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-183847
    PROTAC STAT6 degrader-10 3077464-23-1
    PROTAC STAT6 degrader-10 is a STAT6 PROTAC degrader with a DC50 value >1 μM and a DCmax value >0.1 μM. PROTAC STAT6 degrader-10 has the potential for application in inflammation-related diseases.
    PROTAC STAT6 degrader-10
  • HY-148276
    KTX-497 2432993-46-7
    KTX-497 is an IRAK4 PROTAC degrader with a DC50 value of 3 nM. KTX-497 can be used for the research of oncology.(Pink:IRAK4 inhibitor (HY-150735); Black: linker; Blue: CRBN Ligand (HY-10984))
    KTX-497
  • HY-174975
    JY-21
    JY-21 is a BRD4 PROTAC degrader with a DC50 of 3.797 μM. JY-21 has a potent anticancer activity against MDA-MB-231 cells. Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-174994); Black: linker (HY-151862)
    JY-21
  • HY-183100
    UNC8461
    UNC8461 is a PROTAC and is negative control CRBN-recruiting PROTAC analog of UNC8209 (HY-183098). UNC8461 features a methyl group substitution on its CRBN ligand to disrupt CRBN binding. UNC8461 fails to reduce TBK1, AAK1, GAK, and AURKA protein levels in renal cancer cells. UNC8461 does not suppress 3-D soft agar colony formation in renal cancer cells, and exerts modest, partial inhibition on colony formation in some renal cancer cells.
    UNC8461
  • HY-184362
    P-SETDB1-4
    P-SETDB1-4 is a SETDB1 PROTAC degrader with a Kd of 86 nM. P-SETDB1-4 recruits CRBN to SETDB1, induces proteasome-dependent degradation of SETDB1, and forms a ternary complex with CRBN to achieve targeted degradation. P-SETDB1-4 reduces DNA synthesis. P-SETDB1-4 exhibits anticancer activity against breast cancer. P-SETDB1-4 can be used in breast cancer-related research.
    P-SETDB1-4
  • HY-161636
    PROTAC SOS1 degrader-9 3036155-21-9
    PROTAC SOS1 degrader-9 (Compd 10) is a PROTAC-based SOS1 degrader (Red: SOS1 Ligand (HY-161635), Black: linker (HY-W056267), Blue: E3 ligase ligand (HY-161639)).
    PROTAC SOS1 degrader-9
  • HY-157788
    ZX703
    ZX703 (compound 5I) is a PROTAC that significantly degrades GPX4 in a dose- and time-dependent manner through the ubiquitin-proteasome and autophagy-lysosome pathways (DC50=0.315 µM). ZX703 induces ferroptosis by inducing Reactive Oxygen Species (ROS) accumulation in cells. ZX703 can be used for cancer research.
    ZX703
  • HY-181318
    PROTAC EZH2 Degrader-20 3093642-35-1
    PROTAC EZH2 Degrader-20 (compound 54) is an EZH2-target PROTAC degrader with antiproliferative activity and IC50 values of about 10 μM against lymphoma cells. PROTAC EZH2 Degrader-20 can be used for the research of lymphoma.
    PROTAC EZH2 Degrader-20
  • HY-148275
    KTX-955 2573302-50-6
    KTX-955 is an antumor and effective IRAK4 degrader, with DC50 values of 5 nM and 130 nM for IRAK4 and Ikaros, respectively. KTX-955 is composed of CRBN ligand (blue part) Pomalidomide (HY-10984) and target protein ligand (red part) IRAK4-IN-20 (HY-150735).
    KTX-955
  • HY-170335
    PROTAC c-Met degrader-2 2254608-80-3
    PROTAC c-Met degrader-2 (PROTAC2) is a PROTAC-based c-Met degrader, with a DC50 of 50 nM.
    PROTAC c-Met degrader-2
  • HY-184005
    IHMT-BMX-068
    IHMT-BMX-068 is a BMX PROTAC degrader with a DC50 of 0.007 μM. IHMT-BMX-068 promotes ubiquitination and degradation of BMX. IHMT-BMX-068 increases the levels of cleaved PARP and cleaved Caspase-3, and induces Apoptosis. IHMT-BMX-068 exerts anti-cancer effects against prostate cancer. IHMT-BMX-068 can be used for the research of prostate cancer.
    IHMT-BMX-068
  • HY-159570
    XD2-149 2710221-08-0
    XD2-149 is a PROTAC targeting STAT3. XD2-149 consists of PROTAC target protein ligand Napabucasin (HY-13919) (red part), E3 ligase Thalidomide (HY-14658) (black part), and linker NH2-C5-Azacyclohexane-N-Boc (HY-159572) (blue part). The E3 ligase + linker conjugate is Thalidomide-NH-C5-azacyclohexane-N-Boc (HY-159571), and the active control of the target protein ligand is Thalidomide acid (HY-159573)[1].
    XD2-149
  • HY-150797
    QA-68
    QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines
    QA-68
  • HY-183251
    PROTAC p300 degrader-1
    PROTAC p300 degrader-1 is a paralog-selective, PROTAC-based degrader targeting the p300/CBP protein. It exhibits potent antiproliferative, cell cycle arrest and pro-apoptotic activities, and can be used in the research and development of antitumor drugs and related mechanism studies for hematological malignancies (AML, MM, NHL).
    PROTAC p300 degrader-1
  • HY-184230
    PROTAC HPK1 Degrader-8 3120899-50-2
    PROTAC HPK1 Degrader-8 is a HPK1 PROTAC degrader with a DC50 of 1-10 nM. PROTAC HPK1 Degrader-8 promotes HPK1 ubiquitination and degradation. PROTAC HPK1 Degrader-8 induces IL-2 production, with an EC50 of 3 nM. PROTAC HPK1 Degrader-8 can be used in research related to hematologic malignancies and solid tumors.
    PROTAC HPK1 Degrader-8
  • HY-182970
    PROTAC SAMHD1 Degrader-1
    PROTAC SAMHD1 Degrader-1 is an orally active targeted SAMHD1 PROTAC degrader, with an IC50 of 6.3 μM against the dNTP hydrolase activity of SAMHD1. PROTAC SAMHD1 Degrader-1 binds to SAMHD1 inside cells and mediates its degradation, with low off-target effects. PROTAC SAMHD1 Degrader-1 inhibits the production of pro-inflammatory cytokines and interferes with the cascade amplification process of inflammatory responses. PROTAC SAMHD1 Degrader-1 delays the progression of pulmonary fibrosis and exerts protective effects on lung tissues. PROTAC SAMHD1 Degrader-1 can be used in pulmonary fibrosis-related research. (Pink: SAMHD1 Target protein ligand (HY-182973); Blue: DCAF1 ligand (HY-182974); Black: linker (HY-W067705)).
    PROTAC SAMHD1 Degrader-1
  • HY-181326
    PROTAC EZH2 Degrader-25 2653338-69-1
    PROTAC EZH2 Degrader-25 (compound 10) is an EZH2-targeting PROTAC degrader. PROTAC EZH2 Degrader-25 triggers ubiquitination and subsequent proteasomal degradation of EZH2. PROTAC EZH2 Degrader-25 can be used for the research of lymphoma.
    PROTAC EZH2 Degrader-25
  • HY-160562
    PROTAC ERα Degrader-7 3025781-93-2
    PROTAC ERα Degrader-7 (compound i-320) is a potent estrogen receptor alpha(ERα) PROTAC degrader with a DC50 value of 0.000006 µM. PROTAC ERα Degrader-7 comprises a cereblon-binding moiety LBM linked to a ligand ERBM that binds ERα and comprises a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring.
    PROTAC ERα Degrader-7
  • HY-181410
    PROTAC EZH2 Degrader-41 3093642-41-9
    PROTAC EZH2 Degrader-41 is an EZH2-targeting PROTAC and cIAP E3 ubiquitin ligase recruiter. PROTAC EZH2 Degrader-41 induces EZH2 degradation via ubiquitination and proteasomal breakdown. PROTAC EZH2 Degrader-41 exerts antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 can be used for the research of lymphoma.
    PROTAC EZH2 Degrader-41
  • HY-162245
    PROTAC SMARCA2 degrader-3 3024266-69-8
    PROTAC SMARCA2 degrader-3 is a PROTAC degrader of the SWI/SNF ATPase subunits, SMARCA2. PROTAC SMARCA2 degrader-3 has anticancer effects (WO2023244764A1; Compound 153).
    PROTAC SMARCA2 degrader-3
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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