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-163440
    PROTAC NAMPT Degrader-1
    PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC50 value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC50 value of 0.12μM against A2780 cells. (Structure Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker).
    PROTAC NAMPT Degrader-1
  • HY-163877
    PROTAC SMARCA2/4-degrader-19 2568277-57-4
    PROTAC SMARCA2/4-degrader-19 (Compound I-412) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-19 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-163949); Black: Linker (HY-W006635); Blue: Ligand for E3 Ligase (HY-125845))
    PROTAC SMARCA2/4-degrader-19
  • HY-170448
    PROTAC AR Degrader-9
    PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 promotes the expressions of paracrine factors, such as TGF-β1 and β-catenin, exhibits hair regenerating efficacy in mouse models. (Pink: ligand for target protein AR ligand-38 (HY-170450); Black: linker; Blue: ligand for E3 ligase Cereblon (HY-170449))
    PROTAC AR Degrader-9
  • HY-174453
    PROTAC ERα Degrader-12
    PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)).
    PROTAC ERα Degrader-12
  • HY-175321
    PROTAC c-Met degrader-6
    PROTAC c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC50s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC c-Met degrader-6 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer (Pink: c-Met ligand (HY-W425461); Blue: E3 ligand (HY-14658); Black: Linker (HY-20797)).
    PROTAC c-Met degrader-6
  • HY-171148
    F1-RIBOTAC 3019907-96-8
    F1-RIBOTAC is a ribonuclease-targeting chimeras (RIBOTACs). F1-RIBOTAC decreases QSOX1-a mRNA expression level in an RNase L-dependent manner. F1-RIBOTAC can be used for the research of cancer. (Pink: RNA ligand (HY-168460); Black: linker (HY-W008005); Blue: RNase L ligand (HY-168452))
    F1-RIBOTAC
  • HY-175022
    PROTAC IRAK4 degrader-13 2432992-21-5
    PROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC50s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research. Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker
    PROTAC IRAK4 degrader-13
  • HY-169433
    Naph-Se-TMZ
    Naph-Se-TMZ is a PROTAC-like HDAC1 degrader. Naph-Se-TMZ can reduce the total HDAC activity in glioma cells and enhance the inhibitory effect of Temozolomide (HY-17364). Naph-Se-TMZ consists of the target protein ligand (red part) Temozolomide (HY-17364), the DNA-targeting intercalator (blue part) Nitro-Naphthalimide-C2-acylamide (HY-169437) and the molecular linker (black part). At the same time, the active control of the target protein ligand is: Temozolomide-amino hydrochloride (HY-169439), and the DNA targeting intercalator + linker is: NNISC-2 (HY-169438).
    Naph-Se-TMZ
  • HY-168448
    dBAZ2 3104449-57-9
    dBAZ2 is a first-in-class BAZ2A and BAZ2B PROTAC degrader with DC50 values of 180 nM and 250 nM for BAZ2A and BAZ2B, respectively. (Blue: E3 ligase ligand (VH 101, thiol (HY-47851); Black: linker (HY-168450); pink: target protein ligand (HY-168449)).
    dBAZ2
  • HY-176421
    PROTAC PI3K/110β degrader-1 3070438-85-3
    PROTAC PI3K/110β degrader-1 (J-9) is a PROTAC based PI3K/110β degrader (Red: PI3K/110β inhibitor (HY-75124), black: linker, Blue: E3 ligase ligand).
    PROTAC PI3K/110β degrader-1
  • HY-145514B
    dTAGV-1-NEG TFA
    dTAGV-1-NEG TFA is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1-NEG TFA is an FKBP12F36V-selective degrader.
    dTAGV-1-NEG TFA
  • HY-175240
    PROTAC BRD4 Degrader-38
    PROTAC BRD4 Degrader-38 is a BRD4 PROTAC degrader with DC50s of 86 and 106 nM for the short and long isoforms of BRD4, respectively. PROTAC BRD4 Degrader-38 significantly induces the degradation of BRD4 by covalently engaging C232 of E3 ligase TRIM28.Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-203082); Black: linker (HY-40172)
    PROTAC BRD4 Degrader-38
  • HY-174351
    NU-PRO-1
    NU-PRO-1 is a covalent Telomerase reverse transcriptase (TERT) PROTAC degrader. NU-PRO-1 dose not induce DNA damage on its own but acts to further delay DNA repair after irradiation. Pink: TERT ligand (HY-174352); Blue: VHL ligase ligand (HY-125845); Black: linker (HY-W005056)
    NU-PRO-1
  • HY-160262
    AR/BET protein degrader-1 2571123-81-2
    AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research.
    AR/BET protein degrader-1
  • HY-174996
    NEP162 3031840-36-2
    NEP162 is a BRD4 PROTAC degrader with DC50s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc. (Pink: BRD4 ligand : (HY-78695), Blue: E3 ligase Ligand (HY-D2259), BLACK: Linker, E3 ligase ligand-linker conjugate (HY-174997)).
    NEP162
  • HY-161450
    LHF418
    LHF418 is an effective SOS1 PROTAC degrader with a DC50 value of 209.4 nM in A549 cells. LHF418 can effectively inhibit RAS signaling and colony formation in KRAS-driven cancer cells. (Structural note: (Blue: Cereblon ligand (HY-A0003), Black: linker; Pink: SOS1 binder SOS1 Ligand intermediate-3 (HY-161452)).
    LHF418
  • HY-159087
    RGB110
    RGB110 (Compound 10d) is a PROTAC inhibitor for D-dopachrome tautomerase with an IC50 of 5.9 μM. RGB110 causes no degradation of D-DT. (Pink: ligand for target protein (HY-159164); Black: linker (HY-W125017); Blue: ligand for E3 ligase CRBN (HY-10984))
    RGB110
  • HY-158551
    PROTAC BcI-2/BcI-xI Degrader-1 3034200-49-9
    PROTAC BcI-2/BcI-xI Degrader-1 (15) is a PROTAC based BcI-2/BcI-xI degrader (Red: BcI-2/BcI-xI inhibitor (HY-158677), black: linker, Blue: E3 ligase ligand).
    PROTAC BcI-2/BcI-xI Degrader-1
  • HY-161769
    HL435
    HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
    HL435
  • HY-157767
    Abd110 3021581-79-0
    Abd110 (compound 42i) is a Lenalidomide-based PROTAC ATR kinase degrader. Abd110 selectively decreases ATR and phospho-ATR without affecting related kinases ATM and DNA-PKcs.
    Abd110
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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