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-155356A
    YN14 (mixture of diastereomers) 3053689-54-3
    YN14 mixture of diastereomers is the diastereomers of YN14 (HY-155356). 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 (mixture of diastereomers)
  • HY-178858
    PROTAC FLT3/CHK1 Degrader-1
    PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)).
    PROTAC FLT3/CHK1 Degrader-1
  • HY-184335
    PROTAC BET Degrader-18 3097564-20-7
    PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis, while suppressing oncoprotein expression. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer.
    PROTAC BET Degrader-18
  • HY-181537
    PROTAC TEAD1/IAP degrader-2
    PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC50 of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research.
    PROTAC TEAD1/IAP degrader-2
  • HY-176823
    PROTAC SGK3 degrader-2 2381196-78-5
    PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878), with a cis hydroxyl group in its VH032 moiety, which is incapable of binding to the VHL E3 ligase. PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but shows no SGK3 degradation efficiency. PROTAC SGK3 degrader-2 can be used as a control compound to study the specific effects of SGK3-PROTAC1-mediated SGK3 degradation. (Pink: SGK3 ligand (HY-167701), Blue: VHL Ligand (HY-120217A), Black: Linker (HY-130618), SGK3 ligand-linker conjugate (HY-176824)).
    PROTAC SGK3 degrader-2
  • HY-162450
    Antitumor agent-150
    Antitumor agent-150 (V10), an anti-breast cancer agent, is a PROTAC-based MDM2 protein degrader (Red: Ganoderic acid A; Black: 4O-PEG linker; Blue: VHL ligand).
    Antitumor agent-150
  • HY-169232
    PCC16 chloride
    PCC16 chloride is a CRBN-based cp-PCC with an IC50 value of 102 nM for the degradation of DHHC3. PCC16 chloride has antitumor activity.
    PCC16 chloride
  • HY-179657
    PROTAC MLT Degrader 1
    PROTAC MLT Degrader 1 (M-PRORAC) is an asymmetric dual-functional degrader based on MLT PROTAC. PROTAC MLT Degrader 1 significantly reduces the protein level of p300 in the cell. PROTAC MLT Degrader 1 can be used in Alzheimer's disease research (pink: MLT ligand (HY-B0075); blue: CRBN ligand (HY-41547); black: linker (HY-140208)).
    PROTAC MLT Degrader 1
  • HY-169072
    PROTAC MLKL Degrader-2 3103327-20-1
    PROTAC MLKL Degrader-2 (compound MP-1) is a PROTAC targeting MLKL (Mixed Lineage Kinase). PROTAC MLKL Degrader-2 is composed of PROTAC target protein ligand PROTAC MLKL Degrader-2 (HY-169072) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part) and PROTAC Linker N-Methylpiperazine (HY-78871) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-N-methylpiperazine (HY-169074)[1].
    PROTAC MLKL Degrader-2
  • HY-146369
    PROTAC VEGFR-2 degrader-2 2353417-85-1
    PROTAC VEGFR-2 degrader-2 is a VEGFR-2 (KDR) PROTAC degrader with weak inhibitory activity against VEGFR-2 (IC50 > 1 μM). It is applicable to the research of cancer-related pathological angiogenesis.
    PROTAC VEGFR-2 degrader-2
  • HY-179384
    PROTAC FSP1 degrader 1 3096510-51-6
    PROTAC FSP1 degrader 1 is a highly efficient and selective PROTAC degrader targeting FSP1. PROTAC FSP1 degrader 1 significantly induces the accumulation of intracellular lipid peroxides. PROTAC FSP1 degrader 1 exhibits synergistic induction of ferroptosis with GPX4 inhibitors. PROTAC FSP1 degrader 1 can induce ROS production. PROTAC FSP1 degrader 1 upregulates the mRNA expression of ferroptosis-related proteins (GPX4, FTH1, ACSL4, TfR1, FSP1). PROTAC FSP1 degrader 1 can be used for the study of triple-negative breast cancer.
