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-184195
    PROTAC AR Degrader-13
    PROTAC AR Degrader-13 is a proteolysis-targeting chimera (PROTACs) that targets the androgen receptor (AR). PROTAC AR Degrader-13 has a DC50 of 0.90 nM in LNCaP cells and a DC50 of 0.23 nM in hDPC cells. PROTAC AR Degrader-13 induces AR degradation, downregulates TGF-β1 expression, upregulates β-catenin levels, and restores the Wnt/β-catenin pro-proliferation signaling in hair follicles. In a testosterone-induced androgenetic alopecia mouse model, PROTAC AR Degrader-13 accelerates hair regeneration rate, increases hair density and hair diameter. PROTAC AR Degrader-13 can be used for the research of androgenetic alopecia.
    PROTAC AR Degrader-13
  • HY-181134
    PROTAC HMGCR Degrader-2 2715104-46-2
    PROTAC HMGCR Degrader-2 is a HMGCR PROTAC degrader with an IC50 value of 0.25 μM. PROTAC degrades HMGCR-2 in Insig-silenced HepG2 cells with a DC50 of 0.12 μM. PROTAC HMGCR Degrader-2 takes PROTAC HMGCR Degrader-1 (HY-171823) as the oral prodrug. PROTAC HMGCR Degrader-2 degrades HMGCR by the VHL-dependent ubiquitin-proteasome system and reduces cellular cholesterol in HepG2 cells. PROTAC CDK2/4/6 Degrader-2 can be used for hyperlipidemia research.
    PROTAC HMGCR Degrader-2
  • HY-180957
    NEP108 3031840-31-7
    NEP108 is a GID4 E3 ligase-based BRD4 PROTAC degrader, with its DC50 value approximately 3.8 μM. NEP108 has a strong affinity for GID4, with a KD value of 0.22 μM, and the KD value of its trimeric complex is 2.85 μM. NEP108 can be used for cancer research.
    NEP108
  • HY-163876
    PROTAC SMARCA2/4-degrader-23 2568277-50-7
    SMARCA2 degrader-15 (compound I-409) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment.
    PROTAC SMARCA2/4-degrader-23
  • HY-184193
    M9101
    M9101 is a selective Aurora A PROTAC degrader with a DC50 of 2.3 nM. M9101 induces G2/M arrest in triple-negative breast cancer cells and potently inhibits the proliferation of multiple tumor cell lines. M9101 can be used in the research of various cancers including triple-negative breast cancer.
    M9101
  • HY-155393
    PROTAC BRD4 Degrader-22 3032850-37-3
    PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based BRD4 degrader, with a pDC50 (MOLT4, 24 h) of 9.2.
    PROTAC BRD4 Degrader-22
  • HY-159462
    PROTAC SMARCA2 degrader-10 2568279-34-3
    PROTAC SMARCA2 degrader-10 (compound I-507) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment.
    PROTAC SMARCA2 degrader-10
  • HY-173256
    Hyp-dBET1
    Hyp-dBET1 is a PROTAC degrader targeting BRD4. Hyp-dBET1 has an IC50 value of 3.4 μM in MDA-MB-231 cells. Hyp-dBET1 can be activated by hypoxia and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.
    Hyp-dBET1
  • HY-177729
    PROTAC BRD9 Degrader-9
    PROTAC BRD9 Degrader-9 (Compound 16) is an efficient and selective targeting BRD9 PROTAC degrader. PROTAC BRD9 Degrader-9 does not cause significant cytotoxicity. PROTAC BRD9 Degrader-9 can be used for cancer research
    PROTAC BRD9 Degrader-9
  • HY-158760
    PROTAC IRAK4 degrader-11 3033830-07-5
    PROTAC IRAK4 degrader-11 (compound 15) is PROTAC based on Cereblon ligand, and induces the degradation of IRAK4 with maximum degradation of 96.25% and the DC50 of 2.29 nM in HEK293 cells(Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker；Pink: IRAK4 inhibitor).
    PROTAC IRAK4 degrader-11
  • HY-162748
    PROTAC SMARCA2/4-degrader-30 2568276-44-6
    PROTAC SMARCA2/4-degrader-30 (Compound I-291) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-30 degrades SMARCA2 in A549 and in MV411 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM.
    PROTAC SMARCA2/4-degrader-30
  • HY-169367
    ERD-1233
    ERD-1233 is a potent and orally active estrogen receptor PROTAC degrader, with the DC50 of 0.9 nM. ERD-1233 plays an important role in ER+ breast cancer research (Pink: ligand for target protein (HY-201580); Black: linker (HY-W889109); Blue: E3 ligase ligand (HY-W1009348)).
    ERD-1233
  • HY-157805
    PROTAC SARS-CoV-2 Mpro degrader-2 3057294-32-0
    PROTAC SARS-CoV-2 Mpro degrader-2 (Compound 6) is a potent PROTAC degrader of SARS-CoV-2 Mpro. PROTAC SARS-CoV-2 Mpro degrader-2 has broad-spectrum antiviral activity against CoVs, including SARS-CoV-2 (EC50 = 10.8 μM), HCoV-OC43 (EC50 = 1.6 μM) and HCoV-229E (EC50 = 6.5 μM). PROTAC SARS-CoV-2 Mpro degrader-2 exhibits potent activity against SARS-CoV-2 in Calu-3 cells, with an EC50 of 0.89 μM.
    PROTAC SARS-CoV-2 Mpro degrader-2
  • HY-186110
    PROTAC LRRK2 Degrader-5 2839665-11-9
    PROTAC LRRK2 Degrader-5 Formula (V) is a LRRK2 PROTAC degrader. PROTAC LRRK2 Degrader-5 can be used for thet study of the diseases associated with LRRK2, such as Parkinson’s Disease (PD).
    PROTAC LRRK2 Degrader-5
  • HY-177730
    PROTAC BRD4 Degrader-40
    PROTAC BRD4 Degrader-40 is a Bromodomain protein 4 (BRD4) PROTAC degrader. PROTAC BRD4 Degrader-40 can induce BRD4 degradation in cancer cells. PROTAC BRD4 Degrader-40 can be used for the research of cancer, such as leukemia. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-163927))
    PROTAC BRD4 Degrader-40
  • HY-153938A
    PROTAC PTPN2 degrader-2 TFA 2912307-39-0
    PROTAC PTPN2 degrader-2 TFA is a potent PTPN2 PROTAC degrader with a DC50 of <50 nM. PROTAC PTPN2 degrader-2 TFA is potential for studying cancer or metabolic diseases, such as colon cancer.
    PROTAC PTPN2 degrader-2 TFA
  • HY-115718B
    PZ703b hydrochloride 99.18%
    PZ703b hydrochloride is a Bcl-xl PROTAC degrader that induces apoptosis and inhibits cancer cell proliferation. PZ703b hydrochloride can be used for the research of bladder cancer research.
    PZ703b hydrochloride
  • HY-179734
    PROTAC BRD4 Degrader-41
    PROTAC BRD4 Degrader-41 (Compound A5) is a BRD4 PROTAC degrader with a DC50 of 0.97 nM. PROTAC BRD4 Degrader-41 exhibits potent anti-proliferative activity against various types of cancer cells such as AML, lymphoma, breast cancer, ovarian cancer, and non-small cell lung cancer. PROTAC BRD4 Degrader-41 can induce G0/G1 phase arrest and apoptosis in MV4-11 cells. PROTAC BRD4 Degrader-41 downregulates the transcriptional level of c-Myc.
    PROTAC BRD4 Degrader-41
  • HY-180966
    Gly-PEG3-BA 3057939-66-6
    Gly-PEG3-BA is an EML4-ALK PROTAC degrader. Gly-PEG3-BA effectively reduces EML4-ALK with a DC50 value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC50 of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC50s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research.
    Gly-PEG3-BA
  • HY-177041
    PROTAC BRD4 Degrader-35 2503035-53-6
    PROTAC BRD4 Degrader-35 (Compound 17) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-35 can be studied in anticancer research. (Pink: BRD4 ligand (HY-78695); Black: linker; Blue: ligase).
    PROTAC BRD4 Degrader-35
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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