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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
11 Results for "
neosubstrate
" in MedChemExpress (MCE) Product Catalog:
Products (11)
11 Results for "neosubstrate" in MCE Product Catalog:
4
4 Cited Publications
Synonyms: NX-5948; BTK-IN-24
Research Areas:
Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
Research Areas:
SJ988497 is a PROTAC degrader targeting JAK2. SJ988497 induces the proteasomal degradation of CRBN-mediated JAK2, JAK1, JAK3, GSPT1, and IKZF1, and functions as a CRBN neosubstrate for GSPT1. SJ988497 retains binding affinity for the kinase domain of JAK2. SJ988497 can be used in studies related to cancers such as crlf2-rearranged acute lymphoblastic leukemia .
Cat. No.: HY-W133627
CAS No.: 118719-16-7
Target:
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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 .
Cat. No.: HY-178683
CAS No.: 2438125-72-3
ALV-05-077-01 is a BCL6/BCL6B degrader. ALV-05-077-01 binds to CRBN and recruits specific zinc finger proteins as neo-substrates for ubiquitination and proteasomal degradation. ALV-05-077-01 induces the degradation of full-length endogenous BCL6 zinc finger protein. ALV-05-077-01 induces the degradation of full-length endogenous BCL6B zinc finger protein. ALV-05-077-01 can be used in the research of hematological malignancies .
Cat. No.: HY-176067
Target:
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LO-4-25 is a CUL4 DCAF16 based covalent PROTAC-like degrader. LO-4-25 induces degradation of the androgen receptor (AR) and androgen receptor truncation variant AR-V7. LO-4-25 covalently targets cysteine residues on CUL4DCAF16 to mediate degradation of neo-substrates. LO-4-25 triggers proteasome-dependent degradation of target proteins via CUL4DCAF16-mediated ubiquitination. LO-4-25 can be used for the research of androgen-independent prostate cancer .
Cat. No.: HY-177730
Research Areas:
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-W947273
CAS No.: 2766178-72-5
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CRBN ligand-898 is a CRBN ligand with a Kd of 216 nM. CRBN ligand-898 binds to CRBN, and when incorporated into proteolysis targeting chimeras (PROTACs), mediates degradation of intended target proteins. CRBN ligand-898 does not induce degradation of IMiD-associated neosubstrates Ikaros (IKZF1) and Aiolos (IKZF3). CRBN ligand-898 can be used to synthesize PROTACs .
Cat. No.: HY-189222
CAS No.: 3118096-98-0
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RP04340 is an orally active, selective pan-KRAS PROTAC degrader. RP04340 hijacks the CRBN E3 ligase and the cellular proteasome system to degrade KRAS, without degrading HRAS, NRAS, or common CRBN neosubstrates. RP04340 inhibits KRAS downstream signaling pathways, including pERK and DUSP6. RP04340 exhibits anticancer activity in various KRAS-mutant cancers. RP04340 can be used to study kras-driven cancers, including pancreatic ductal adenocarcinoma, colorectal cancer, and lung adenocarcinoma .
Cat. No.: HY-133616
CAS No.: 2374699-35-9
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JH-XIII-05-01 is a cereblon-recruiting PROTAC degrader targeting IRAK1 and IRAK4, with DC50 values of 0.065 μM and 3.63 μM, respectively (TMD8 cells). JH-XIII-05-01 reduces cancer cell viability, induces apoptosis in primary MYD88-mutant WM cells and MYD88-mutant/wild-type lymphoma cells, and selectively degrades additional cereblon neosubstrates and kinases IKZF1, IKZF3, CSNK1A1, CSNK1D, CSNK1E, and PAK4. JH-XIII-05-01 can be used for research on Waldenström macroglobulinemia, diffuse large B-cell lymphoma, and B-cell lymphoma .
Cat. No.: HY-189226
Research Areas:
PROTAC BRD9 Degrader-12 is a BRD9 PROTAC degrader, with DC50 values of 57 pM and 62 pM against BRD9 and IKZF1, respectively. PROTAC BRD9 Degrader-12 promotes CRL-CRBN-dependent ubiquitination and proteasome-mediated BRD9 degradation by simultaneously binding to BRD9 and CRBN, and concurrently recruits IKZF1 as a neosubstrate via CRBN to induce its degradation. PROTAC BRD9 Degrader-12 selectively degrades BRD9 and IKZF1. The synergistic degradation of BRD9/IKZF1 downregulates MYC-related signaling, induces apoptosis and S-phase cell cycle arrest, and thereby inhibits the proliferation of hematological malignant cells. PROTAC BRD9 Degrader-12 is used for research related to hematological malignancies .
Cat. No.: HY-179499
CAS No.: 2978620-84-5
Research Areas:
PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer 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
