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-125877
    PROTAC Mcl1 degrader-1 2163793-38-0 98.13%
    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM.
    PROTAC Mcl1 degrader-1
  • HY-111433
    BRD4 degrader AT1 2098836-45-2 98.69%
    BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4BD2 in cells.
    BRD4 degrader AT1
  • HY-148771
    MTX-23 2488296-74-6 99.79%
    MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis.
    MTX-23
  • HY-123921
    Gefitinib-based PROTAC 3 2230821-27-7 99.98%
    Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.
    Gefitinib-based PROTAC 3
  • HY-150608
    PROTAC STING Degrader-1 2762552-74-7 98.26%
    PROTAC STING Degrader-1 is a PROTAC degrader targeting the STING pathway with a DC50 of 3.2 μM. PROTAC STING Degrader-1 exerts high anti-inflammatory efficacy. PROTAC STING Degrader-1 can be used to study diseases such as acute kidney injury and inflammatory bowel diseases (IBDs). (Pink: STING ligand (HY-138682); Blue: CRBN ligand (HY-10984); Black: linker (HY-W015883)).
    PROTAC STING Degrader-1
  • HY-114322
    VZ185 2306193-61-1 99.95%
    VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively.
    VZ185
  • HY-125876
    PROTAC Bcl2 degrader-1 2378801-85-3 99.80%
    PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker;Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
    PROTAC Bcl2 degrader-1
  • HY-141512
    JB170 2705844-82-0 98.97%
    JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.
    JB170
  • HY-134850
    QC-01–175 2267290-96-8 99.94%
    QC-01-175 is a heterobifunctional molecule, which degrades aberrant tau. QC-01-175 reduces the levels of A152T and P301L mutant tau protein and protects neurons from tau-mediated toxicity and improve cell survival (Pink: ligand for target protein Aberrant tau ligand 1 (HY-W453397); Black: linker NH2-PEG3 (HY-W007545); Blue: ligand for E3 ligase Pomalidomide (HY-10984)).
    QC-01–175
  • HY-151902
    SJ988497 2595365-41-4 99.03%
    SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL).
    SJ988497
  • HY-157839
    PROTAC α-Synuclein/Tau degrader 1 3032208-24-2 99.28%
    PROTAC α-Synuclein/Tau degrader 1 is a blood-brain barrier-penetrant dual PROTAC degrader of α-synuclein (α-Syn) and tau, with DC50 of 1.57 μM and 4.09 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 binds to α-Syn and tau PFF, with KDs of 0.47 and 2.78 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 exhibits degradation effect mediated by the ubiquitin-proteasome system (UPS). PROTAC α-Synuclein/Tau degrader 6 can be used for the study of Parkinson’s disease (PD) (Pink: α-Synuclein/Tau ligand (HY-151035); Blue: CRBN ligase ligand (HY-14658); Black: Linker (HY-128803)).
    PROTAC α-Synuclein/Tau degrader 1
  • HY-161176
    PROTAC KRAS G12D degrader 1 3033583-54-6 98.32%
    PROTAC KRAS G12D degrader 1 is a selective PROTAC KRASG12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRASG12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRASG12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893)).
    PROTAC KRAS G12D degrader 1
  • HY-128600
    ERD-308 2320561-35-9 98.13%
    ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC50 values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity. (Pink: Target Protein Ligand (HY-48027); Black: Linker (HY-172643); Blue: VHL Ligand (HY-112078); VHL Ligand+Linker:(HY-172645))
    ERD-308
  • HY-154984
    JET-209 3033714-58-5 98.07%
    JET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia (Pink: CBP/p300 ligand (HY-175620); Blue: CRBN ligand (HY-132248); Black: Linker; CBP/p300 ligand + Linker (HY-175621)).
    JET-209
  • HY-153188
    JNJ-1013 2597343-08-1 99.80%
    JNJ-1013 is a potent and selective IRAK1 PROTAC degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705) (Pink: ligand for target protein (HY-138834); black: linker (HY-Y1760); Blue: E3 ligase ligand (HY-112078)).
    JNJ-1013
  • HY-155994
    PIK5-12d 99.90%
    PIK5-12d is a PROTAC PIKfyve degrader (DC50 = 1.48 nM). PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d significantly suppresses tumor proliferation in mice bearing LTL-331R human prostate cancer PDX tumors. PIK5-12d can be used for the study of prostate cancer. (Pink: PIKfyve ligand (HY-175631), Blue: VHL Ligand (HY-125845), Black: Linker, PIKfyve ligand-linker conjugate (HY-175632)).
    PIK5-12d
  • HY-145514A
    dTAGV-1-NEG 2451573-87-6 99.73%
    dTAGV-1-NEG is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1 is an FKBP12F36V-selective degrader.
    dTAGV-1-NEG
  • HY-170451
    Seldegamadlin 2713618-08-5 98.53%
    Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC50 = 0.4 nM). Seldegamadlin inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927)).
    Seldegamadlin
  • HY-145696
    SJ10542 2789678-92-6 99.32%
    SJ10542 is a potent and selective JAK2/3 PROTAC degrader. In PDX cells lSJBALL020589, SJ10542 has DC50 values of 14 and 11 nM for JAK2 and JAK3, respectively. SJ10542 exhibits antitumor activity and can be used for the research of hematological malignancies and autoimmune diseases. (Pink: Target protein ligand (HY-47073); Black: Linker (HY-W251248); Blue: E3 ligase ligand (HY-W890189); E3 ligase ligand+Linker (HY-176425))
    SJ10542
  • HY-111518
    JH-XI-10-02 2209085-22-1 99.73%
    JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.
    JH-XI-10-02
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