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PROTAC CRBN Degrader 1

" in MedChemExpress (MCE) Product Catalog:

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Art. -Nr. Produktname Target Forschungsgebiete Chemical Structure
  • HY-155008
    PROTAC HK2 Degrader-1
    2 Publications Verification

    PROTACs Hexokinase Cancer
    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-41547

    Cereblon ligand 4; E3 ligase Ligand 4

    Ligands for E3 Ligase Autophagy Apoptosis Cancer
    Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966) .
    Thalidomide 4-fluoride
  • HY-128845

    PROTACs E1/E2/E3 Enzyme Cancer
    PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other .
    PROTAC CRBN Degrader-1
  • HY-139186

    PROTACs Ras Cancer
    PROTAC KRAS G12C degrader-1 is a Cereblon-based KRAS G12C PROTAC degrader. PROTAC KRAS G12C degrader-1 induces CRBN/ KRAS G12C dimerization and degrades GFP- KRAS G12C in reporter cells .
    PROTAC KRAS G12C degrader-1
  • HY-163757

    PROTACs PD-1/PD-L1 Inflammation/Immunology Cancer
    PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745)) .
    PROTAC PD-L1 degrader-1
  • HY-157839

    PROTACs α-synuclein Tau Protein Neurological Disease
    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-114407

    PROTACs Epigenetic Reader Domain Cancer
    TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .
    TD-428
  • HY-150608
    PROTAC STING Degrader-1
    1 Publications Verification

    PROTACs STING Inflammation/Immunology Cancer
    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-125876
    PROTAC Bcl2 degrader-1
    1 Publications Verification

    PROTACs Bcl-2 Family Cancer
    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-111594
    Homo-PROTAC cereblon degrader 1
    1 Publications Verification

    PROTACs Cancer
    Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3 .
    Homo-PROTAC cereblon degrader 1
  • HY-126534A
    Abemaciclib metabolite M18 hydrochloride
    2 Publications Verification

    LSN3106729 hydrochloride

    Ligands for Target Protein for PROTAC CDK Cancer
    Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
    Abemaciclib metabolite M18 hydrochloride
  • HY-158342

    PROTACs YAP Cancer
    PROTAC TEAD degrader-1 is a TEAD2 degrader and antiproliferative agent with selective activity toward TEAD2 relative to other TEAD family members. PROTAC TEAD degrader-1 relies on CRBN and the proteasome system for TEAD2 degradation; disruption of CRBN binding attenuates this activity. PROTAC TEAD degrader-1 decreases expression of YAP target genes CYR61 and CTGF. PROTAC TEAD degrader-1 can be used for the research of NF2-deficient cancer .
    PROTAC TEAD degrader-1
  • HY-176428

    P11-2

    PROTACs MNK Apoptosis Eukaryotic Initiation Factor (eIF) Cancer
    PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety . Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430
    PROTAC MNK1 degrader-1
  • HY-149845

    PROTACs GSK-3 Neurological Disease
    PROTAC GSK-3β Degrader-1 (compound 1) is a degrader targets GSK-3β degradation with an IC50 value of 833 nM. PROTAC GSK-3β Degrader-1 contains SB-216763 (a GSK-3β inhibitor), a PEG linker and a CRBN (E3 ligase liand). PROTAC GSK-3β Degrader-1 reduces the neurotoxicity induced by Aβ25-35 peptide and CuSO4. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease .
    PROTAC GSK-3β Degrader-1
  • HY-114406

    Ligands for E3 Ligase Cancer
    TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .
    TD-106
  • HY-126534
    Abemaciclib metabolite M18
    2 Publications Verification

    LSN3106729

    Ligands for Target Protein for PROTAC CDK Cancer
    Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
    Abemaciclib metabolite M18
  • HY-142662A

    PROTACs IRAK Others
    PROTAC IRAK3 degrader-1 formic is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 formic induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 formic can be used for cancer research .
    PROTAC IRAK3 degrade-1 formic
  • HY-177008

