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-159608
    PROTAC Cbl-b-IN-1 3035210-39-7
    PROTAC Cbl-b-IN-1 (compound 64) is a PROTAC targeting Cbl-b. PROTAC Cbl-b-IN-1 is composed of PROTAC target protein ligand Cbl-b-IN-21 (HY-159615), PROTAC Linker Cbz-Pip-2C-Pip-C-Pip (HY-159617) and E3 ubiquitin ligase ligand (3S) Lenalidomide-5-Br (HY-W797329), where the E3 ubiquitin ligase ligand + Linker conjugate is (3S) Lenalidomide-5-Pip-C-Pip-2C-Pip (HY-159618)[1].
    PROTAC Cbl-b-IN-1
  • HY-172590
    LZ-07
    LZ-07 is a IRAK4 PROTAC degrader (DC50 = 1.14 nM). LZ-07 leads to marked suppression of cytokines including IL-6, IL-1β, TNF-α, and IL-10 upon degradation of IRAK4. LZ-07 can be studied in research for autoimmune diseases (Pink: IRAK4 ligand (HY-172591); Blue: CRBN ligand (HY-34590); Black: linker (HY-B0149); CRBN ligand + linker: HY-172593).
    LZ-07
  • HY-168487
    PROTAC WDR5 degrader 1 2737222-94-3
    PROTAC WDR5 degrader 1 (compound 8g) is a PROTAC degrader targeting WDR5. PROTAC WDR5 degrader 1 is composed of a target protein ligand (red part) WDR5 ligand 2 (HY-168488), a VHL-type E3 ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and a PROTAC linker (balck part) 5-Aminovaleric acid (HY-W015878), in which the VHL ligand and the PROTAC linker form a conjugate (HY-114176A).
    PROTAC WDR5 degrader 1
  • HY-163938A
    PROTAC erf3a Degrader-2 3033871-15-4
    PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-2 inhibits protein expression of SRD5A3 and GSPT1(eRF3a). PROTAC erf3a Degrader-2 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-2 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: E3 ligase ligand (HY-W763812)).
    PROTAC erf3a Degrader-2
  • HY-153574
    BI01826025
    BI01826025 (pArg-JQ1) is a bromodomain1 of BRDT (BRDTBD1) PROTAC degrader. BI01826025 can be used for testing the regulatory effect of ClpC2 on the ClpC1P1P2 protease.
    BI01826025
  • HY-155396
    PRO-HD1
    PRO-HD1 is a PROTAC HDAC6 degrader. PRO-HD1 degrades HDAC6 in A549 cells, and inhibits proliferation of Jurkat cells (IC50: 5.8 μM).
    PRO-HD1
  • HY-159454
    PROTAC SMARCA2/4-degrader-3 2568507-10-6
    SMARCA2/4-degrader-3 (compound I-433) is a PROTAC SMARCA2/4-degrader based on VH032-NH2, with a degradation potency (DC50) <100 nM in MV4-11 cells.
    PROTAC SMARCA2/4-degrader-3
  • HY-145073
    PROTAC ER Degrader-10 2504911-58-2
    PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research. PROTAC ER Degrader-10 is extracted from patent WO2021133886, example 36.
    PROTAC ER Degrader-10
  • HY-168554
    STING-IN-10
    STING-IN-10 (P8) is a dual STING PROTAC degrader and inhibitor with a DC50 value of 2.58 μM in THP-1 cells. STING-IN-10 has anti-inflammatory activity.(Pink: Target protein ligand (HY-168676); Black: linker (HY-W123015); Blue: E3 ligase ligand (HY-126457))
    STING-IN-10
  • HY-159449
    PROTAC SMARCA2 degrader-5 2568277-68-7
    PROTAC SMARCA2 degrader-5 (Compound I-425) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2 degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 with DC50 of 100-500 nM. (Pink: Ligand for target protein (HY-159531); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2 degrader-5
  • HY-158429
    PROTAC CYP1B1 degrader-2 2836297-26-6
    PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with the DC50 of 1.0 nM at 24 h in A549/Taxol cells. PROTAC CYP1B1 degrader-2 inhibits growth, migration, and invasion of A549/Taxol cell(Sturcture Note:(Blue: VHL ligand (HY-112078), Black: linker (HY-W007700), Pink: CYP1B1 ligand (HY-159006).
