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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
44 Results for "
human cereblon
" in MedChemExpress (MCE) Product Catalog:
Products (44)
44 Results for "human cereblon" in MCE Product Catalog:
8
8 Publications Verification
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MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC50 values of 4.5 nM and 31 nM against wild-type BTK and BTK C481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies .
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1 Cited Publications
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ARD-1676 is an orally active androgen receptor (AR) PROTAC degrader . ARD-1676 induces proteasomal degradation of AR, inhibits AR-regulated gene expression, suppresses cell growth, reduces AR protein levels and inhibits tumor growth in in vivo models. ARD-1676 can be used in studies related to AR+ human prostate cancer and spinal bulbar muscular atrophy .
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1 Cited Publications
Cat. No.: HY-P702820
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: CRBN; MRT2; Prev. MRT2A; Protein X 0001; Protein cereblon; cereblon; Mental Retardation, Non-Syndromic, Autosomal Recessive, 2A
Cat. No.: HY-169179
CAS No.: 2984505-88-4
AK-1690 is a selective PROTAC degrader targeting STAT6 (DC50=1 nM) with a Ki of 6 nM against human STAT6. AK-1690 degrades STAT6 via the interaction of STAT6 with cereblon and a ubiquitin-like process. AK-1690 effectively depletes STAT6 protein in mouse liver and lung tissues, and is applicable to research related to leukemia, Hodgkin's lymphoma, follicular lymphoma, etc. .
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BODIPY FL thalidomide is a high-affinity and selective human cereblon (CRBN)-targeting fluorescent probe with a Kd of 3.6 nM. BODIPY FL thalidomide enables use as a probe in time-resolved fluorescence resonance energy transfer (TR-FRET) binding assays for cereblon ligands. BODIPY FL thalidomide supports development of highly sensitive, selective, stable cereblon TR-FRET binding assays (Ex/Em = 502/510 nm) .
Cat. No.: HY-159098
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dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease .
Cat. No.: HY-148837
CAS No.: 2883535-99-5
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GT19630 is an orally active c-Myc PROTAC targeted degrader based on the cereblon E3 ubiquitin ligase, with an IC50 of 1.5 nM against human c-Myc. GT19630 mediates the degradation of MYC, GSPT1, GSPT2, CK1 alpha, N-Myc, B7-H3 and XIAP, and disrupts the MYC-GSPT1 synergistic regulatory feedback loop. GT19630 inhibits cell proliferation, blocks S-phase progression of the cell cycle, promotes cell apoptosis, reduces cell migration capacity, induces integrated stress response, and blocks oxidative phosphorylation by inhibiting the TCA cycle. GT19630 can be used in the research of Myc-driven hematological cancers, small cell lung cancer, breast cancer, TP53-mutant cancers, and venetoclax-resistant cancers .
Cat. No.: HY-173679
CAS No.: 2569517-30-0
RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD + site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC50=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections .
Cat. No.: HY-164891
CAS No.: 2839138-44-0
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EM12-FS is a cereblon (CRBN) ligand that binds CRBN at His353 and a molecular glue degrader of NTAQ1. EM12-FS has a human plasma half-life of 196 min .
Cat. No.: HY-153932
CAS No.: 2550399-06-7
NR-7h is a selective p38α/p38β MAPK PROTAC degrader with multiple activities including anti-leishmanial, anti-malarial, and anti-Mayaro virus properties. NR-7h induces specific degradation of p38α/p38β isoforms and p38-MAPK via the ubiquitin-proteasome system. NR-7h reduces the load of Leishmania donovani, modulates the cytokine profile toward a pro-inflammatory phenotype, and enhances the oxidative burst of macrophages. NR-7h inhibits the growth of Plasmodium falciparum in human red blood cells and merozoite invasion. NR-7h reduces the replication of Mayaro virus and the expression of E1 protein in primary human dermal fibroblasts. NR-7h can be used in studies related to parasitic infections, viral infections, and breast cancer .
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Thalidomide-piperazine hydrochloride is a synthetic E3 ligase ligand-linker conjugate, containing a cereblon ligand based on Thalidomide (HY-14658) and one linker. Thalidomide-piperazine hydrochloride can be used in studies related to PROTAC synthesis .
Cat. No.: HY-153220A
CAS No.: 3024312-52-2
Synonyms: (R)-NX-2127
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(R)-Zelebrudomide ((R)-NX-2127) is an isomer of Zelebrudomide (HY-153220). Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC50 values of 4.5 nM and 31 nM against wild-type BTK and BTK C481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies .
Cat. No.: HY-173066
CAS No.: 3048196-52-4
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NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer .
Cat. No.: HY-163564
CAS No.: 3117543-71-9
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JYQ-194 is a PROTAC degrader that selectively induces PARK7 degradation by recruiting cereblon. JYQ-194 induces proteasome-dependent degradation of PARK7 in human tumor cells. JYQ-194 is applicable to research related to Parkinson's disease and cancer .
Cat. No.: HY-163168
CAS No.: 2412985-00-1
Synonyms: CFT-4531
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aTAG 4531 (CFT-4531) is a PROTAC-class degrader that induces the degradation of the MTH1/aTAG fusion protein by recruiting cereblon, with a DC50 of 0.28 nM in Jurkat cells. aTAG 4531 inhibits MTH1 enzymatic activity, with a Ki of 1.8 nM. aTAG 4531 rapidly, selectively and reversibly regulates SMART-CAR protein levels, CAR-mediated target cell killing and IL-2 release, and is applicable both in vitro and in vivo. aTAG 4531 can be used in studies of targeted protein degradation, target validation and CAR-T activity regulation .
Cat. No.: HY-170598
CAS No.: 3119106-17-8
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HP211206 is a bifunctional CRBN-recruiting SARS-CoV-2 M pro PROTAC degrader with a CRBN IC50 of 3.2 μM and a SARS-CoV-2 M pro DC50 of 621 nM. HP211206 recruits E3 ubiquitin ligase CRBN to drive ubiquitination and proteasomal degradation of wild-type SARS-CoV-2 M pro and E166 mutant while inhibiting M pro enzymatic activity, exhibits no cytotoxicity against normal mammalian cells at tested concentrations, and can be used for the study of COVID-19 and SARS-CoV-2 infection
Cat. No.: HY-170448
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PROTAC AR Degrader-9 is a topically applicable androgen receptor (AR) PROTAC degrader. PROTAC AR Degrader-9 recruits Cereblon (CRBN) E3 ubiquitin ligase to induce AR ubiquitination and proteasomal degradation in human dermal papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 possesses excellent skin retention, modulates androgenetic alopecia (AGA)-related downstream paracrine factors including TGF-β1 and β-catenin, promotes hair regeneration in mice. and exhibits favorable skin pharmacokinetics profiles with minimal systemic exposure. PROTAC AR Degrader-9 can be used for the study of androgenetic alopecia (AGA) .
Cat. No.: HY-173372
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PROTAC AR Degrader-10 is a potent cereblon (CRBN)-recruited androgen receptor (AR) PROTAC degrader. PROTAC AR Degrader-10 exhibits high AR degradation activity and can be applied to research related to prostate cancer .
Cat. No.: HY-169367
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ERD-1233 is an orally active ERα PROTAC degrader with a DC50 of 0.9 nM. ERD-1233 exhibits plasma stability and microsomal stability across multiple species, and shows no significant inhibitory effect on major cytochrome P450 subtypes and hERG channels. ERD-1233 inhibits tumor growth and degrades ERα protein levels in xenograft tumor models, with favorable biosafety. ERD-1233 can be used in breast cancer-related research .
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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