    PROTACs EGFR Apoptosis Akt ERK Cancer
    PROTAC HER2 degrader-1 is a highly selective HER2 PROTAC degrader, with a DC50 of 69 nM and a Dmax of 96%. PROTAC HER2 degrader-1 inhibits HER2-positive cell proliferation and tumor growth through persistent HER2 degradation and potent inhibition of downstream pathways (AKT and ERK). PROTAC HER2 degrader-1 induces apoptosis in BT-474 cells. PROTAC HER2 degrader-1 can be used for research of HER2-positive cancers. (Pink: HER2 ligand: (HY-177009); Black: Linker; Blue: CRBN ligand: (HY-W023573) .
    PROTAC HER2 degrader-1
  • HY-174461

    PROTACs PI3K Cancer
    PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885)) .
    PROTAC PI3Kα degrader-1
  • HY-130991

    Target Protein Ligand-Linker Conjugates Cancer
    K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
    K-Ras ligand-Linker Conjugate 6
  • HY-168135

    PROTACs c-Met/HGFR Cancer
    PROTAC c-Met degrader-1 is a selective and orally active c-Met PROTAC degrader with a DC50 of 6.21 nM against c-Met. PROTAC c-Met degrader-1 induces CRBN-dependent ubiquitination and proteasomal degradation of c-Met. PROTAC c-Met degrader-1 induces G0/G1 phase arrest in c-Met-dependent cancer cells. PROTAC c-Met degrader-1 kills c-Met-dependent cancer cells. PROTAC c-Met degrader-1 inhibits tumor growth in animal models. PROTAC c-Met degrader-1 can be used for the research of gastric cancer .
    PROTAC c-Met degrader-1
  • HY-179055

    PROTACs DAPK Neurological Disease
    PROTAC DAPK1 Degrader-1 (Compound CP1) is a DAPK1 PROTAC degrader with a DC50 of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increased the MDM2 protein level. PROTAC DAPK1 Degrader-1 significantly reduced the levels of cleaved caspase-3 and cleaved PARP in a cell apoptosis model induced by the neurotoxin ceramide, indicating that it effectively inhibits neuronal apoptosis by degrading DAPK1. PROTAC DAPK1 Degrader-1 can be used to study neurological diseases such as cerebral ischemia and traumatic brain injury (pink: DAPK1 ligand (HY-179071); blue: CRBN ligand (HY-10984); black: linker (HY-40171)) .
    PROTAC DAPK1 Degrader-1
  • HY-168593

    β-catenin PROTACs Wnt Histone Demethylase Cancer
    PROTAC KDM3 degrader-1 (Compound 4) is a CRBN-recruiting PROTAC designed based on the IOX1 (HY-12304) scaffold. PROTAC KDM3 degrader-1 selectively degrades the KDM3A and KDM3B proteins, thereby inhibiting the Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 significantly suppresses the self-renewal capacity of colorectal cancer stem cells and inhibits the growth of colorectal cancer tumors. PROTAC KDM3 degrader-1 is suitable for research on colorectal cancer (Target protein ligand (Pink): HY-12304; linker (Black): HY-22335; Conjugate of E3 ligase ligand and linker: HY-112599; E3 ligase (Blue): HY-41547) .
    PROTAC KDM3 degrader-1
  • HY-130713

    E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-C2-amido-C2-COOH contains a CRBN ligand and a linker for recruiting E3 ubiquitin ligases. Thalidomide-C2-amido-C2-COOH can be used to design and synthesize PROTAC CDK2/9 Degrader-1 (HY-130709). PROTAC CDK2/9 Degrader-1 is applicable to prostate cancer-related research .
    Thalidomide-C2-amido-C2-COOH
  • HY-150839

    Ligands for E3 Ligase Cancer
    E3 ligase Ligand PG is a E3 ligase ligand that can be used in the recruitment of CRBN protein. E3 ligase Ligand PG exhibits potent binding activity with CRBN (IC50 of 2.191 μM). E3 ligase Ligand PG can be connected to the BMS-202 (HY-19745) by a linker to form PROTAC, PROTAC PD-L1 degrader-1 (HY-163757) .
    E3 ligase Ligand PG
  • HY-142662

    PROTACs IRAK Cancer
    PROTAC IRAK3 degrader-1 is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 can be used for cancer research .
    PROTAC IRAK3 degrader-1
  • HY-158381

    PROTACs Phosphatase Metabolic Disease
    PROTAC PTP1B degrader 1 (compound 75) is a CRBN-based PTP1B PROTAC degrader, with DC50 values of 0.2 μM (48 h) and 0.05 μM (72 h) (Red: PTP1B ligand Oleanolic acid (HY-N0156); Black: linker; Blue: CRBN ligand) .
    PROTAC PTP1B degrader 1
  • HY-163938

