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-132857
    ZXH-4-130 2711006-66-3 99.70%
    ZXH-4-130 is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC).
    ZXH-4-130
  • HY-172946
    SD-2301 3054116-24-1
    SD-2301 is a selective STAT3 PROTAC degrader. SD-2301 induces STAT3 degradation without affecting the protein levels of other STAT family members (STAT1, STAT2, STAT4, STAT5, STAT6). SD-2301 exerts anti-tumor effects in B16F10-bearing mice. SD-2301 can be used for the study of cancer. (Pink: STAT3 ligand (HY-172947), Blue: VHL Ligand (HY-172948), Black: Linker (HY-W577012), VHL ligand-linker conjugate (HY-172949)).
    SD-2301
  • HY-147100
    α1A-AR Degrader 9c 2863635-02-1
    α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research.
    α1A-AR Degrader 9c
  • HY-183013
    PROTAC PARP2 degrader-1 2925182-32-5
    PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer.
    PROTAC PARP2 degrader-1
  • HY-163938
    PROTAC erf3a Degrader-1 3033871-19-8 99.44%
    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-174866
    BT-O2C 3055107-34-8
    BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer. (Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869)).
    BT-O2C
  • HY-149616
    PPM-3 3032388-42-1 98.2%
    PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages.
    PPM-3
  • HY-107425A
    cis-MZ 1 1797406-72-4 99.8%
    cis-MZ 1 is a cis isomer of meso-zeaxanthin, a xanthophyll carotenoid component of total zeaxanthin measured in serum and egg yolks.cis-MZ 1 is a triphenyltin benzoate that adopts either a tetrahedral monomeric structure (I) or a trans-SnR3O2 polymeric structure (III), with structure determined by a balance of steric and electronic factors.
    cis-MZ 1
  • HY-146393
    PROTAC CYP1B1 degrader-1 2411389-67-6 98.09%
    PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer.
    PROTAC CYP1B1 degrader-1
  • HY-148066
    DB0662 2769753-51-5 99.66%
    DB0662 is a multi-target kinase-directed PROTAC degrader, targeting kinases including PTK2B, MAPK9, BLK, CSK, LIMK1, etc.
    DB0662
  • HY-171769
    dAurAB2 3115765-38-0
    dAurAB2 is a dual-degrading PROTAC that potently degrades Aurora-A and Aurora-B with DC50s of 59 nM and 39 nM, respectively. dAurAB2 reduces N-Myc levels in MYCN-amplified IMR32 neuroblastoma cells. dAurAB2 can be used for the study of neuroblastoma. (Pink, Aurora ligand (HY-10804); Blue, E3 ligand: (HY-103597); Black, linker (HY-W105740)).
    dAurAB2
  • HY-162702
    AZ'3137 2960179-55-7 99.90%
    AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC50 value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC50 of 92 nM). AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice.
    AZ'3137
  • HY-P10446
    TAT-PiET-PROTAC 3036046-04-2 98.04%
    TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer.
    TAT-PiET-PROTAC
  • HY-175652
    AZD9750 3056515-10-4 98.15%
    AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant ARL702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research.
    AZD9750
  • HY-147174
    PROTAC_ERRα 1801547-15-8 99.71%
    PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker.
    PROTAC_ERRα
  • HY-165298
    DGY-09-192 2504949-52-2 99.50%
    DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM). DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN). DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers.
    DGY-09-192
  • HY-162537
    LYP-8 2484876-99-3 99.89%
    LYP-8 is a potent and effective NAMPT degrader with maximum degradation of 97% at 0.5 μM in SKOV-3 cells. LYP-8 shows anti-cancer activity in vivo and in vitro.
    LYP-8
  • HY-171334
    (Rac)-P1D-34 2957895-04-2 99.45%
    PROTAC PIN1 degrader-2 (1) is a PROTAC-based PIN1 degrader (Pink: PIN1 ligand HY-171442, Blue: cereblon ligand Thalidomide (HY-14658), Black: linker HY-W014883). PROTAC PIN1 degrader-2 (1) possesses anti-cancer activity, with IC50 values of 2248 nM (MV-4-11 cells), 3984 nM (MOLM-13), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60) and 3925 nM (HL-60) respectively.
    (Rac)-P1D-34
  • HY-168669
    PROTAC K-Ras Degrader-5 3052745-16-8
    PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC50 of <100 nM for KRASG12D. PROTAC K-Ras Degrader-5 recruits KRASG12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses pERK levels downstream of KRASG12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer.
    PROTAC K-Ras Degrader-5
  • HY-147858A
    PROTAC EGFR degrader 7 diTFA
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13.2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46.82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research.
    PROTAC EGFR degrader 7 diTFA
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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