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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
15 Results for "
CRBN/DDB1 complex
" in MedChemExpress (MCE) Product Catalog:
Products (15)
15 Results for "CRBN/DDB1 complex" 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.
4
Research Areas:
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
Target:
Research Areas:
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 .
Cat. No.: HY-172113
H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM. H122 exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki values of 2.0, 3.6 and 1.6 nM, respectively. H122 relies on binding to TEAD1 and CRBN, functional E3 ligase activity, and a functional proteasome for degradation.H122 induces degradation of TEAD3 and forms a ternary complex with TEAD4 and CRBN/DDB1 to mediate degradation.H122 downregulates expression of Myc target genes. H122 exhibits antitumor efficacy in MSTO-211H mouse xenograft models.H122 can be used for the research of malignant mesothelioma .
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Research Areas:
SJ995973 is a BRD4 PROTAC degrader with DC50 values of 0.87 nM (12 h) and 0.16 nM (24 h), respectively. SJ995973 induces the formation of a ternary complex between purified BRD4 and CRBN-DDB1 proteins, with an IC50 of 17 nM against CRBN. SJ995973 inhibits the viability of human acute myeloid leukemia cells. SJ995973 can be used in studies related to acute myeloid leukemia and medulloblastoma .
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-170900
Research Areas:
SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC50 = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma .
Cat. No.: HY-177559
CAS No.: 3037413-54-7
Research Areas:
NEK7 degrader-2 is a NEK7 molecular glue degrader that promotes the formation of the NEK7-compound-CRBN/DDB1 ternary complex. NEK7 degrader-2 reduces the release of IL-1β after NLRP3 inflammasome activation induced by LPS (HY-D1056). NEK7 degrader-2 can be applied in studies related to NEK7-dependent NLRP3 inflammasome activation and inflammatory responses .
Cat. No.: HY-175280
CAS No.: 3095033-62-5
Research Areas:
Lck degrader-1 is a molecular glue degrader that recruits cereblon to target LCK and CK1α. Lck degrader-1 promotes the formation of the LCK/CRBN-DDB1 ternary complex with an EC50 of 77.1 nM, and induces the degradation of LCK and CK1α. LCK degradation induced by Lck degrader-1 depends on the G415-containing helical G-loop degron, and maintains LCK-degrading activity in cells with the LCK T316I gatekeeper mutation. Lck degrader-1 can be used for research related to T-cell acute lymphoblastic leukemia (T-ALL) and LCK inhibitor resistance .
Cat. No.: HY-D3392
Thalidomide-cyanine 5 is a fluorescent probe prepared by conjugating the CRBN binder Thalidomide (HY-14658) with the near-infrared fluorescent dye Cy5. Thalidomide-cyanine 5 binds to DDB1-CRBN protein complex with a Kd of 121.6 nM. Thalidomide-cyanine 5 binds to CRBN to form a binary complex, and is mainly used for the visual tracking research of degradants such as PROTAC (Ex/Em = 650/665 nm) .
Cat. No.: HY-188006
CAS No.: 3052938-18-5
Research Areas:
GSPT1 degrader-18 is a GSPT1 degrader that inhibits the proliferation of cancer cells. GSPT1 degrader-18 has weak ability to induce the formation of the GSPT1-CRBN/DDB1 ternary complex and belongs to a weak molecular glue. GSPT1 degrader-18 can be used in cancer-related research .
Cat. No.: HY-P702817
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; DDB1; XPE-BF; Damage Specific DNA Binding Protein 1; XAP-1; DNA Damage-Binding Protein 1; XAP1; Xeroderma Pigmentosum Group E-
Species:
Human
Source:
HEK293
Cat. No.: HY-P702826
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; DDB1; XPE-BF; Damage Specific DNA Binding Protein 1; XAP-1; DNA Damage-Binding Protein 1; XAP1; Xeroderma Pigmentosum Group E-
Species:
Human
Source:
Sf9 insect cells
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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
