2. PROTAC
  3. Ligands for E3 Ligase

Ligands for E3 Ligase

A PROTAC (Proteolysis Targeting Chimeric Molecule) is a protein degrader comprised of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand for target protein (target binder). The association between an E3 ligase and a target protein induced by a PROTAC will lead to the transfer of ubiquitin and degradation of the targeted protein.

E3 ligases catalyze the transfer of ubiquitin to targeted proteins and determine the specificity of the proteins. There are hundreds of E3 ligases in cells, but only a limited number of them are successfully used in reported PROTACs, such as VHL (von Hippel-Lindau disease tumor suppressor protein), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue) and IAP (inhibitor of apoptosis).

Ligands for E3 Ligase Related Products (349):

Cat. No. Product Name Effect Purity
  • HY-130800
    Eragidomide Modulator 99.86%
    Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation[1][2].
  • HY-14658
    Thalidomide
    Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
  • HY-10984
    Pomalidomide
    Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
  • HY-101488
    CC-885 99.85%
    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity. CC-885 is also a known degrader of GSPT1, inhibiting protein translation.
  • HY-A0003
    Lenalidomide
    Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
  • HY-173627
    (R,S,S)-VH032-Me
    (R,S,S)-VH032-Me is a ligand for E3 ubiquitin ligase. (R,S,S)-VH032-Me can be connected to the ligand for protein by a linker to form dTAGV-1-NEG (HY-145514A). PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
  • HY-172563
    BTR2000
    BTR2000, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562)[1].
  • HY-176036
    MS1262
    MS1262 is the E3 ubiquitin ligase ligand of MS1262-C3-amide-C10-amine (HY-176035). MS1262 can be used to synthesize PROTACs[1].
  • HY-W898983
    CRBN ligand-181
    CRBN ligand-181 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
  • HY-41547
    Thalidomide 4-fluoride
    Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966)[1].
  • HY-123215
    CC-17369 98.68%
    CC-17369 (7-Hydroxy pomalidomide) is a metabolite of Pomalidomide. CC-17369 is the Pomalidomide -based cereblon (CRBN) ligand used in the recruitment of CRBN protein. CC-17369 can be connected to the ligand for protein by a linker to form PROTAC[1].
  • HY-10984S2
    Pomalidomide-d4
    Pomalidomide-d4 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<
  • HY-145776
    ALV1 98.62%
    ALV1 is a molecular glue degrader for Ikaros (IKZF1) and Helios (IKZF2), with DC50 values of 2.5 nM and 10.3 nM, respectively. ALV1 binds CRBN with an IC50 of 0.55 µM. ALV1 induces CRBN-Helios dimerization. ALV1 can be used to study the properties and functions of Treg cells[1].
  • HY-161185
    Thalidomide-piperidine-O-azetidine-boc
    Thalidomide-piperidine-O-azetidine-boc is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
  • HY-125845
    (S,R,S)-AHPC
    (S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells[1].
  • HY-W382038
    E3 ligase Ligand 32
    E3 ligase Ligand 32 (First product in Example 52) is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 32 can be connected to the ligand for protein by a linker to form PROTACs and can be used for the synthesis of PROTAC SMARCA2/4-degrader-29 (HY-162743)[1].
  • HY-W460193
    N-Me-Thalidomide 4-fluoride 99.41%
    N-Me-Thalidomide 4-fluoride is a ligand for E3 ligase, used for the synthesis of Anti-inflammatory agent 70 (HY-157570)[1].
  • HY-157758
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3 is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker . (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3 can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
  • HY-A0003B
    Lenalidomide hemihydrate 99.98%
    Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
  • HY-153215
    MEL24
    MEL24 is an Mdm2 E3 ligase inhibitor that reduces cell survival and increases sensitivity to DNA damaging agents in a p53-dependent manner for in vitro antitumor studies[1].