    PROTAC CYP1B1 degrader-2
  • HY-178118
    PROTAC PDIA1 degrader 1 3024292-21-2
    PROTAC PDIA1 degrader 1 (Compound H4) is a PDIA1 PROTAC degrader with a DC50 of 29.71 μM. PROTAC PDIA1 degrader 1 has potent anticancer activity and significantly inhibits cancer cell proliferation. Pink: PDIA1 ligand (HY-100433); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W015088)
    PROTAC PDIA1 degrader 1
  • HY-159452
    PROTAC SMARCA2/4-degrader-1 2568273-68-5
    SMARCA2/4-degrader-1 (compound I-430) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment.
    PROTAC SMARCA2/4-degrader-1
  • HY-145737
    PROTAC SOS1 degrader-1 2913185-35-8
    PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity.
    PROTAC SOS1 degrader-1
  • HY-164906
    TMX-2138 2488892-07-3
    TMX-2138 is a CDKs PROTAC degrader, with IC50s of 8.7 nM, 10.9 nM, 7.0 nM and 25.7 nM for CDK1/cyclinB, CDK2/cyclinA, CDK5/p25 and CDK9/cyclinT1, respectively. TMX-2138 promotes ubiquitination and degradation of CDKs. TMX-2138 can be used for the research of ovarian cancer (Pink: CDKs ligand (HY-151071); Blue: E3 ligase CRBN ligand (HY-14658); Black: linker (HY-W008352)).
    TMX-2138
  • HY-P5559
    ND1-YL2 2582803-80-1
    ND1-YL2 is a PROTAC that selectively degrades SRC-1 via the N-degron pathway. ND1-YL2 significantly inhibits cancer invasion and migration in vitro and in vivo. ND1-YL2 can be used in cancer research.
    ND1-YL2
  • HY-178825
    LD-110
    LD-110 is a highly efficient and effective PROTAC degrader targeting LSD1 (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 can be used for the study of esophagus squamous cancer. Red: LSD1 ligand (HY-178826); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-N2578).
    LD-110
  • HY-169279
    PROTAC SMARCA2/4-degrader-34
    PROTAC SMARCA2/4-degrader-34 (compound 38) is a potent is a potent SMARCA2 and SMARCA4 PROTAC degrader. PROTAC SMARCA2/4-degrader-34 shows PXR binding affinity with DC50 value of 85.1 nM. PROTAC SMARCA2/4-degrader-34 decreases the protein expression of 3xFLAG-PXR. (Pink: Ligand for target protein (HY-169280); Black: Linker (HY-43048); Blue: Ligand for E3 ligase (HY-125845).
    PROTAC SMARCA2/4-degrader-34
  • HY-159175
    XM-U-14 3098519-83-3
    XM-U-14 is a selective PROTAC USP7 Degrader (DC50: 0.74 nM in inducing USP7 degradation in RS4;11 cell line). XM-U-14 upregulates the levels of p53 and p21. XM-U-14 also significantly inhibits acute lymphoblastic leukemia (ALL) cell growth (IC50: 0.5 nM and 8.3 nM for RS4;11 cells and Reh cells respectively). XM-U-14 induces apoptosis and cycle arrest. XM-U-14 inhibits tumor growth. (Blue: VHL ligand (HY-159465), Black: linker (HY-W539783); Pink: USP7 inhibitor (HY-159464)).
    XM-U-14
  • HY-172562
    BTR2004
    BTR2004 is a selective BET family (BRD2/3/4) protein PROTAC degrader. BTR2004 forms a ternary complex with BRD proteins and KLHL20, inducing ubiquitination and proteasomal degradation through the UPS pathway. BTR2004 is promising for research of PC3 prostate cancer and MDA-MB-231 breast cancer cell lines. Pink: (+)-JQ1-OH (HY-161125); Blue: BTR2000 (HY-172563); Black: Linker (HY-W015236).
    BTR2004
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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