    PROTAC FSP1 degrader 1
  • HY-186132
    PROTAC CDK2-pRb degrader-1 3030276-48-0
    PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer).
    PROTAC CDK2-pRb degrader-1
  • HY-176740
    PROTAC Bcl-xL degrader-4 2930759-37-6
    PROTAC Bcl-xL degrader-4 (Compound 2-38-III) is a Bcl-xL PROTAC degrader. PROTAC Bcl-xL degrader-4 has strong anti-tumor activity against HepG2 cells and HUVEC cells. PROTAC Bcl-xL degrader-4 induces cells apoptosis by decreasing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTAC Bcl-xL degrader-4 significantly inhibits tumor growth in xenograft tumor mouse models. Pink: MAPK ligand (HY-176741); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W017440)
    PROTAC Bcl-xL degrader-4
  • HY-170390
    AB3067
    AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM.
    AB3067
  • HY-171802
    PROTAC LRRK2 Degrader-2 3080678-93-6
    PROTAC LRRK2 Degrader-2 is a PROTAC-based degrader targeting LRRK2 with a DC50 of 0.14 nM. PROTAC LRRK2 Degrader-2 recruits LRRK2 or its mutants to the cereblon E3 ubiquitin ligase, thereby mediating the targeted ubiquitination and subsequent proteasomal degradation of LRRK2. PROTAC LRRK2 Degrader-2 can be used in research related to Parkinson's disease.
    PROTAC LRRK2 Degrader-2
  • HY-181568
    PROTAC Aurora A Degrader-1 3115344-59-4
    PROTAC Aurora A Degrader-1 (Compound 280) is a blood-brain barrier-permeable selective Aurora A PROTAC degrader, with DC50 values of 1 nM and 2 nM in LAN5 and SMS-SAN cells, respectively. PROTAC Aurora A Degrader-1 induces the formation of a ternary complex between AURKA and CRBN, degrades AURKA, reduces MYCN levels, induces DNA damage and apoptosis, exerts antiproliferative activity in cancer cells, and regulates the immune system. PROTAC Aurora A Degrader-1 is applicable to the research of neuroblastoma and small cell lung cancer.
    PROTAC Aurora A Degrader-1
  • HY-169861
    PROTAC SMARCA2/4 degrader-37 2688882-69-9
    PROTAC SMARCA2/4 degrader-37 (Example 4) is a PROTAC-based SMARCA2/4 degrader, with an IC50 of ≤0.1 μM (Pink: SMARCA2/4 lignad (HY-172446); Black: CRBN ligand (HY-41547); Linker (HY-N2407)).
    PROTAC SMARCA2/4 degrader-37
  • HY-176440
    BP-198
    BP-198 is an Mpro PROTAC degrader. BP-198 promotes the ubiquitination and degradation of Mpro. BP-198 has antiviral effects against SARS-CoV-2 (IC50: 11.8 μM) and has stronger activity against drug-resistant viruses. (Pink: target protein ligand (HY-176442); blue: E3 ligase ligand (HY-176441); black: linker (HY-W457968); E3 ligase-linker conjugate (HY-176443)).
    BP-198
  • HY-103636R
    PROTAC Sirt2 Degrader-1 (Standard) 2098487-75-1
    PROTAC Sirt2 Degrader-1 (Standard) is the analytical standard of PROTAC Sirt2 Degrader-1 (HY-103636). This product is intended for research and analytical applications. PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM).
    PROTAC Sirt2 Degrader-1 (Standard)
  • HY-163851
    PROTAC Vif degrader-1
    PROTAC Vif degrader-1 (Compound L15) is a Vif PROTAC degrader. PROTAC Vif degrader-1 has antiviral activity against HIV-1 (EC50: 33.35 μM against HIV-1IIIB).
    PROTAC Vif degrader-1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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