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-157765
    PROTAC ERα Degrader-6 3065420-66-5
    PROTAC ERα Degrader-6 (compound A2) is a potent PROTAC degrader of ERα, with IC50 of 0.11 μM in MCE-7 cells. PROTAC ERα Degrader-6 has anti-tumor effect. PROTAC ERα Degrader-6 is a fluorescent probes with Em of 582 nm that enable real-time visualization of ERα protein degradation.
    PROTAC ERα Degrader-6
  • HY-155356
    YN14 99.08%
    YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
    YN14
  • HY-186067
    PROTAC BCL6 Degrader-3 3005272-58-9 99.76%
    PROTAC BCL6 Degrader-3 (compound 92) is a BCL6 PROTAC degrader. PROTAC BCL6 Degrader-3 can be used for the study of cancer or an autoimmune disease.
    PROTAC BCL6 Degrader-3
  • HY-159098
    dWIZ-1
    dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease.
    dWIZ-1
  • HY-164807
    SARD279 1489236-55-6
    SARD279 is a potent and selective Androgen Receptor degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research.(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))
    SARD279
  • HY-180132
    PROTAC AURKA degrader 2 3093582-13-6 98.36%
    PROTAC AURKA degrader 2 (compound D) is a potent and selective PROTAC AURKA degrader with an IC50 of 3.58 nM. PROTAC AURKA degrader 2 exhibits 21.6-fold selectivity for AURKA over AURKB (IC50 = 77.2 nM). PROTAC AURKA degrader 2 specifically depletes AURKA on the mitotic spindle.
    PROTAC AURKA degrader 2
  • HY-176792
    ACBI-4 3097985-19-5 98.01%
    ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader, with Kd values of 141 nM against KRASG12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer.
    ACBI-4
  • HY-156774
    CCW 28-3 2361142-23-4 99.38%
    CCW 28-3 is a PROTAC-based BRD4 degrader in a proteasome- and RNF4-dependent manner.
    CCW 28-3
  • HY-177008
    PROTAC HER2 degrader-1 2897640-93-4 98.0%
    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-145737A
    PROTAC SOS1 degrader-1 TFA 98.38%
    PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity.
    PROTAC SOS1 degrader-1 TFA
  • HY-172590
    LZ-07 98.27%
    LZ-07 is a IRAK4 PROTAC degrader (DC50 = 1.14 nM). LZ-07 leads to marked suppression of cytokines including IL-6, IL-1β, TNF-α, and IL-10 upon degradation of IRAK4. LZ-07 can be studied in research for autoimmune diseases (Pink: IRAK4 ligand (HY-172591); Blue: CRBN ligand (HY-34590); Black: linker (HY-B0149); CRBN ligand + linker: HY-172593).
    LZ-07
  • HY-143344
    NJH-2-056 2858812-69-6 98.31%
    NJH-2-056 is a deubiquitinase-targeting chimera (DUBTAC) linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor. NJH-2-056 can be used for cystic fibrosis research.
    NJH-2-056
  • HY-176919
    PROTAC STAT6 degrader-3 3077385-98-6 98.66%
    PROTAC STAT6 degrader-3 is a potent STAT6 PROTAC degrader with a DC50 of less than 1 nM. PROTAC STAT6 degrader-3 can be used for research on allergic/inflammatory diseases and cancer.
    PROTAC STAT6 degrader-3
  • HY-153864
    PROTAC MEK1 Degrader-1 2671004-41-2 98.28%
    PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells.
    PROTAC MEK1 Degrader-1
  • HY-162014
    WDR5 degrader-1 3032434-45-7 98.00%
    WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1.
    WDR5 degrader-1
  • HY-160502
    CST967 3093667-09-2 98.31%
    CST967 (Compound 17) is a USP7 PROTAC degrader, and increasing the PROTAC concentration can enhance the degradation rate of USP7. CST967 can be used in cancer research.
    CST967
  • HY-148063
    DB0614 2769753-47-9
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
  • HY-153572A
    Homo-BacPROTAC7 TFA
    Homo-BacPROTAC7 TFA is a PROTAC protein degrader targeting ClpC1/ClpC2 with a Kd of 0.5-2.5 nM for both targets. Homo-BacPROTAC7 (TFA) acts as a bactericidal agent, induces killing of pathogenic mycobacteria, retains activity against dormant-like mycobacterial cells with reduced intracellular ATP levels, and shows elevated antibiotic potency relative to its parent monomer. Homo-BacPROTAC7 (TFA) can be used for the research of tuberculosis.
    Homo-BacPROTAC7 TFA
  • HY-138634
    GNE-987 GSH linker-2 99.48%
    GNE-987 GSH linker-2 is a drug-linker conjugates for ADC. GNE-987 GSH linker-2 is a conjugation of PROTAC GNE-987 (HY-129937A) and ADC linker GSH linker-2 (HY-182740), and can be used to prepare antibody-drug conjugates (ADC) for BRD4 degradation. GNE-987 GSH linker-2 can be used for the research of cancer.
    GNE-987 GSH linker-2
  • HY-138635
    PROTAC BRD4 Degrader linker conjugate-3 2417370-90-0 98.54%
    PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-12 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.39 nM and 0.24 nM, respectively.
    PROTAC BRD4 Degrader linker conjugate-3
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