2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. E1/E2/E3 Enzyme
  5. E1/E2/E3 Enzyme Degrader

E1/E2/E3 Enzyme Degrader

E1/E2/E3 Enzyme Degraders (11):

Cat. No. Product Name Effect Purity
  • HY-180538
    MRT-31619
    		Degrader
    MRT-31619 is a molecular gel degrader (MGD) targeting CRBN. MRT-31619 drives the self-dimerization of the E3 ligase by mimicking the degradation subunit, and promotes its rapid, effective and selective degradation through the ubiquitin-proteasome system.
  • HY-W1128879
    XMU-MP-8
    		Degrader 99.23%
    XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncoprotein SKP2. XMU-MP-8 simultaneously binds to the F-box domain of SKP2 (Kd ≈ 36 μM) and the N-terminal TPR domain of the E3 ligase STUB1 (Kd ≈ 2.5 μM), forming a stable SKP2-SKPer1-STUB1 ternary complex (Kd ≈ 8.9 nM) that induces SKP2 ubiquitination and proteasomal degradation. XMU-MP-8 selectively eliminates SKP2-expressing cancer cells. XMU-MP-8 exhibits substantial tumour suppression with good safety profiles in vivo. XMU-MP-8 can be used for cancer research, such as non-small cell lung adenocarcinoma (NSCLC) and prostatic adenocarcinoma.
  • HY-136262
    CRBN-6-5-5-VHL
    		Degrader 99.45%
    CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3. (Pink: VHL ligand (HY-125845); Blue: E3 Ligase ligand (HY-10984); Black: linker (HY-403544)).
  • HY-128845
    PROTAC CRBN Degrader-1
    		Degrader 98.77%
    PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other. (Blue: VHL ligand (S,R,S)-AHPC (HY-125845); Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846); Black: Linker (HY-128847))
  • HY-167673
    RNF5-IN-1
    		Degrader 98.52%
    RNF5-IN-1 (FX12) is a selective RNF5 degrader. RNF5-IN-1 binds to RNF5 and inhibits its E3 activity, and promotes proteasomal degradation of RNF5 in an endoplasmic reticulum (ER)-associated degradation (ERAD) way in cells. RNF5-IN-1 inhibits α-1-antitrypsin (NHK) dislocation with an IC50 value of 2.7 μM. RNF5-IN-1 can be used for research of cystic fibrosis, acute myeloid leukemia, and certain viral infections.
  • HY-181692
    PROTAC RNF4 degrader-1
    		Degrader
    PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (Kd = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma.
  • HY-181653
    PROTAC SKP2 Degrader-1
    		Degrader
    PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research.
  • HY-159615
    Cbl-b-IN-21
    		Degrader
    Cbl-b-IN-21 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Cbl-b-IN-21 can be used for synthesis PROTAC Cbl-b-IN-1 (HY-159608).
  • HY-159608
    PROTAC Cbl-b-IN-1
    		Degrader
    PROTAC Cbl-b-IN-1 (compound 64) is a potent Cbl-b PROTAC degrader with a DC50 of less than 30 nM. PROTAC Cbl-b-IN-1 can be used for cancer research.
  • HY-W854844B
    JP-2-196 hydrochloride
    		Degrader
    JP-2-196 hydrochloride is a covalent molecular glue degrader targeting RNF126. JP-2-196 hydrochloride induces the formation of a ternary complex between RNF126 and target proteins (e.g., BRD4, AR-V7), promoting their ubiquitination and proteasomal degradation. JP-2-196 hydrochloride is promising for research of cancers (e.g., prostate cancer, leukemia).
  • HY-N18301
    Americanin A
    		Degrader
    Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer.