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-162106
    PROTAC GPX4 degrader-2 3035509-76-0
    PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 48h value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect.
    PROTAC GPX4 degrader-2
  • HY-159456
    PROTAC SMARCA2/4-degrader-5 2568277-84-7
    PROTAC SMARCA2/4-degrader-5 (Compound I-437) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 of 100-500 nM.
    PROTAC SMARCA2/4-degrader-5
  • HY-139996
    Pomalidomide-C5-Dovitinib 2732969-67-2
    Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD+ acute myeloid leukemia.
    Pomalidomide-C5-Dovitinib
  • HY-181354
    PROTAC EZH2 Degrader-36 2653338-72-6
    PROTAC EZH2 Degrader-36 (compound 15) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 16.00 nM.PROTAC EZH2 Degrader-36 applicable to lymphoma-related research.
    PROTAC EZH2 Degrader-36
  • HY-162815
    PROTAC SMARCA2/4-degrader-26
    PROTAC SMARCA2/4-degrader-26 (compound 6) is a PROTAC targeting SMARCA2/4. SMARCA2 and SMARCA4 are genes and cancer targets with complementary functions that catalyze nucleosome movement. PROTAC SMARCA2/4-degrader-25 is composed of PROTAC target protein ligand 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid (HY-46618) (red part), E3 ligase ligand (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (HY-W998248) (blue part), PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid (HY-59140) (black part), and the conjugate composed of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC (HY-125845)[1].
    PROTAC SMARCA2/4-degrader-26
  • HY-169327
    MD-265 2415160-21-1 99.31%
    MD-265 is a PROTAC degrader that can break down MDM2, leading to activation of p53 in cancer cells carrying wild-type p53. MD-265 achieves complete tumor regression and improves long-term survival of mice with leukemia.
    MD-265
  • HY-178516
    PROTAC CDK4/6/9 degrader 2
    PROTAC CDK4/6/9 degrader 2 (Compound P4) is a CDK4/6/9 PROTAC prodrug with oral activity and low toxicity. PROTAC CDK4/6/9 degrader 2 can significantly inhibit tumor growth and suppress tumor lung metastasis. PROTAC CDK4/6/9 degrader 2 can be used in the research of cancer such as breast cancer. (Pink: CDK4/6/9 Ligand (HY-168440); Blue: CRBN Ligand (HY-178517); Black: Linker (HY-178512))
    PROTAC CDK4/6/9 degrader 2
  • HY-170601
    PROTAC JNK1 Degrader-1
    PROTAC JNK1 Degrader-1 is a JNK1 PROTAC degrader with a DC50 of 10 nM. PROTAC JNK1 Degrader-1 reduces the level of fibronectin. PROTAC JNK1 Degrader-1 can be used for the research of pulmonary fibrosis.
    PROTAC JNK1 Degrader-1
  • HY-181834
    PROTAC MLLT1 Degrader-1 3111054-37-3
    PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML).
    PROTAC MLLT1 Degrader-1
  • HY-155398
    PRO-HD3 3126555-94-7
    PRO-HD3 is a cell-specific, PROTAC-based HDAC6 degrader.
    PRO-HD3
  • HY-161710
    XYD129
    XYD129 is an effective CBP/p300 PROTAC degrader. XYD129 has antiproliferative activity on MV4-11 cell line (IC 50=0.044 μM). XYD129 can be used for the study of acute myeloid leukemia (AML). (Structure Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)).
    XYD129
  • HY-171958
    PROTAC EGFR degrader 12 2654821-05-1
    PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM.
    PROTAC EGFR degrader 12
  • HY-180923
    AB3145
    AB3145 is a selective Brd4 BromoTag PROTAC degrader (DC50: 120-140 pM). AB3145 promotes the ubiquitination and degradation of Brd4. AB3145 can be used in cancer research.
    AB3145
  • HY-174233
    PROTAC SARS-CoV-2 Mpro degrader-4
    PROTAC SARS-CoV-2 Mpro degrader-4 (Compound LLP019) is a SARS-CoV-2 MPro PROTAC degrader with a DC50 value of 4.7 μM. PROTAC SARS-CoV-2 Mpro degrader-4 induces MPro ubiquitination and proteasomal degradation to inhibit SARS-CoV-2 replication. PROTAC SARS-CoV-2 Mpro degrader-4 is promising for research of COVID-19 and related coronavirus infections. (Pink: DH03 (HY-32717); Black: linker (HY-42149); Blue: Thalidomide-4-O-CH2-COO(t-Bu) (HY-42771).
    PROTAC SARS-CoV-2 Mpro degrader-4
  • HY-153023
    PROTAC STAT3 degrader-2 2429877-78-9
    PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC50 of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research. PROTAC STAT3 degrader-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC STAT3 degrader-2
  • HY-163609
    PROTAC AKR1C3 degrader-1
    PROTAC AKR1C3 degrader-1 (compound 5) is a potent AKR1C3 PROTAC degrader. PROTAC AKR1C3 degrader-1 decreases the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTAC AKR1C3 degrader-1 has the potential for the research of prostate cancer. (Blue:ubiquitin E3 ligase cereblon ligand (HY-A0003), Black: linker (HY-163647); Pink: AKR1C3 inhibitor (HY-163610)).
    PROTAC AKR1C3 degrader-1
  • HY-181231
    PROTAC CDK9 degrader-12 3052648-82-2
    PROTAC CDK9 degrader-12 is a selective CDK9 PROTAC degrader with a DC50 of 23 nM. PROTAC CDK9 degrader-12 induces proteasome-dependent degradation of CDK9, blocks CDK9-mediated HIV-1 transcriptional elongation, and reduces HIV-1 RNA synthesis. PROTAC CDK9 degrader-12 is applicable to research related to HIV-1 infection.
    PROTAC CDK9 degrader-12
  • HY-168725
    PROTAC KSP degrader 1 3099825-86-9
    PROTAC KSP degrader 1 (Compound 21) is a PROTAC Degrader for kinesin spindle protein (KSP), that degrades KSP in HCT-116 with DC50 of 114.8 nM. PROTAC KSP degrader 1 inhibits the proliferation of HCT-116 with IC50 of 10 nM, arrests the cell cycle of HCT-116 at G2/M phase, and induces apoptosis in HCT-116. PROTAC KSP degrader 1 exhibits antitumor efficacy in mouse model.
    PROTAC KSP degrader 1
  • HY-172934
    FGT-4
    FGT-4 is a folate receptor β (FR-β) targeting chimeric molecule. FGT-4 is a TLR7 agonist. FGT-4 facilitates the secretion of iNOS and proinflammatory cytokine IL-6 associated with M1 macrophages and enhances the proliferation of cytotoxic CD8+ T cells. FGT-4 has anti-tumor activity in the 4T1 breast cancer mouse model. FGT-4 can be used for the study of cancer immunity. (Pink: target protein TLR7/8 agonist 1 ligand (HY-103698); black: linker (HY-172936); blue: FR-β ligand (HY-172935)).
    FGT-4
  • HY-169378
    CSI86
    CSI86 is a MYC-targeting PROTAC degrader with antiproliferative activity (IC50: 13-18 μM).
    CSI86
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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