    PROTACs Cancer
    PROTAC erf3a Degrader-1 (Compound C63) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-1 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-1 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: CRBN ligand (HY-41547)) .
    PROTAC erf3a Degrader-1
  • HY-178176

    PROTACs Cannabinoid Receptor Akt ERK Bcl-2 Family Apoptosis Cancer
    PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)) .
    PROTAC CB1R Degrader-1
  • HY-179112

    PROTACs IKK Nuclear Hormone Receptor 4A/NR4A Caspase Necroptosis Apoptosis Inflammation/Immunology Cancer
    PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577) .
    PROTAC IKKβ/NR4A1 degrader-1
  • HY-168274

    PROTACs Apoptosis Cancer
    PROTAC TRIB2 degrader-1 (Compound 5k) is an effective TRIB2 degrader that selectively induces TRIB2 degradation through the CRBN-dependent ubiquitin-proteasome pathway. PROTAC TRIB2 degrader-1 can inhibit cell proliferation and induce cell apoptosis, and can be used in cancer research. (Target protein ligand (Pink): HY-168275; linker (black): HY-168276; E3 Ligase Ligand-Linker Conjugates: HY-168277; E3 ligase (Blue): HY-W023573) .
    PROTAC TRIB2 degrader-1
  • HY-178858

    PROTACs FLT3 Checkpoint Kinase (Chk) STAT ERK c-Myc Akt Cancer
    PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)) .
    PROTAC FLT3/CHK1 Degrader-1
  • HY-175830

    PROTACs Aurora Kinase Cancer
    PROTAC AURKA degrader 1 (Compound A16 + X7) is a Aurora kinase A (AURKA) PROTAC degrader. PROTAC AURKA degrader 1 can be used for cancers research . Pink: AURKA ligand (HY-175827); Blue: CRBN ligase ligand (HY-W867704); Black: linker (HY-132208)
    PROTAC AURKA degrader 1
  • HY-178452

    PROTACs CDK Apoptosis Cancer
    PROTAC CDK4/6/9 degrader 1 is a CDK4/6/9 PROTAC degrader. PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6, and CDK9 in TNBC cells and inhibits TNBC cell proliferation. PROTAC CDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. PROTAC CDK4/6/9 degrader 1 can be used for the study of triple-negative breast cancer (TNBC). (Pink: CDK4/6/9 ligand (HY-168440), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-178512), E3 ligase ligand-linker conjugate (HY-178515)) .
    PROTAC CDK4/6/9 degrader 1
  • HY-163851

    PROTACs HIV Infection
    PROTAC Vif degrader-1 (Compound L15) is a Vif PROTAC degrader. PROTAC Vif degrader-1 has antiviral activity against HIV-1 (EC50: 33.35 μM against HIV-1IIIB). Blue: CRBN ligand (HY-10984); Black: linker; Pink: HIV-1 inhibitor(HY-163852) .
    PROTAC Vif degrader-1
  • HY-179077

    PROTACs Btk IKZF Family Cancer
    PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BTK/IKZF1/3 Degrader-1 exhibits antitumor activity. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma . (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179076); Blue: CRBN ligand (HY-41547))
    PROTAC BTK/IKZF1/3 Degrader-1
  • HY-174405

    PROTACs Phosphodiesterase (PDE) TNF Receptor Interleukin Related Inflammation/Immunology
    PROTAC PDE4 degrader-1 (Compound 9m) is a selective and orally active PDE4 PROTAC degrader with a DC50 of 41.98 μM. PROTAC PDE4 degrader-1 potently inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. PROTAC PDE4 degrader-1 significantly alleviates pulmonary inflammation in LPS (HY-D1056)-induced acute lung injury (ALI) mice Model . Pink: PDE4 ligand (HY-174410); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC PDE4 degrader-1
  • HY-179075

    PROTACs BCL6 IKZF Family Cancer
    PROTAC BCL6/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BCL6/IKZF1/3 Degrader-1 exhibits superior antiproliferative effects in various germinal center B-cell-like (GCB) and activated B-cell-like (ABC) diffuse large B-cell lymphoma (DLBCL) cell lines. PROTAC BCL6/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma . (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179064); Blue: CRBN ligand (HY-41547); Black: linker (HY-42427); CRBN ligand-Linker: (HY-179066))
    PROTAC BCL6/IKZF1/3 Degrader-1
  • HY-172368

    PROTACs Histone Methyltransferase IKZF Family Apoptosis Inflammation/Immunology Cancer
    PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reduces the methylation level of its substrate BAF155. PROTAC CARM1/IKZF3 degrader-1 is the PROTAC degrader for IKZF 1/3 through a CRBN-dependent pathway. PROTAC CARM1/IKZF3 degrader-1 inhibits the expression of MYC protein, thereby inhibiting the proliferation of a variety of multiple myeloma cells. PROTAC CARM1/IKZF3 degrader-1 induces apoptosis in cell H929. PROTAC CARM1/IKZF3 degrader-1 overcomes immunomodulatory drugs (IMiD, such as pomalidomide) resistance. PROTAC CARM1/IKZF3 degrader-1 can be used in cancer and immunology research . (Pink: ligand for target protein CARM1/IKZF3 ligand 1 (HY-172369); Active form of target protein ligand: EZM 2302 (HY-111109); Black: linker (HY-21999); Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride (HY-41547))
    PROTAC CARM1/IKZF3 degrader-1
  • HY-175610

    PROTACs FLT3 JAK Epigenetic Reader Domain Cancer
    PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .
    PROTAC FLT3/JAK2/BRD4 Degrader-1
  • HY-174410

    Ligands for Target Protein for PROTAC Inflammation/Immunology
    PDE4 ligand 2 is a CRBN E3 ligase ligand. PDE4 ligand 2 can be used to synthesize PROTAC such as PDE4 degrader-1 (HY-174405). PDE4 ligand 2 can be studied in research for autoimmune and anti-inflammatory diseases .
    PDE4 ligand 2
  • HY-170869

    PROTACs FGFR Cancer
    PROTAC FGFR1 degrader-1 (compound S2H) is a PROTAC degrader targeting FGFR1, with IC50=26.81 nM and DC50=39.78 nM in KG1a cells. PROTAC FGFR1 degrader-1 is composed of CRBN-type E3 ligase ligand (blue part) Pomalidomide (HY-10984), target protein ligand (red part) FGFR1 ligand-1 (HY-170871), and PROTAC linker (black part) 9-Bromononanoic acid (HY-W007587), in which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 164 (HY-170870) .
    PROTAC FGFR1 degrader-1
  • HY-129776

    Target Protein Ligand-Linker Conjugates Cancer
    K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
    K-Ras ligand-Linker Conjugate 2
  • HY-129775

    Target Protein Ligand-Linker Conjugates Cancer
    K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
    K-Ras ligand-Linker Conjugate 1
  • HY-178118

    PROTACs PDI Cancer
    PROTAC PDIA1 degrader 1 (Compound H4) is a PDIA1 PROTAC degrader with a DC50 of 29.71 μM. PROTAC PDIA1 degrader 1 has potent anticancer activity and significantly inhibits cancer cell proliferation . Pink: PDIA1 ligand (HY-100433); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W015088)
    PROTAC PDIA1 degrader 1
  • HY-178066

    Bcl-2 Family PROTACs Cancer
    PROTAC BCL-xL/BCL-w Degrader 1 (Compound 44) is a BCL-xL/BCL-w PROTAC degrader. PROTAC BCL-xL/BCL-w Degrader 1 has significant anticancer activity with reduced on-target platelet toxicity . Pink: BCL-xL/BCL-w ligand (HY-10087); Blue: CRBN ligase ligand (HY-163233); Black: linker (HY-Y1230)
    PROTAC BCL-xL/BCL-w Degrader 1
  • HY-162098

    PROTACs Microtubule/Tubulin Apoptosis Cancer
    PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
    PROTAC tubulin-Degrader-1
  • HY-178964

    PROTACs RET Cancer
    PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker) .
    PROTAC RET Degrader 1
  • HY-44148

    Target Protein Ligand-Linker Conjugates Cancer
    FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation .
    FAK ligand-Linker Conjugate 1
  • HY-126534S

    LSN3106729-d8

    CDK Ligands for Target Protein for PROTAC Cancer
    Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
    Abemaciclib metabolite M18-d8

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