E1/E2/E3 Enzyme Ligand

CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The K_D values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC₅₀ against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma.

Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin can also bind to SKP2, with K_D = 67.9 μM. Hederagenin also has preventive potential against alcoholic liver injury.

HGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (K_a=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death.

dTAG-TRIMTAC is a PROTAC-like degrader targeting TRIM21. dTAG-TRIMTAC forms a ternary complex with TRIM21 and target proteins to drive degradation of oligomeric/assembled substrates via TRIM21 clustering-based activation, with degradation dependent on endogenous TRIM21. dTAG-TRIMTAC can be used for the research of neurodegenerative disease and inflammatory disease.

TRIM21 ligand-1 is a TRIM21 ligand. TRIM21 ligand-1 mediates the degradation of nuclear pore complex proteins GLE1 and NUP155. TRIM21 ligand-1 induces the disassembly of nuclear pore complexes, which in turn leads to cell death. TRIM21 ligand-1 can be used in cancer research.

PRC1 ligand 1 is a target protein ligand of MS147 (HY-160924). PRC1 ligand 1 can be used to study cancer.

EN10 is a ligand for the muscle-specific E3 ligase KLHL41, which can be used to synthesize PROTAC KBD-1 (HY-184151) targeting BRD4.

FITC-Acp-RpYTPEP-NH2 is a potent fluorescent tracer. FITC-Acp-RpYTPEP-NH2 shows a binding affinity (K_d = 0.07 μM) for the Cbl-b SH2 domain. Fluorescence polarization assay based on FITC-Acp-RpYTPEP-NH2 can be for evaluating Cbl-b SH2 domain inhibitors.

ZER1 binder-2 is a ZER1 E3 ubiquitin ligase binder with an EC₅₀ value of 51.04 nM. ZER1 binder-2 is applicable to the research of cancers induced by HPV infection.

ZER1 binder-1 is a pyridazinone derivative and a binding agent for the E3 ubiquitin ligase ZER1, with an FP EC₅₀ value of 55.59 nM. ZER1 binder-1 is applicable to the research of cancers induced by human papillomavirus (HPV) infection.

TRIM25 ligand-1 (Compound 10) is a covalent ligand. TRIM25 ligand-1 can covalently bind to Cys498 in the PRYSPRY domain of TRIM25 and enhance its auto-ubiquitination activity. TRIM25 ligand-1 is selective for TRIM25 in vitro and in live cells.

Tracer AL244 is a BODIPY-based fluorescent tracer and also a TRIM21 binder. Tracer AL244 enables evaluation of TRIM21 target binding in both intact and permeabilized cells.

ZER1 binder-3 is an E3 ubiquitin ligase ZER1-binding pyridazinone derivative with an FP EC₅₀ value of 56.61 nM. ZER1 binder-3 can be used for the research of cancers arising from infection by human papillomavirus (HPV).

PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a K_i value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease.