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-162241
    SJH1-62B
    SJH1-62B is a proteolysis targeting chimera (PROTAC) that can target the androgen receptor (AR).
    SJH1-62B
  • HY-153573
    SRG-II-19F
    SRG-II-19F (dCym-JQ1) is a bromodomain1 of BRDT (BRDTBD1) PROTAC degrader. SRG-II-19F can be used for testing the regulatory effect of ClpC2 on the ClpC1P1P2 protease.
    SRG-II-19F
  • HY-163873
    PROTAC SMARCA2/4-degrader-20 2568277-38-1
    PROTAC SMARCA2/4-degrader-20 (Compound I-405) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2/4-degrader-20 degrades SMARCA2 in A549 and MV411 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 of 100-500 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-W006635); Blue: Ligand for E3 Ligase (HY-163932))
    PROTAC SMARCA2/4-degrader-20
  • HY-173437
    CW-2
    CW-2 is a PARP1 PROTAC degrader. CW-2 has potent antiproliferative effects against MDA-MB-231 cells (IC50 = 0.72 μM) and CDDP-resistant cells (A549/CDDP: IC50 = 3.52 μM). CW-2 has synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts antitumor effects by inducing DNA damage, impairing DNA repair, and activating mitochondria-dependent apoptosis (Pink: PARP1 ligand (HY-173441); Blue: E3 CRBN ligand (HY-173439); Black: linker (HY-173440)).
    CW-2
  • HY-161167
    MM-02-08
    MM-02-08 is the potent BRD4 degrader and binds to DDB1.
    MM-02-08
  • HY-175040
    PROTAC FLT-3 degrader 5
    PROTAC FLT-3 degrader 5 is a FLT3 PROTAC degrader (DC50 = 1.2 nM). PROTAC FLT-3 degrader 5 functions as a molecular glue to degrade cereblon substrates GSPT1 and IKZF1/3. PROTAC FLT-3 degrader 5 exhibits antiproliferative activity against drug-resistant acute myeloid leukemia (AML) cells and is potentially useful in AML research. (Pink: FLT3/GSPT1/IKZF1/3 ligand: (HY-169374); Blue: Thalidomide: (HY-14658); Black: linker; Thalidomide + linker: (HY-W1123823)).
    PROTAC FLT-3 degrader 5
  • HY-157577
    PROTAC(H-PGDS)-8 2761281-51-8
    PROTAC(H-PGDS)-8 is a Hematopoietic prostaglandin D synthase (H-PGDS) PROTAC degrader, with a IC50 of 0.14 μM.
    PROTAC(H-PGDS)-8
  • HY-175678
    PROTAC BRD2 BD1 Degrader-1
    PROTAC BRD2 BD1 Degrader-1 (compound 21-1) is a potent and selective BRD2 BD1 PROTAC degrader. PROTAC BRD2 BD1 Degrader-1 induces the association of BRD2 BD1 and von Hippel–Lindau-elongin C-elongin B (VCB). (Pink: BRD2-BD1 Ligand (HY-175679); Blue: E3 ligase ligand (HY-125845); Black: Linker (HY-W069332)).
    PROTAC BRD2 BD1 Degrader-1
  • HY-163679
    PROTAC ERα Degrader-9
    PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7EGFR (IC50=0.075 μM), MCF-7D538G (IC50=0.31 μM), MCF-7Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
    PROTAC ERα Degrader-9
  • HY-170595
    PROTAC LZK-IN-1 2763268-64-8
    PROTAC LZK-IN-1 (Compound 21A) is a PROTAC that targets the degradation of LZK (Leucine Zipper Kinase, encoded by MAP3K13). PROTAC LZK-IN-1 (10 μM) promotes the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. PROTAC LZK-IN-1 can be used in cancer research. PROTAC LZK-IN-1 consists of an E3 ligase ligand (blue part, HY-112078), a target protein ligand (red part, HY-170596), and a linker (black part, HY-W019543)[1].
    PROTAC LZK-IN-1
  • HY-169264
    SJYHJ-026
    SJYHJ-026 (compound 37) is a pregnane X receptor (PXR) PROTAC degrader with the DC50 of 86.6 nM and maximal degradation of 66.4%. SJYHJ-026 shows cell cytotoxic aganist SNU-C4 HiBiT-PXR KI cells with the IC50 values of 97.4 μM (24 h) and 99.5 μM (72 h) (Blue: VHL ligand HY-125845,Black: linker HY-43048；Pink: PXR inhibitor HY-169277).
    SJYHJ-026
  • HY-142662
    PROTAC IRAK3 degrader-1 2712600-00-3
    PROTAC IRAK3 degrade-1 (compound 23) is a potent and selective degrader of IRAK3 (IC50 = 5 nM).
    PROTAC IRAK3 degrader-1
  • HY-162098
    PROTAC tubulin-Degrader-1
    PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)).
    PROTAC tubulin-Degrader-1
  • HY-150400
    XF056-132 free base 2407450-73-9
    XF056-132 free base is a potent WDR5 (WD40 repeat domain protein 5) PROTAC degrader.
    XF056-132 free base
  • HY-173467
    PROTAC MTP3 degrader-1
    PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader (Red: MYC inhibitor (HY-173469), black: linker (HY-W008296), Blue: E3 ligase ligand (HY-14658)).
    PROTAC MTP3 degrader-1
  • HY-178215
    PROTAC SMARCA2/4 degrader-40
    BRM/BRG1 ligand 4 (Compound 6) is a SMARCA2/4 PROTAC degrader. BRM/BRG1 ligand 4 exhibits potent degradation activity against both SMARCA2 and SMARCA4 in HeLa cells, with DC50 less than 0.1 nM. BRM/BRG1 ligand 4 can be used for the study of cancers associated with SMARCA2/SMARCA4 abnormalities or SWI/SNF mutations.
    PROTAC SMARCA2/4 degrader-40
  • HY-170855A
    YW-N-7 TFA
    YW-N-7 (TFA) is a PROTAC that targets both the inhibition and degradation of RET kinase, with a DC50 of 88 nM. YW-N-7 (TFA) exhibits antitumor activity in a KIF5B-RET-driven xenograft mouse tumor model and can be used in the area of cancer (Structure: red part represents the target protein ligand: HY-170856; blue part represents the E3 ligase ligand: HY-1708557; black part represents the linker; E3 ligase ligand + linker: HY-170858).
    YW-N-7 TFA
  • HY-178797
    PROTAC LRRK2 Degrader-3 3080678-98-1
    PROTAC LRRK2 Degrader-3 is a PROTAC LRRK2 degrader with a DC50 of 0.17 nM. PROTAC LRRK2 Degrader-3 can be used for research in Parkinson’s disease and inflammation. (Pink: LRRK2 ligand: LRRK2-IN-19 (HY-177016); Black: Linker (HY-178830); Blue: E3 ligand (HY-163927); E3+Linker (HY-178828)).
    PROTAC LRRK2 Degrader-3
  • HY-139315
    PROTAC IRAK4 degrader-4 2360528-45-4
    PROTAC IRAK4 degrader-4 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127.
    PROTAC IRAK4 degrader-4
  • HY-175867
    PROTAC SMARCA2 degrader-34
    PROTAC SMARCA2 degrader-34 (compound 52) is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: < 0.1 μM for SMARCA2, > 1 μM for SMARCA4). PROTAC SMARCA2 degrader-34 can be used for study of cancer. (Pink: SMARCA2 ligand (HY-178414) ; Blue: E3 ligand (HY-168055) ; Black: linker).
    PROTAC SMARCA2 degrader-34
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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