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 (105):

Cat. No. Product Name Effect Purity
  • HY-130800
    Eragidomide Modulator 99.76%
    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-101291
    Iberdomide 98.84%
    Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities[1][2].
  • 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 99.23%
    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.
  • HY-A0003
    Lenalidomide 99.91%
    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-148834
    Pomalidomide-piperazine
    Pomalidomide-piperazine is an active compound that can be used to synthesis the E3 ligand for PROTAC[1].
  • HY-14658
    Thalidomide 99.91%
    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-152231
    BODIPY FL thalidomide
    BODIPY FL thalidomide is a high-affinity fluorescent probe for the human cereblon protein with a Kd value of 3.6 nM[1]
  • 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 98.13%
    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
    ALV1 potently induces degradation of both Ikaros and Helios without unexpected off-target activity. ALV1 binds CRBN with IC50 of 0.55 µM. ALV1 degrades cells stably expressing IKZF1Δ and IKZF2Δ GFP fusions with mCherry reporter with DC50s of 2.5 and 10.3 nM[1].
  • HY-125845
    (S,R,S)-AHPC 98.92%
    (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-A0003B
    Lenalidomide hemihydrate 99.67%
    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-W077589A
    Lenalidomide-5-aminomethyl
    Lenalidomide-5-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC[1].
  • HY-W087383
    Thalidomide 5-fluoride 99.85%
    Thalidomide 5-fluoride is Thalidomide-based cereblon ligand that incorporates to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
  • HY-103597
    Thalidomide-O-COOH 99.73%
    Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs[1].
  • HY-139546
    Thalidomide-5-propargyne-NH2 hydrochloride
    Thalidomide-5-propargyne-NH2 hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-propargyne-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].
  • HY-128806
    E3 ligase Ligand 9
    E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
  • HY-103596
    Thalidomide-4-OH
    Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs[1].