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-169389
    OICR41114
    OICR41114 is a WDR5 PROTAC degrader with an EC50 of 40 nM. OICR41114 binds both DCAF1 and WDR5, and its binding affinity for DCAF1 is significantly enhanced in the presence of WDR5 (KD increases from 59 nM to 5 nM). OICR41114 exerts antiproliferative effects on MV4-11 cells. OICR41114 can be used for the research of acute myeloid leukemia.
    OICR41114
  • HY-173369
    PROTAC MAGL degrader-1
    PROTAC MAGL degrader-1 is an orally active PROTAC agent that simultaneously targets monoacylglycerol lipase (MAGL) and E3 ubiquitin ligase MDM2. PROTAC MAGL degrader-1 degrades MAGL and inhibits the binding of MDM2 to p53. PROTAC MAGL degrader-1 can partially penetrate the blood-brain barrier (BBB). PROTAC MAGL degrader-1 induces glioblastoma stem cells (GSCs) apoptosis. (E3 ligase ligand: HY-128837; target protein ligand + linker: HY-173370; target protein inhibitor: HY-15249).
    PROTAC MAGL degrader-1
  • HY-162589
    Lw13
    Lw13 is a Hsp90-targeting PROTAC and achieves maximum degradation at a concentration of 0.05 μM in Siha cells. Lw13 induces cell apoptosis and exhibits potent anti-tumor activity both in vitro and in vivo(Sturcture Note:(Blue: Cereblon ligand (HY-A0003), Black: linker；Pink: Hsp90 inhibitor SNX-5422 (HY-10213)).
    Lw13
  • HY-181000
    PROTAC PLK1 Degrader-3 3074520-74-1
    PROTAC PLK1 Degrader-3 (Compound DD-1) is a PLK1 PROTAC degrader based on the N-deglycosylation pathway, with a Kd value of 2.2 μM. The cell penetration ability of PROTAC PLK1 Degrader-3 is limited and a higher concentration is required to achieve significant degradation effects. PROTAC PLK1 Degrader-3 can be used for research on non-small cell lung cancer.
    PROTAC PLK1 Degrader-3
  • HY-149495
    CP-07
    CP-07 is a potent and selective PROTACCDK9 degrader (DC50: 43 nM). CP-07 inhibits 22RV1 cell proliferation (IC50: 62 nM) and colony formation by down-regulating Mcl-1 and c-Myc. CP-07 inhibits 22RV1 xenograft tumor growth. CP-07 can be used for research of prostate cancer.
    CP-07
  • HY-174877
    PROTAC HDAC6 degrader 6 3068162-16-0
    PROTAC HDAC6 degrader 6 (Compound 12) is a selective HDAC6-targeting photochemically targeting chimeras (PHOTACs) (subset of PROTAC) degrader with a ∼50% Dmax only upon activation to its cis-state with 390 nm light irradiation. Pink: HDAC6 ligand; Blue: CRBN ligase ligand (HY-A0003); Black: linker
    PROTAC HDAC6 degrader 6
  • HY-158036
    PROTAC STING Degrader-2 3023095-61-3
    PROTAC STING Degrader-2 is a STING PROTAC degrader with a DC50 of 0.53 μM. PROTAC STING Degrader-2 reduces the phosphorylation levels of TBK1 and IRF3. PROTAC STING Degrader-2 decreases the mRNA expression levels of IFN-β, CXCL10 and TNF-α, and blocks luciferase secretion. PROTAC STING Degrader-2 can be used in the research of autoimmune diseases.
    PROTAC STING Degrader-2
  • HY-185230
    HC278 3096503-40-8
    HC278 is a selective TEAD1/TEAD3 PROTAC degrader. HC278 induces proteasome-dependent degradation by forming a stable ternary complex with CRBN/DDB1. HC278 is applicable to the research of mesothelioma.
    HC278
  • HY-170978
    PROTAC CDK9 degrader-11 3039540-19-4
    PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models.(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
    PROTAC CDK9 degrader-11
  • HY-181052
    PROTAC NTRK1 degrader-1 2922274-35-7
    PROTAC NTRK1 degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). PROTAC NTRK1 degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1. PROTAC NTRK1 degrader-1 can be used for the research of solid tumors.
    PROTAC NTRK1 degrader-1
  • HY-161368
    BRD-SF2 3050690-26-8
    BRD-SF2 is a BRD4-targeted PROTAC degrader (DC50: 17.2 μM) (Blue: VHL ligand, black: linker, pink: BRD4 ligand).
    BRD-SF2
  • HY-147373
    DA-PROTAC 2488660-12-2
    DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research.
    DA-PROTAC
  • HY-170852
    QZ2135
    QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854).
    QZ2135
  • HY-132997
    PROTAC Bcl-xL degrader-3 2471970-60-0
    PROTAC Bcl-xL degrader-3 is a potent PROTAC Bcl-xL degrader. PROTAC Bcl-xL degrader-3 forms ternary complexes with the VHL-complex and BCL-XL. PROTAC Bcl-xL degrader-3 can be used in research on acute lymphoblastic leukemia.
    PROTAC Bcl-xL degrader-3
  • HY-170347
    PROTAC SMARCA2/4 degrader-36 3033588-00-7
    PROTAC SMARCA2/4 degrader-36 (Compound 29) is an effective dual degrader of SMARCA2/4,with DC50 values of 0.22 nM and 0.85 nM for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2/4 degrader-36 has anti-cell proliferation activity (Pink: Target Protein Ligand (HY-170354); Black: Linker (HY-W895794); Blue: E3 Ligase Ligand (HY-170353); E3 Ligase Ligand-Linker Conjugate (HY-170356)).
    PROTAC SMARCA2/4 degrader-36
  • HY-169276
    PROTAC SMARCA2 degrader-25 2770571-17-8
    PROTAC SMARCA2 degrader-25 (example 86) is a potent PROTAC SMARCA2 degrader with the DC50 of ＜0.01 μM (Pink: ligand for target protein (HY-169487); Black: linker (HY-W052601); Blue: E3 ligase ligand (HY-W087383)).
    PROTAC SMARCA2 degrader-25
  • HY-168586
    PROTAC IRAK4 degrader-12 2919995-09-6
    PROTAC IRAK4 degrader-12 is a PROTAC based on Cereblon ligand, inducing a maximum degradation rate of IRAK4 of 108.46% in K562 cells with an IC50 value of 4.87 nM ( Structure Note: Pink, IRAK4 inhibitor (HY-168611); Blue, E3 (HY-W733885); Black, linker (HY-168613)).
    PROTAC IRAK4 degrader-12
  • HY-164924
    ERD-12310A
    ERD-12310A is a PROTAC targeting Estrogen Receptor α (ERα) with a ED50 value of 47 pM. ERD-12310A has oral activity. ERD-12310A is composed of PROTAC target protein ligand ER ligand-4 (HY-164925) (red part), E3 ligase ligand (S)-Deoxy-thalidomide (HY-168055) (blue part). ERD-12310A can be used in the research of ER+ breast cancer.
    ERD-12310A
  • HY-177759
    PROTAC HDAC6 degrader 9
    PROTAC HDAC6 degrader 9 is a selective HDAC6 PROTAC degrader. PROTAC HDAC6 degrader 9 can be used for the research cancers related to HDAC6 abnormalities, such as multiple myeloma.
    PROTAC HDAC6 degrader 9
  • HY-181758
    PROTAC CBP/p300/BRD4 Degrader-1 3109024-12-3
    PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer.
    PROTAC CBP/p300/BRD4 Degrader-1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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