK ligand & linker (HY-170414); Black: linker (HY-30105); Blue: CRBN ligand ( HY-W245311)).
    PROTAC BTK Degrader-12
  • HY-163709
    PROTAC FAK degrader 2
    PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))
    PROTAC FAK degrader 2
  • HY-154860
    PTD10 2642231-19-2
    PTD10 is a highly potent PROTAC BTK degrader (DC50: 0.5 nM, KD: 2.28 nM). PTD10 degrades BTK in Ramos and JeKo-1 cells with DC50s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation. (Pink: Btk ligand (HY-19834); Blue: E3 ligase ligand (HY-14658); Black: linker (HY-Y0966); E3 ligase ligand + linker (HY-131717)).
    PTD10
  • HY-152036
    SIAIS100 3033463-06-5
    SIAIS100 is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 can be used to research chronic myeloid leukemia (CML).
    SIAIS100
  • HY-148276
    KTX-497 2432993-46-7
    KTX-497 is an IRAK4 PROTAC degrader with a DC50 value of 3 nM. KTX-497 can be used for the research of oncology.(Pink:IRAK4 inhibitor (HY-150735); Black: linker; Blue: CRBN Ligand (HY-10984))
    KTX-497
  • HY-174975
    JY-21
    JY-21 is a BRD4 PROTAC degrader with a DC50 of 3.797 μM. JY-21 has a potent anticancer activity against MDA-MB-231 cells. Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-174994); Black: linker (HY-151862)
    JY-21
  • HY-161636
    PROTAC SOS1 degrader-9 3036155-21-9
    PROTAC SOS1 degrader-9 (Compd 10) is a PROTAC-based SOS1 degrader (Red: SOS1 Ligand (HY-161635), Black: linker (HY-W056267), Blue: E3 ligase ligand (HY-161639)).
    PROTAC SOS1 degrader-9
  • HY-157788
    ZX703
    ZX703 (compound 5I) is a PROTAC that significantly degrades GPX4 in a dose- and time-dependent manner through the ubiquitin-proteasome and autophagy-lysosome pathways (DC50=0.315 µM). ZX703 induces ferroptosis by inducing Reactive Oxygen Species (ROS) accumulation in cells. ZX703 can be used for cancer research.
    ZX703
  • HY-148275
    KTX-955 2573302-50-6
    KTX-955 is an antumor and effective IRAK4 degrader, with DC50 values of 5 nM and 130 nM for IRAK4 and Ikaros, respectively. KTX-955 is composed of CRBN ligand (blue part) Pomalidomide (HY-10984) and target protein ligand (red part) IRAK4-IN-20 (HY-150735).
    KTX-955
  • HY-170335
    PROTAC c-Met degrader-2 2254608-80-3
    PROTAC c-Met degrader-2 (PROTAC2) is a PROTAC-based c-Met degrader, with a DC50 of 50 nM (Pink: Foretinib (HY-10338); Black: linker (HY-45124); Blue: CRBN ligand Thalidomide-4-O-C2-NH2 (HY-136162A)).
    PROTAC c-Met degrader-2
  • HY-159570
    XD2-149 2710221-08-0
    XD2-149 is a PROTAC targeting STAT3. XD2-149 consists of PROTAC target protein ligand Napabucasin (HY-13919) (red part), E3 ligase Thalidomide (HY-14658) (black part), and linker NH2-C5-Azacyclohexane-N-Boc (HY-159572) (blue part). The E3 ligase + linker conjugate is Thalidomide-NH-C5-azacyclohexane-N-Boc (HY-159571), and the active control of the target protein ligand is Thalidomide acid (HY-159573)[1].
    XD2-149
  • HY-150797
    QA-68
    QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines. QA-68 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319).
    QA-68
  • HY-161597
    PROTAC DYRK2 degrader 1 3061366-76-2
    PROTAC DYRK2 degrader 1 (compound CP134) is a PROTAC degrader of DYRK2 (Red: DYRK2 inhibitor(HY-161598), black: linker (HY-42776), Blue: E3 ligase ligand (HY-10984)).
    PROTAC DYRK2 degrader 1
  • HY-160562
    PROTAC ERα Degrader-7 3025781-93-2
    PROTAC ERα Degrader-7 (compound i-320) is a potent estrogen receptor alpha(ERα) PROTAC degrader with a DC50 value of 0.000006 µM. PROTAC ERα Degrader-7 comprises a cereblon-binding moiety LBM linked to a ligand ERBM that binds ERα and comprises a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring.
    PROTAC ERα Degrader-7
  • HY-162245
    PROTAC SMARCA2 degrader-3 3024266-69-8
    PROTAC SMARCA2 degrader-3 is a PROTAC degrader of the SWI/SNF ATPase subunits, SMARCA2. PROTAC SMARCA2 degrader-3 has anticancer effects (WO2023244764A1; Compound 153).
    PROTAC SMARCA2 degrader-3
  • HY-175036
    YTHu78
    YTHu78 is a KDM5B PROTAC-type degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 exhibits significant antiproliferative activity against a variety of hematological cancer cell lines and can be used to study hematological cancers. (Pink: KDM5B ligand: (HY-116761); Blue: Thalidomide ligand: (HY-14658), Black + Pink: KDM5B ligand + linker: (HY-175145)).
    YTHu78
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