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-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
    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. (Pink: MI-1063 (HY-133754); Black: linker; Blue: Lenalidomide (HY-A0003).
    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-targeted-1
    PROTAC JNK1-targeted-1 (PA2) is a JNK1 PROTAC degrader, with a DC50 of 10 nM. PROTAC JNK1-targeted-1 (PA2) decreases the level of Fibronectin protein. PROTAC JNK1-targeted-1 can be used for the research of pulmonary fibrosis. (Pink: JNK1 inhibitor (HY-170602); Black: linker (HY-40178); Blue: CRBN Ligand (HY-41547))
    PROTAC JNK1-targeted-1
  • HY-155398
    PRO-HD3
    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-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-168725
    PROTAC KSP-IN-1 3099825-86-9
    PROTAC KSP-IN-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-IN-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-IN-1 exhibits antitumor efficacy in mouse model. (Blue: Ligand for E3 Ligase Cereblon (HY-103596); Blank: Linker (HY-168726); Pink: Target Protein Ligand (HY-168727))
    PROTAC KSP-IN-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-161708
    PROTAC FLT3/CDKs degrader-1
    PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))
    PROTAC FLT3/CDKs degrader-1
  • HY-169378
    CSI86
    CSI86 is a MYC-targeting PROTAC degrader with antiproliferative activity (IC50: 13-18 μM). CSI86 is composed of MYC inhibitor (red part) CSI118 TFA (HY-169379), E3 ligase ligand (blue part) VH032 (HY-120217), and PROTAC linker (black part) Succinic anhydride (HY-79369). The conjugate composed of E3 ligase ligand and linker is (S,R,S)-CO-C2-acid (HY-131866).
    CSI86
  • 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-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-161806
    ZXH-8-004
    ZXH-8-004 (2-12-2-deg) is a potent DENV E PROTAC degrader with an DC50 value of 0.21 µM. ZXH-8-004 shows exhibit antiviral potencies (Blue: E3 ligase (HY-103596), Black: linker (HY-42149); Pink: DENV E ligand (HY-161807)).
    ZXH-8-004
  • 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 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. (Pink: BRD9 Ligand (HY-107446); Blue: CRBN Ligand (HY-W877239))
    PROTAC BRD9 Degrader-9
  • HY-158760
    PROTAC IRAK4 degrader-11
    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
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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