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-157213
    LWY713
    LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models. LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
    LWY713
  • HY-159451
    PROTAC SMARCA2 degrader-7 2568277-71-2
    PROTAC SMARCA2 degrader-7 (Compound I-428) is a PROTAC degrader for SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A (SMARCA) SMARCA2. PROTAC SMARCA2 degrader-7 degrades SMARCA2 and SMARCA4 in MV411 with DC50 of <100 and 100-500 nM. (Pink: Ligand for target protein (HY-159542); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2 degrader-7
  • HY-172265
    FKBP12 PROTAC FM4
    FKBP12 PROTAC FM4 is a PROTAC degrader of MTH1, with a DC50 values of 0.09–0.22 nM. FKBP12 PROTAC FM4 is composed of PROTAC target protein ligand AP1867-3-(aminoethoxy) (HY-129363) (red part), E3 ligase ligand MTH1 ligand 1 (HY-134724) (blue part) and PROTAC Linker t-Boc-N-amido-PEG5-acetic acid (HY-W190962) (black part), among which the conjugate of PROTAC target protein ligand + Linker is FKBP12 Ligand-Linker Conjugate 2 (HY-172266).
    FKBP12 PROTAC FM4
  • HY-176489
    PROTAC pan-KRAS degrader-1 3043908-63-7
    PROTAC pan-KRAS degrader-1 is a pan-KRAS PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc. Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);
    PROTAC pan-KRAS degrader-1
  • HY-135382
    PROTAC IRAK4 degrader-2 2374122-27-5
    PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs.
    PROTAC IRAK4 degrader-2
  • HY-176180
    PROTAC STING degrader-4
    PROTAC STING degrader-4 is a nitro-free covalent STING PROTAC degrader with a DC50 of 3.23 μM. PROTAC STING degrader-4 effectively inhibits STING as well as its downstream signaling, such as p-TBK1 and p-NF-κB (p-P65), and immune-inflammatory cytokines. PROTAC STING degrader-4 mitigates kidney and blood inflammation in Cisplatin (HY-17394)-induced acute kidney injury (AKI) mice model. Pink: STING ligand (HY-176183); Blue: CRBN ligase ligand (HY-103596); Black: linker (HY-176182); CRBN ligase ligand + linker: HY-176181
    PROTAC STING degrader-4
  • HY-122829
    BCL6 PROTAC 1 2257479-54-0
    BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) PROTAC. BCL6 PROTAC 1 inhibits BCL6 cell reporter with an IC50 value of 8.8 µM. BCL6 PROTAC 1 significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6 PROTAC 1 can be used in tumor related research.
    BCL6 PROTAC 1
  • HY-146423
    PROTAC EGFR degrader 6 2409793-28-6
    PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase.
    PROTAC EGFR degrader 6
  • HY-148277
    KTX-612 2573298-14-1
    KTX-612 is an orally active IRAK4 PROTAC degrader with a DC50 value of 7 nM. KTX-612 can be used for the research of oncology.(Pink:IRAK4 inhibitor (HY-150735); Black: linker; Blue: CRBN Ligand (HY-10984))
    KTX-612
  • HY-145514D
    dTAGV-1 2451573-86-5
    dTAGV-1 is a potent and selective degrader of FKBP12F36V-tagged proteins PROTAC degrader. dTAGV-1 can induce degradation of FKBP12F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A)).
    dTAGV-1
  • HY-174428
    PROTAC JAK2 degrader-1
    PROTAC JAK2 degrader-1 (Compound 10i) is a JAK2 PROTAC degrader with a DC50 of 27.35 nM for JAK2 V617F. PROTAC JAK2 degrader-1 promotes the ubiquitination and degradation of JAK2. PROTAC JAK2 degrader-1 inhibits the phosphorylation of JAK2, STAT3 and STAT5. PROTAC JAK2 degrader-1 can be used in the research of myeloproliferative neoplasms (Pink: JAK2 ligand (HY-174430); Blue: E3 ligase ligand (HY-W087383); Black: E3 ligase ligand + linker (HY-174432)).
    PROTAC JAK2 degrader-1
  • HY-128843
    PROTAC MDM2 Degrader-4 2249750-24-9
    PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
    PROTAC MDM2 Degrader-4
  • HY-169269
    PROTAC SMARCA2 degrader-18 2408393-47-3
    PROTAC SMARCA2 degrader-18 (Example144) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-18 has the potential for the research of non-small cell lung cancer (NSCLC).
    PROTAC SMARCA2 degrader-18
  • HY-170859A
    AH081
    AH081 (Compound 38) is a CK1δ/ε PROTAC degrader. AH081 is the negative control compound of AH078 (HY-170859). AH081 has inhibitory but no degradation activity for CK1δ/ε by using an inactive stereoisomer of the VHL ligand. Pink: CK1δ/ε ligand (HY-148251); Blue: VHL ligase ligand (HY-125845B); Black: linker
    AH081
  • HY-163866
    PROTAC SMARCA2 degrader-14 2568276-73-1
    SMARCA2 degrader-3 (compound I-323) 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-14
  • HY-169355
    TrimTAC1 3095569-91-5
    TrimTAC1 is a TRIM21-based PROTAC targeting BRD4. TrimTAC1 selectively degrads NUP98FG-mEGFP-BRD4BD2 nuclear condensates. TrimTAC1 does not degrade soluble mEGFP-BRD4BD2 in A549 cells. (Pink: target protein ligand (+)-JQ-1 (HY-13030); Blue:E3 ligase ligand Acepromazine-OTs (HY-169356); Black: PROTAC linker (HY-W088456); E3 ligase ligand + linker: HY-169357).
    TrimTAC1
  • HY-152133
    PROTAC HDAC6 degrader 1 2785404-76-2
    PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines.
    PROTAC HDAC6 degrader 1
  • HY-168635
    SJ46420
    SJ46420, a SJ46421 (HY-168634) pro-drug variant, is a potent and selective BRD3 PROTAC degrader. SJ46420 degrads BRD3 in a KLHDC2-dependent manner, thereby partially reducing the levels of BRD2 or BRD4 (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-159973)).
    SJ46420
  • 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-169134
    PROTAC 20S proteasome subunit β5 degrader 1
    PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) is a targeted degrader of PROTAC for 20S proteasome subunit β5, with a DC50 value of 0.11 μM in FaDu cells. PROTAC 20S proteasome subunit β5 degrader 1 disrupts the cell cycle, promotes apoptosis, and inhibits cell proliferation and migration in both FaDu and KM3/BTZ cells. PROTAC 20S proteasome subunit β5 degrader 1 can be used to study the resistance of pharyngeal cancer and multiple myeloma to Bortezomib (HY-10227) (Pink: Target protein ligand (HY-10227); Blue: E3 ligase ligand (HY-103596); Black: Linker (HY-169142)).
    PROTAC 20S proteasome subunit β5 degrader 1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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