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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
13 Results for "
E3 ligase CRL4CRBN
" in MedChemExpress (MCE) Product Catalog:
Products (13)
13 Results for "E3 ligase CRL4CRBN" in MCE Product Catalog:
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Research Areas:
Eragidomide (CC-90009) is a GSPT1 Molecular Glue degrader. Eragidomide exhibits antiproliferative and pro-apoptotic (apoptosis) activities against acute myeloid leukemia cells. Eragidomide recruits the CRL4CRBN E3 ubiquitin ligase complex to selectively target GSPT1 for ubiquitination and proteasomal degradation. Eragidomide reduces leukemia cell engraftment and eliminates leukemia stem cells. Eragidomide promotes the activation of the GCN1/GCN2/ATF4 pathway and the integrated stress response pathway, inhibits global protein translation, promotes preferential translation of ATF4, and induces the accumulation of ATF4, CHOP and ATF3. The response to Eragidomide is regulated by the ILF2/ILF3 heterodimer complex, the mTOR signaling pathway and the integrated stress response. Eragidomide can be used in research related to acute myeloid leukemia and relapsed/refractory acute myeloid leukemia .
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3 Cited Publications
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ZXH-3-26 is a CRBN-recruiting BRD4 PROTAC degrader with a DC50/5h of approximately 5 nM. ZXH-3-26 drives the ubiquitination and degradation of BRD4 by recruiting BRD4BD1 to the CRL4 CRBN E3 ubiquitin ligase complex, thereby inhibiting the dynamic distribution of super-enhancers. ZXH-3-26 reverses TNF-α-induced impairment of the immunosuppressive function of mesenchymal stem cells, and affects RNA synthesis and the transcriptional elongation process of Pol II. ZXH-3-26 can be used in studies related to inflammatory arthritis, malignant tumors, and HIV latency .
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Molecular Glues IKZF Family Casein Kinase Phosphodiesterase (PDE) MDM-2/p53 NF-κB Interleukin Related Apoptosis
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FPFT-2216 is an orally active Molecular glue degrader targeting IKZF1, IKZF3, CK-1α, and PDE6D, with a DC50 of 8 nM against PDE6D. FPFT-2216 mediates ubiquitin-proteasome degradation via the CRL4 CRBN E3 ubiquitin ligase complex and interacts with the non-isoprenoid-binding region of PDE6D. FPFT-2216 activates the p53 signaling pathway, inhibits the CBM complex/NF-κB pathway, upregulates IL-2, suppresses IL-1β and IL-6, and induces tumor cell Apoptosis. FPFT-2216 exhibits anticancer activity against multiple myeloma and lymphoma. FPFT-2216 can be used in research related to multiple myeloma, lymphoma, acute lymphoblastic leukemia, acute myeloid leukemia, pancreatic ductal adenocarcinoma, non-small cell lung cancer, and gastric adenocarcinoma .
Cat. No.: HY-178700
CAS No.: 2744249-11-2
ALV-05-151-02 is a BCL6B zinc finger protein degrader that selectively targets BCL6B over BCL6. ALV-05-151-02 redirects the E3 ubiquitin ligase CRL4CRBN to induce BCL6B degradation and interacts with the H357 residue of BCL6B .
Cat. No.: HY-177694
CAS No.: 2798907-41-0
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PROTAC AR Degrader-11 is a PROTAC degrader that targets the androgen receptor (AR) and its splice variant AR-V7. PROTAC AR Degrader-11 simultaneously degrades full-length AR and AR-V7 via the ubiquitin-proteasome system by recruiting the CRL4-CRBN E3 ligase (FIG.2A). PROTAC AR Degrader-11 reduces the viability of cancer cells. PROTAC AR Degrader-11 can be used in studies related to castration-resistant prostate cancer .
Cat. No.: HY-W1128213
CAS No.: 2983841-00-3
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IKZF2-degrader 2 is a selective and orally active IKZF2 molecular glue degrader with DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS. The IKZF2-degrader 2 mediates the ubiquitination and degradation of target proteins by recruiting the CRL4-CRBN E3 ubiquitin ligase. IKZF2-degrader 2 displays moderate degradation against SALL4 with a DC50 of 9 nM but does not induce any significant degradation towards IKZF1, IKZF3, CK1α and GSPT1. IKZF2-degrader 2 can be used for the study of cancer immunology .
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XY-06-007 is a mutation-selective PROTAC degrader targeting BRD4BD1L94V, with a DC50, 6 h of 10.2 nM in Flp293T cells. XY-06-007 recruits the E3 ligase CRL4CRBN to BRD4BD1L94V, triggering ubiquitination and proteasomal degradation. XY-06-007 can be combined with the dTAG strategy to achieve degrader-mediated synchronous depletion of the corresponding protein fusion in cells. XY-06-007 is applicable for cancer research .
Cat. No.: HY-177730
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PROTAC BRD4 Degrader-40 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-40 binds to Cereblon and recruits the CRL4 CRBN E3 ubiquitin ligase complex, mediates BRD4 degradation via the ubiquitin-proteasome pathway, and does not induce the degradation of classic CRBN neo-substrates IKZF1 and IKZF3. PROTAC BRD4 Degrader-40 induces BRD4 degradation in cancer cells. PROTAC BRD4 Degrader-40 can be used in research related to diffuse large B-cell lymphoma and acute myeloid leukemia .
Cat. No.: HY-183117
CAS No.: 3084635-77-5
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NEO-811 is a selective and orally active ARNT (HIF-1β) molecular glue degrader. NEO-811 is mediated by CRL4-CRBN E3 ligase for ARNT degradation. NEO-811 can be used for the study of clear cell renal cell carcinoma (ccRCC) .
Cat. No.: HY-183892
CAS No.: 2690350-15-1
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d9A1-2 is a potent SLC9A1 PROTAC degrader. d9A1-2 binds to SLC9A1 via the d9A1 warhead, recruits the CRL4CRBN E3 ubiquitin ligase through EBM, and thereby induces ubiquitination and proteasomal degradation of SLC9A1. d9A1-2 can be used for research on cancers such as acute myeloid leukemia .
Cat. No.: HY-184913
JHK-02-102-1 is a selective CDK5 degrader derived from the regorafenib kinase inhibitor scaffold. JHK-02-102-1 recruits CRL4CRBN E3 ubiquitin ligase to induce ternary complex formation between CDK5 and CRBN, triggering ubiquitin-proteasome system-dependent degradation. JHK-02-102-1 achieves selectivity redirection from CDK6 to CDK5 via subtle PROTAC architecture modifications .
Cat. No.: HY-130800R
CAS No.: 1860875-51-9
Synonyms: CC-90009 (Standard)
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Eragidomide (Standard) is the analytical standard of Eragidomide (HY-130800). This product is intended for research and analytical applications. Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4 CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation .
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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
