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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
68 Results for "
Cullin
" in MedChemExpress (MCE) Product Catalog:
Products (68)
68 Results for "Cullin" in MCE Product Catalog:
Cat. No.: HY-10484R
CAS No.: 1160295-21-5
Synonyms: MLN4924 hydrochloride (Standard)
Research Areas:
Pevonedistat hydrochloride (Standard) is the analytical standard of Pevonedistat hydrochloride (HY-10484). This product is intended for research and analytical applications. Pevonedistat (MLN4924) hydrochloride is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM. Pevonedistat hydrochloride induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat hydrochloride suppresses the growth of human tumour xenografts in mice .
Cat. No.: HY-189074
Research Areas:
JN210 is a dual inhibitor of DCN1 and HDAC, with an IC50 of 94.26 nM against human DCN1. JN210 disrupts the UBE2M-DCN1 protein-protein interaction, blocks the neddylation modification of cullin-RING ligases, inhibits HDAC activity and induces histone hyperacetylation. JN210 impairs DNA damage repair function, induces cell apoptosis, exerts cytotoxicity and inhibits tumor growth. JN210 can be used for the research of non-small cell lung cancer .
Cat. No.: HY-187338
Target:
Research Areas:
CRBN ligand-908 is a cereblon (CRBN) ligand and also a HaloTag-binding degrader. CRBN ligand-908 competes with fluorescent lenalidomide ligands for binding to full-length CRBN protein. CRBN ligand-908 contains a chlorohexyl group that covalently reacts with HaloTag fused to target proteins. CRBN ligand-908 induces degradation of HaloTag-fused FAK, endogenous MARC1, and BRD4 proteins. CRBN ligand-908 is a proteasome- and Cullin-dependent degrader. CRBN ligand-908 does not induce degradation of the novel CRBN substrates GSPT1, SALL4, or CSNK1α. CRBN ligand-908 can be used to synthesize PROTACs, such as HaloPROTAC 4 (HY-187337) .
Cat. No.: HY-182945
Research Areas:
IKZF2-degrader 5 is a highly efficient, highly selective, rapidly acting, and orally active IKZF2 molecular glue degrader. IKZF2-degrader 5 induces IKZF2 degradation via the Cullin-CRBN-dependent pathway. IKZF2-degrader 5 promotes the production of pro-inflammatory IL-2. IKZF2-degrader 5 attenuates the immunosuppressive function of regulatory T cells (Tregs). IKZF2-degrader 5 triggers rapid, significant, and sustained IKZF2 degradation in the spleen and thymus of mice. IKZF2-degrader 5 inhibits tumor growth. IKZF2-degrader 5 can be used for the research of B16F melanoma .
Cat. No.: HY-P701587
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: KLHL42; Cullin-3-Binding Protein 9; Prev. KLHDC5; KIAA1340; Ctb9; Kelch Domain Containing 5; Kelch Domain-Containing Protein 5; Kelch Like Family Member 42; Kelch-Like Protein 42
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P701588
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: KLHL42; Cullin-3-Binding Protein 9; Prev. KLHDC5; KIAA1340; Ctb9; Kelch Domain Containing 5; Kelch Domain-Containing Protein 5; Kelch Like Family Member 42; Kelch-Like Protein 42
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-L128
187 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.
Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).
MCE carefully prepared a unique collection of 187 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.
Cat. No.: HY-187396
Target:
Research Areas:
FD1-C10-CB is a PROTAC degrader targeting the BRD4 protein. FD1-C10-CB binds to FEM1B to form a ternary complex with BRD4, achieving FEM1B-dependent degradation of BRD4 via the ubiquitin-proteasome system. FD1-C10-CB binds to CD36 to mediate endocytic cellular delivery, thereby enhancing its degrading activity. FD1-C10-CB mediates protein degradation through the Cullin-dependent ubiquitin-proteasome pathway, rather than the lysosomal autophagy pathway. FD1-C10-CB induces a decrease in BRD4 protein levels, and its degrading activity is competitively inhibited by FL47 or JQ1. FD1-C10-CB can be used in the research of breast cancer and osteosarcoma .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
