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-136250
    BSJ-03-204 2349356-09-6 99.76%
    BSJ-03-204 is a PROTAC linking a Cereblon ligand to a CDK ligand, serving as a potent and selective dual degrader of CDK4/6. BSJ-03-204 exhibits IC50 values of 26.9 nM and 10.4 nM against CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 can be utilized for cancer-related research.
    BSJ-03-204
  • HY-151623
    ACBI2 2913161-19-8 99.38%
    ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer.
    ACBI2
  • HY-111519
    dTRIM24 2170695-14-2 99.89%
    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.
    dTRIM24
  • HY-141796
    MS67 2407452-77-9 99.12%
    MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.
    MS67
  • HY-158113
    CBPD-409 3037549-86-0 99.38%
    CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker).
    CBPD-409
  • HY-P5819
    xStAx-VHLL 99.95%
    xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity.
    xStAx-VHLL
  • HY-139156
    SK-575 2523016-96-6 99.86%
    SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations.
    SK-575
  • HY-122826
    ZXH-3-26 2243076-67-5 99.53%
    ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.
    ZXH-3-26
  • HY-145925B
    CFT8634 2704617-96-7 98.10%
    CFT8634 is an orally bioavailable PROTAC BRD9 targeted degrader based on the E3 ubiquitin ligase CRBN mechanism. CFT8634 can be used for the study of synovial sarcoma and SMARCB1-deficient solid tumors (Pink: BRD9 ligand (HY-169988); Blue: E3 ligase ligand (HY-169989); Black: linker (HY-169991). CFT8634 is a heterobifunctional molecule that binds to BRD9 at one end and recruits CRBN at the other end, which can inhibit the growth of tumor cells that depend on BRD9. CFT8634 can be used for the study of SMARCB1-related cancers (such as synovial sarcoma and malignant rhabdoid tumor).
    CFT8634
  • HY-162723
    FOSL1 degrader 1 99.66%
    FOSL1 degrader 1 is a FOSL1 PROTAC degrader with a DC50 of 2.3 μM. FOSL1 degrader 1 induces proteasomal degradation of FOSL1. FOSL1 degrader 1 eliminates cancer stem cells in head and neck squamous cell carcinoma. FOSL1 degrader 1 suppresses head and neck squamous cell carcinoma tumorigenesis. FOSL1 degrader 1 can be used for the research of head and neck squamous cell carcinoma.
    FOSL1 degrader 1
  • HY-160141
    Catadegbrutinib 2736508-60-2 99.18%
    BGB-16673 (BGB-16673) is an orally active, selective BTK PROTAC degrader (IC50=0.69 nM). BGB-16673 ligates BTK to E3 ubiquitin ligase, causing BTK to undergo polyubiquitination, which is then recognized and degraded by the proteasome, thereby exerting efficient BTK degradation activity. BGB-16673 can be used in the research of B-cell malignancies such as chronic lymphocytic leukemia, small lymphocytic lymphoma, and mantle cell lymphoma.
    Catadegbrutinib
  • 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).
    Seldegamadlin
  • HY-155008
    PROTAC HK2 Degrader-1 3033812-84-6 99.76%
    PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research.
    PROTAC HK2 Degrader-1
  • HY-145765
    JQAD1 2417097-18-6 98.24%
    JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.
    JQAD1
  • HY-132296
    GSK215 2743427-26-9 99.26%
    GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
    GSK215
  • HY-148030
    XL01126 3011029-58-3 98.90%
    XL01126 is a potent LRRK2 PROTAC (DC50: 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2)). XL01126 crosses the blood-brain barrier and is used as a degradation probe in Parkinson's disease research. XL01126 can be used to study the non-catalytic and framework functions of LRRK2.
    XL01126
  • HY-162307
    Nrf2 degrader 1 3025286-00-1 99.12%
    Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with a DC50 of 0.1-1 μM in huH1 cells. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively. Nrf2 degrader 1 can be used for the study of liver cancer, non-small cell lung cancer (NSCLC) and squamous cell carcinoma of lung cancer.
    Nrf2 degrader 1
  • 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-130492
    ARCC-4 1973403-00-7 99.88%
    ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
    ARCC-4
  • HY-172736
    BMS-986458 3005272-36-3 99.65%
    BMS-986458 is a highly selective, orally active cereblon-based BCL6 PROTAC degrader and antitumor agent. BMS-986458 selectively degrades BCL6 by binding cereblon to the BTB domain of BCL6, thereby regulating the cell cycle, antiproliferative and interferon signaling pathways, and upregulating the expression and distribution of CD20. BMS-986458 modulates the phenotype of follicular helper T cells and reduces circulating tumor DNA levels. The combination of BMS-986458 with CD20xCD3 bispecific antibody also enhances the efficiency of T cell tumor infiltration and expansion. BMS-986458 induces regression of BCL6-positive tumors and prolongs survival, and it is suitable for research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma.
    BMS-986458
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