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-131188
    PROTAC Bcl-xL degrader-1 2450351-07-0
    PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively.
    PROTAC Bcl-xL degrader-1
  • HY-129937
    (S)-GNE-987 2738533-33-8
    (S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).
    (S)-GNE-987
  • HY-P10446
    TAT-PiET-PROTAC 3036046-04-2
    TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer.
    TAT-PiET-PROTAC
  • HY-178066
    PROTAC BCL-xL/BCL-w Degrader 1
    PROTAC BCL-xL/BCL-w Degrader 1 (Compound 44) is a BCL-xL/BCL-w PROTAC degrader. PROTAC BCL-xL/BCL-w Degrader 1 has significant anticancer activity with reduced on-target platelet toxicity . Pink: BCL-xL/BCL-w ligand (HY-10087); Blue: CRBN ligase ligand (HY-163233); Black: linker (HY-Y1230)
    PROTAC BCL-xL/BCL-w Degrader 1
  • HY-158048
    UNC9036
    UNC9036 is a PROTAC-based STING degrader, with a DC50 of 227 nM. UNC9036-mediated STING degradation is proteasome and VHL dependent (Structure Note: Red, STING agonist diABZI (HY-112921A); Blue, VHL ligand VH032 (HY-120217); Black, linker).
    UNC9036
  • HY-168678
    PROTAC K-Ras Degrader-6 3052745-46-4
    pan-KRAS degrader 5 (compound 102) is a potent cereblon-based KRAS PROTAC degrader, with a DC50 of <100 nM. pan-KRAS degrader 5 shows anticancer effects. (Pink: ligand for target protein (HY-168679); Black: linker (HY-168670); Blue: E3 ligase ligand (HY-W580113)).
    PROTAC K-Ras Degrader-6
  • HY-175652
    PROTAC Androgen receptor degrader-1 3056515-10-4
    PROTAC Androgen receptor degrader-1 (Ex.14) is a PROTAC degrader targeting the androgen receptor with a DC50 of 6 nM. PROTAC Androgen receptor degrader-1 is used in prostate cancer research. (Structure Note: Pink: target protein ligand (HY-175654); Blue: E3 ligase ligand (HY-175654); Black: linker).
    PROTAC Androgen receptor degrader-1
  • HY-156401
    BRD9 Degrader-1
    BRD9 c-1 (Compound 13-7) is a PROTAC BRD9 degrader. BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062). (Blue: VH032-cyclopropane-F (HY-125905); Black: linker (HY-W763939); Pink: HY-168695).
    BRD9 Degrader-1
  • HY-145400
    PROTAC BRD9 Degrader-3 2633632-05-8
    PROTAC BRD9 Degrader-3 is a BRD9 bifunctional degrader for researching cancer.
    PROTAC BRD9 Degrader-3
  • HY-153322
    ITK degrader 2 2858738-65-3
    ITK degrader 2 (compound 30) is an orally active, PROTAC-based ITK-targeted degrader (DC50<10 nM). ITK degrader 2 exhibits Cmax and Tmax in mice (po; 90 mg/kg) of 0.87 μM and 2 h, respectively. At this dose, ITK degrader 2 degrades ITK by 20% (6 h) in mice.
    ITK degrader 2
  • HY-174135
    PROTAC HPK1 Degrader-4
    PROTAC HPK1 Degrader-4 (compound E3) is a selective and orally active PROTAC HPK1 degrader with a DC50 of 3.16 nM. PROTAC HPK1 Degrader-4 demonstrates >1000-fold selectivity over GLK. PROTAC HPK1 Degrader-4 promotes immune activation. PROTAC HPK1 Degrader-4 can be used for the study of colon cancer and lymphoma (Pink: ligand for target protein (HY-174355); Blue: ligand for E3 ligase CRBN (HY-45808); Black: Linker (HY-174356); Target protein ligand-linker Conjugate (HY-174357)).
    PROTAC HPK1 Degrader-4
  • HY-162651
    PROTAC BRD9 Degrader-8 3081180-48-2
    PROTAC BRD9 Degrader-8 (compound E5) is a PROTAC-based BRD9 degrader with a DC50 value of 16 pM. PROTAC BRD9 Degrader-8 has antiproliferation in MV4–11 cells (IC50 = 0.27 nM) and OCI-LY10 cells (IC50 = 1.04 nM).
    PROTAC BRD9 Degrader-8
  • HY-169151
    PROTAC BRD4-DCAF1 degrader-1 3036944-87-0
    PROTAC BRD4-DCAF1 degrader-1 (I-907) is a BRD4-DCAF1 PROTAC degrader, DC50 is 10~100 nM. (Pink: BRD4-DCAF1 ligand (HY-169152); Black: linker (HY-126976); Blue: E3 ligase ligand (HY-15846)).
    PROTAC BRD4-DCAF1 degrader-1
  • HY-163152
    PROTAC BRM degrader-1 2378051-80-8
    PROTAC BRM degrader-1 (compound 17) is a PROTAC-based BRM and BRG1 degrader, with DC50 values of 93 pM and 4.9 nM, respectively.
    PROTAC BRM degrader-1
  • HY-163845
    YX862
    YX862 is a selective HDAC8 PROTAC degrader and induces the degradation of HDAC8 with maximum degradation ＞ 95% at 250 nM in MDA-MB-231 cells(Sturcture Note:(Blue: VHL E3 ligand (HY-112078), Black: linker；Pink: HDAC8 inhibitor (HY-163846)).
    YX862
  • HY-175541
    TQ-3959 2926610-43-5
    TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)).
    TQ-3959
  • HY-169008
    PROTAC ACC degrader-1
    PROTAC ACC degrader-1 (Compound 9b) is a Acetyl-CoA Carboxylase degrader. PROTAC ACC degrader-1 exhibits superior potency against Aphis craccivora (IC50 = 107.8 μg/mL). (Structure Note: Pink, Target protein ligand (HY-169009); Blue, E3 ligand (HY-10984); Black, linker (HY-W007559).
    PROTAC ACC degrader-1
  • HY-163864
    PROTAC SMARCA2/4-degrader-11 2568276-71-9
    SMARCA2 degrader-1 (compound I-321) is a PROTAC degrader of SMARCA with DC50＜100nM (red: SMARCA inhibitor, black: linker (HY-Y1215), blue: E3 ligase ligand (HY-163927) ).
    PROTAC SMARCA2/4-degrader-11
  • HY-158047
    UNC8900
    UNC8900 is a VHL recruiting STING PROTAC degrader (DC50: 0.0.924 μM). UNC8900 can be used for research of viral or bacterial infection. (Blue: VHL ligand, black: linker; Pink: STING inhibitor).
    UNC8900
  • HY-143883
    MS143 2376137-41-4
    MS143 is a potent PROTAC AKT degrader (DC50=46 nM and GI50=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth (Pink: AKT ligand (HY-15431); Blue: E3 ligase ligand (HY-125845); Black: linker).
    MS143
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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