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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
10 Results for "
RBX1 Inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (10)
10 Results for "RBX1 Inhibitor" in MCE Product Catalog:
27
Research Areas:
Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
5
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E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a molecular glue that induces the targeted degradation of splicing factor RBM39 by recruiting the E3 ubiquitin ligase CUL4-RBX1-DDB1-DCAF15 (CRL4 DCAF15). E7820 is an angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. E7820 can be used for the study of acute myeloid leukemia (AML) .
5
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BETd-260 (ZBC 260) is a BET PROTAC degrader. BETd-260 recruits BRD2, BRD3, and BRD4 to the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex, driving cereblon-, proteasome-, and NEDD8-activating enzyme-dependent ubiquitination and degradation, with a DC50 of approximately 30-100 pM in RS4;11 cells. BETd-260 induces cancer cell apoptosis via endogenous signaling pathways, regulates the expression of the Bcl-2 family, inhibits the oncogene c-Myc, and reduces cell viability. BETd-260 suppresses tumor growth in mouse xenograft models with good biosafety. BETd-260 can be used in research related to acute leukemia, hepatocellular carcinoma, osteosarcoma, and triple-negative breast cancer .
2
2 Cited Publications
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BETd-246 is a BRD2/3/4 PROTAC degrader targeting the BET family. BETd-246 induces ubiquitination and proteasomal degradation of BRD2, BRD3 and BRD4 by recruiting the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex; it also inhibits TRAT1 expression and depletes BET proteins. BETd-246 suppresses cancer cell proliferation and invasion, disrupts the cell cycle and induces apoptosis. BETd-246 is applicable to research related to triple-negative breast cancer and T-cell acute lymphoblastic leukemia .
Research Areas:
Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
Cat. No.: HY-14658S
CAS No.: 1219177-18-0
Cat. No.: HY-182063
CAS No.: 2419496-02-7
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Z226407860 is a RING-box protein 1 (RBX1) inhibitor. Z226407860 reduces house dust mite-induced airway epithelial injury and ROS accumulation by inhibiting RBX1. Z226407860 can be used for the research of asthma .
Cat. No.: HY-190178
CAS No.: 2034581-68-3
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Glue02 is a CCNK molecular glue degrader with a DC50 < 0.1 μM. Glue02 binds to the kinase domain of CDK12, promotes the formation of a ternary complex between CDK12 and the DDB1-CUL4-RBX1 E3 ubiquitin ligase complex, converts CDK12 into a substrate-specific receptor, and induces polyubiquitination and proteasomal degradation of CCNK. Glue02 inhibits cancer cell proliferation. Glue02 can be used in cancer-related research .
Cat. No.: HY-190177
CAS No.: 2750644-44-9
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Glue02-35 is a CCNK molecular glue degrader with a DC50 < 0.1 μM. Glue02-35 binds to the kinase domain of CDK12, promotes the formation of a ternary complex between CDK12 and the DDB1-CUL4-RBX1 E3 ubiquitin ligase complex, and converts CDK12 into a substrate-specific receptor, inducing polyubiquitination and proteasomal degradation of CCNK. Glue02-35 inhibits cancer cell proliferation. Glue02-35 can be used for cancer-related research .
Cat. No.: HY-190210
CAS No.: 294647-05-5
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Cyclin K degrader 3 is a potent and selective cyclin K molecular glue degrader with a DC50 of 24 nM. Cyclin K degrader 3 is a CDK inhibitor with IC50 values of 86, 44, and 172 nM against CDK2/9/12, respectively.Cyclin K degrader 3 binds to the CDK12-cyclin K complex and recruits the DDB1-CUL4-RBX1 E3 ubiquitin ligase, thereby triggering ubiquitination and degradation of cyclin K. Cyclin K degrader 3 can be used for research on triple-negative breast cancer .
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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
