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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
77 Results for "
human proteasome
" in MedChemExpress (MCE) Product Catalog:
Products (77)
77 Results for "human proteasome" in MCE Product Catalog:
13
13 Publications Verification
Cat. No.: HY-P9915
CAS No.: 945721-28-8
Synonyms: Anti-human CD38, human Antibody; HuMax-CD38; JNJ-54767414
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13
13 Publications Verification
Cat. No.: HY-P9915A
CAS No.: 945721-28-8
Synonyms: Anti-human CD38, human Antibody (PBS)
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Ixazomib citrate (MLN9708) is a selective, orally active, second-generation proteasome inhibitor. Ixazomib citrate can be used for the study of a broad range of human malignancies .
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1 Cited Publications
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LU-002i is a subunit-selective human proteasome β2c and β2i inhibitor with an IC50 value of 220 nM for β2i .
Cat. No.: HY-172208
CAS No.: 3118499-89-8
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PROTAC cGAS degrader-1 is a potent and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 induces proteasome-mediated degradation of cGAS, inhibits the cGAS signaling pathway, and attenuates double-stranded DNA-induced activation of cGAS in human and mouse cells. PROTAC cGAS degrader-1 is applicable to research related to ulcerative colitis .
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-163944
CAS No.: 3081311-94-3
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LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .
Cat. No.: HY-148381
CAS No.: 2378056-80-3
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A947 is a VHL-based SMARCA2 PROTAC degrader with a DC50 of 39 pM and a Kd of 93 nM for human SMARCA2. A947 recruits SMARCA2 to the VHL E3 ubiquitin ligase for ubiquitination modification, mediates its degradation via the proteasome, and exerts selective degradation effects on SMARCA4 and PBRM1. A947 induces G1 cell cycle arrest, inhibits transcription, and exerts growth inhibitory effects in SMARCA4 G12C-mutant cancer cells. A947 acts synergistically with MCL1 inhibitors to induce apoptosis in SMARCA4 G12C-mutant cancer cells. A947 can be used in studies related to SMARCA4 G12C-mutant non-small cell lung cancer and non-small cell lung cancer .
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Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia .
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PROTAC ER Degrader-4 is a potent ERα PROTAC degrader, with an IC50 of 0.8 nM against human ERα. PROTAC ER Degrader-4 recruits the VHL E3 ligase to ERα, and triggers the ubiquitination modification and degradation of ERα via the UP/26S proteasome system. PROTAC ER Degrader-4 can be used in related research on breast cancer .
Cat. No.: HY-153793
CAS No.: 2660218-70-0
Synonyms: DGKζ-IN-1
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Alcudacigib (ASP1570; DGKζ-IN-1) is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC50 of 4.7 nM against human DGKζ and an IC50 of 3.0 nM against mouse DGKζ. Alcudacigib selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib enhances the anti-tumor functions of T cells and NK cells. Alcudacigib can be used for the research of advanced/metastatic solid tumors .
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MS8815 is a EZH2 PROTAC degrader, with a DC50 of 140 nM in MDA-MB-453 triple-negative breast cancer (TNBC) cells and an IC50 of 8.6 nM against human EZH2. MS8815 induces ubiquitin-proteasome system-mediated degradation of EZH2, reduces the levels of EED, SUZ12, FOXM1, H3K27me3 and global m6A, and increases the protein level of HMGCS2. MS8815 can be used in the research of breast cancer and prostate cancer .
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-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 .
Cat. No.: HY-170824
CAS No.: 3033586-31-8
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SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia .
Cat. No.: HY-N8146
CAS No.: 53729-52-5
Cat. No.: HY-153793A
Synonyms: DGKζ-IN-1 TFA
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Alcudacigib (ASP1570; DGKζ-IN-1) TFA is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC50 of 4.7 nM against human DGKζ and an IC50 of 3.0 nM against mouse DGKζ. Alcudacigib TFA selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib TFA enhances the anti-tumor functions of T cells and NK cells. Alcudacigib TFA can be used for the research of advanced/metastatic solid tumors .
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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
