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-175885
    PROTAC FTO degrader 1
    PROTAC FTO degrader 1 is a Fat Mass and Obesity-associated Protein (FTO) PROTAC degrader. PROTAC FTO degrader 1 selectively degrades FTO depending on VHL E3 ligase and ubiquitin-proteasome system. PROTAC FTO degrader 1 can increase m6A modifications on mRNAs associated with ribosome biogenesis and promote their YTHDF2-mediated decay. PROTAC FTO degrader 1 can inhibit cancer cells proliferation and induce apoptosis. PROTAC FTO degrader 1 can be used for the research of cancer, such as acute myeloid leukemia (AML). (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))
    PROTAC FTO degrader 1
  • HY-174455
    APH02174 3065494-66-5
    APH02174 is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 blocks inflammatory signals by inhibiting IL-6 release. APH02174 can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis. (Pink: IRAK4 Ligand (HY-174470); Blue: CRBN Ligand (HY-45512); Black: Linker; CRBN Ligand+Linker (HY-174796))
    APH02174
  • HY-168257
    PROTAC SMARCA2 degrader-30 2408393-67-7
    PROTAC SMARCA2 degrader-30 (example 85) is a PROTAC SMARCA2 degrader with a DC50 less than 100 nM in H1299 cells.
    PROTAC SMARCA2 degrader-30
  • HY-135558
    PROTAC BRD4 Degrader-3 2313234-00-1
    PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for von Hippel-Lindau and BRD4.
    PROTAC BRD4 Degrader-3
  • HY-173135
    PROTAC KDM4 degrader-1
    PROTAC KDM4 degrader-1 (Compound 11) is a KDM4-targeted proteolysis targeting chimeras (PROTAC) degrader. PROTAC KDM4 degrader-1 can degrade KDM4A-C while sparing KDM4D. PROTAC KDM4 degrader-1 exhibits potent antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 induces apoptosis and cell cycle arrest, and inhibits histone H3 lysine demethylation. (Blue: E3 ligase ligand (HY-112078), Black: linker (HY-W013381); Pink: ligand for target protein (HY-173136) ).
    PROTAC KDM4 degrader-1
  • HY-169273
    PROTAC SMARCA2 degrader-22 2760246-90-8
    PROTAC SMARCA2 degrader-22 (Compound 5) is a PROTAC degrader for SMARCA2 with a degradation efficacy of 94% at 100 nM. PROTAC SMARCA2 degrader-22 inhibits the proliferation of cell A549 with an EC50 < 250 nM.
    PROTAC SMARCA2 degrader-22
  • HY-168246
    PROTAC SMARCA2 degrader-29 2865193-25-3
    PROTAC SMARCA2 degrader-29 (Example 87) is a PROTAC SMARCA2 (BRM) degrader, with DC50 of 10-100 nM (BRM) and > 1 μM (BRG1, also known as SMARCA2) respectively.
    PROTAC SMARCA2 degrader-29
  • HY-168255
    PROTAC BRM/BRG1 degrader-4
    PROTAC BRM/BRG1 degrader-4 (example 047) is a potent BRM and BRG1 PROTAC degrader, with DC50 values of 0.21 nM and 3.4 nM in SW1573 cells, respectively (Pink: ligand for target protein (HY-168252); Black: linker (HY-28911); Blue: E3 ligase ligand (HY-168253)).
    PROTAC BRM/BRG1 degrader-4
  • HY-168551
    PROTAC ALK degrader-3
    PROTAC ALK degrader-3 (4B) is an orally active ALK degrader based on PROTACs, which can effectively induce persistent degradation of ALK fusion protein in Karpas 299 cells and strong inhibition of downstream pathways,IC50 is 119.33 nM. PROTAC ALK degrader-3 exhibits antitumor activity. (Structure Note: PINK, ALK Inhibitor (HY-15656); Blue, E3 (HY-W023573); Black, linker (HY-168552)).
    PROTAC ALK degrader-3
  • HY-175281
    SJ11646 2933135-82-9
    SJ11646 is a Dasatinib (HY-10181)-based LCK PROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)
    SJ11646
  • HY-168229
    PROTAC SMARCA2 degrader-27 2410314-57-5
    PROTAC SMARCA2 degrader-27 (compound 4) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-27 has the potential to be used in cancer research (Pink: SMARCA2 ligand (HY-168230); Blue: VHL ligand (HY-168232); Black: linker (HY-168231)).
    PROTAC SMARCA2 degrader-27
  • HY-148777
    A031 2682255-44-1
    A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP).
    A031
  • HY-169133
    GDCNF-11 2991588-80-6
    GDCNF-11 is a HIM-PROTAC GPX4 degrader based on the chaperone protein HSP90. GDCNF-11 promotes the ubiquitination and degradation of GPX4 through the HSP 90 chaperone complex, reduces endogenous GPX4 expression to induce ferroptosis in HT-1080 cells, and the DC50 value is 0.08 μM (Pink: Target protein ligand (HY-153748); Blue: HSP90 ligand (HY-10212); Black: Linker (HY-W169526)).
    GDCNF-11
  • HY-161498
    XYD198
    XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161499))
    XYD198
  • HY-159651
    PTOTAC HSD17B13 degrader 1 3046195-01-8
    PTOTAC HSD17B13 degrader 1 (compound 1) is a PROTAC targeting 17β-HSD 13 (HSD17B13). PTOTAC HSD17B13 degrader 1 is composed of PROTAC target protein ligand HSD17B13 degrader 2 (HY-159662) (red part), PROTAC Linker tert-Butyl 5-bromoisoindoline-2-carboxylate (HY-W003696) (black part) and E3 ubiquitin ligase ligand E3 ligase Ligand 31 (HY-159660) (blue part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 114 (HY-159661)[1].
    PTOTAC HSD17B13 degrader 1
  • HY-153673
    PROTAC IRAK4 degrader-8 2911615-06-8
    PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC IRAK4 degrader (IC50: 15.5 nM). PROTAC IRAK4 degrader-8 degrades IRAK4 in THP-1 cells (DC50: 1.8 nM)。PROTAC IRAK4 degrader-8 also inhibits L-6 production in human whole blood and LPS-induced human PBMC cells, with IC50s of 246 nM and 2.2 nM respectively.
    PROTAC IRAK4 degrader-8
  • HY-149870
    PROTAC CDK9 degrader-8 2994191-89-6
    PROTAC CDK9 degrader-8 (compound 21) is a potent PROTAC CDK9 degrader with an IC50 value of 0.01 μM. PROTAC CDK9 degrader-8 can be used in research of cancer.
    PROTAC CDK9 degrader-8
  • HY-162106
    PROTAC GPX4 degrader-2
    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. (Pink: Ligand for target protein (HY-159545); Black: Linker (HY-159557); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    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
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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