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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
49 Results for "
CRL4
" in MedChemExpress (MCE) Product Catalog:
Products (49)
49 Results for "CRL4" in MCE Product Catalog:
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20 Publications Verification
Research Areas:
CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer [4] .
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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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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) .
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5 Cited Publications
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dBET57 is a potent and selective BRD4BD1 PROTAC degrader with a DC50 of approximately 500 nM. dBET57 forms a ternary complex with CRL4 CRBN and BRD4BD1, induces the ubiquitination and degradation of BRD4, and indirectly inhibits the transcription of MYCN, c-Myc and PD-L1, ultimately leading to cell cycle arrest and apoptosis. dBET57 can be used in related research on neuroblastoma, non-small cell lung cancer and colorectal cancer [4].
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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 [4] .
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1 Cited Publications
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dCeMM2 (Compound 2) is a molecular glue-type degrader that targets cyclin K. dCeMM2 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
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1 Cited Publications
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KH-4-43 is an inhibitor of E3 CRL4. KH-4-43 inhibits E3 CRL4's core ligase complex and exhibits anticancer activity. KH-4-43 has a binding Kd to E3 ROC1-CUL4A CTD or the highly related ROC1-CUL1 CTD at 83 nM or 9.4 μM, respectively .
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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 [4].
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DCAF1 binder 1 is a selective for the CRL4 DCAF1 E3 ligase complex. DCAF1 binder 1 is a ligands for E3 Ligase, involving in targeted protein degradation (TPD) .
Cat. No.: HY-164891
CAS No.: 2839138-44-0
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EM12‑FS is a selective covalent molecular glue degrader of NTAQ1 that binds to CRBN with an IC50 of 256 nM. EM12‑FS covalently modifies the His353 residue of CRBN via chemical modification, reshapes the surface conformation of CRBN protein, selectively recruits NTAQ1 to form a ternary complex, and mediates the degradation of NTAQ1 protein in a CRL4 CRBN E3 ubiquitin-proteasome pathway-dependent manner. EM12‑FS can be used in cancer-related research .
Cat. No.: HY-W133627
CAS No.: 118719-16-7
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dCeMM1 is a molecular glue degrader that targets RBM39. dCeMM1 serves as a positive control for the screening of DCAF15-dependent molecular glue degraders. dCeMM1 promotes the DCAF15-RBM39 interaction, thereby recruiting RBM39 to the CRL4 DCAF15 E3 ubiquitin ligase complex, inducing ubiquitination and subsequent proteasomal degradation of RBM39. Meanwhile, dCeMM1 stabilizes DCAF15 by mediating neo-substrate recruitment to protect DCAF15 from autodegradation. dCeMM1 reduces the viability of leukemia cells in a neddylation-dependent and proteasome-dependent manner, and can be applied in leukemia-related research [4] .
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dCeMM4 is a Cyclin K Molecular glue degrader. dCeMM4 mediates the direct interaction between CDK12:cyclin K and the CRL4B ligase complex, thereby driving the ubiquitination and proteasomal degradation of Cyclin K. dCeMM4 induces Apoptosis without cell cycle phase-specific arrest. dCeMM4 exhibits synergistic activity with DNA damage inducers, and a correlation exists between Cyclin K degradation and cellular sensitivity. dCeMM4 can be used in studies related to T-cell malignancies .
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TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity .
MMH1 is a novel BRD4 molecular glue degrader. MMH1 functions by recruiting the CUL4 DCAF16 ligase to the second bromodomain of BRD4 (BRD4 BD2). MMH1 binds to the JQ1-binding site of BRD4 BD2, acts as a template to covalently modify Cys58 of DCAF16, stabilizes the BRD4-DCAF16 ternary complex, and thereby promotes BRD4 degradation via the CRL4DCAF16 ubiquitin ligase pathway. Using BRD4 BD2 as a structural template, MMH1 covalently modifies Cys87 of GAK and induces the GAK-BRD4 BD2 interaction. Through its covalent mechanism, MMH1 exhibits sustained BRD4 degradation activity, and shows selective degradation activity for BRD4 BD2 over BRD4 BD1 .
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dCeMM3 (Compound 3) is a molecular glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
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SR-1114 is a ENL PROTAC degrader, with DC50 values of 150 nM, 311 nM and 1.65 μM in MV4;11, MOLM-13 and OCI/AML-2 cells, respectively. SR-1114 has an IC50 of 155 nM against the human CRL4CRBN complex. SR-1114 can be used in research related to acute leukemia and acute myeloid leukemia .
Cat. No.: HY-173614
CAS No.: 1061605-35-3
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CC-647 is a molecular glue-type cereblon modulator and ZBTB16 degrader. CC-647 primarily utilizes the C2H2 ZnF3 degron of ZBTB16 to promote CRL4 CRBN-mediated ubiquitination and proteasomal degradation. CC-647 also induces the degradation of the oncogenic RARα-ZBTB16 fusion protein, while exerting a weaker degrading effect on the reciprocal fusion ZBTB16-RARα. CC-647 can be used in studies related to targeted protein degradation and ZBTB16/RARA-rearranged acute promyelocytic leukemia .
Cat. No.: HY-172770
CAS No.: 3113750-79-8
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KMG-1068 is a molecular glue degrader that induces proteasomal degradation of GSPT1 and GSPT2 with DC50 values of 126.7 nM and 42.2 nM, respectively. KMG-1068 binds to the C-terminal IMiD-binding site of CRBN, forms ternary complexes with GSPT1 and GSPT2, and mediates proteasomal degradation of target proteins via the CRL4 ubiquitination pathway. KMG-1068 is applicable to research related to acute myeloid leukemia .
Cat. No.: HY-177780
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Cyclin K degrader 2 is a molecular glue degrader of Cyclin K. By bridging CDK12 and DDB1, the receptor of the CRL4 E3 ligase, Cyclin K degrader 2 specifically induces the targeted degradation of Cyclin K within the CDK12-Cyclin K complex. Cyclin K degrader 2 can be used in studies related to acute myeloid leukemia .
Cat. No.: HY-175334
CAS No.: 2920443-08-7
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DHC-286 is a molecular glue degrader targeting GSPT1. DHC-286 recruits GSPT1 to the CRL4CRBN ubiquitin ligase complex, promoting GSPT1 ubiquitination and proteasomal degradation, inducing cytotoxicity. DHC-286 is promising for research of cancers such as acute myeloid leukemia .
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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
