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Daratumumab (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab has anti-multiple myeloma (MM) effect. Daratumumab impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
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 .
Q901 (CDK7-IN-21) is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 can be used for the research of cancer, such as colon cancer and lung cancer .
Daratumumab (PBS) (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab (PBS) has anti-multiple myeloma (MM) effect. Daratumumab (PBS) impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
(E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.
Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticumcollagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma .
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 .
Boc-LRR-AMC (Boc-Leu-Arg-Arg-AMC) is a fluorogenic substrate, which can be utilized for detecting the trypsin-like activity of the 26S proteasome or the 20S proteasome core .
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 .
LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits humanCDK12 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 .
Biotin-(Oaa)3-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)3-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain .
Z-GGF-CMK is an Antibacterial agent, an inhibitor of the ClpP1P2 serine protease complex (with an IC50 of 50 μM against intracellular ClpP1P2 protease activity in Mycobacterium bovis BCG), and a selective inhibitor of the mycobacterial Proteasome (with an IC50 of 50 μM against the proteasome in M. bovis BCG). Z-GGF-CMK inhibits the growth of mycobacteria. Z-GGF-CMK exhibits cytotoxic activity against liver cancer cells. Z-GGF-CMK can be used in the research of tuberculosis .
Alcudacigib (ASP1570; DGKζ-IN-1) is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC50 of 4.7 nM against humanDGKζ 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 .
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. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .
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 .
NR-V04 is a selective NR4A1 PROTAC degrader. NR-V04 forms a ternary complex with NR4A1 and the VHL E3 ligase, mediates proteasome-dependent degradation of NR4A1. NR-V04 induces tumor-infiltrating B cells and effector memory CD8 + T cells and reduces monocytic myeloid-derived suppressor cells in tumor microenvironments. NR-V04 can be used for the research of melanoma and colon cancer .
GNF6702 is a selective inhibitor of the kinetoplastid proteasome. GNF6702 clears parasites in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis .
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .
SMD-3236 is a SMARCA2PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against humanSMARCA2. 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 .
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
Alcudacigib (ASP1570; DGKζ-IN-1) TFA is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC50 of 4.7 nM against humanDGKζ 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 .
PROTAC JAK2 degrader-1 is a JAK2PROTAC degrader, with a DC50 of 27.35 nM. PROTAC JAK2 degrader-1 induces JAK2 degradation via the ubiquitin-proteasome pathway. PROTAC JAK2 degrader-1 inhibits the JAK2-STAT signaling pathway. PROTAC JAK2 degrader-1 induces G2/M phase arrest and apoptosis in cancer cells. PROTAC JAK2 degrader-1 exhibits antiproliferative activity against cancer cells. PROTAC JAK2 degrader-1 inhibits recombinant human erythropoietin (rhEPO)-mediated polycythemia and splenomegaly in mice. PROTAC JAK2 degrader-1 can be used for research on myeloproliferative neoplasms, including polycythemia vera .
GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovaniproteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of humanproteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties .
TDI-8304, a macrocyclic peptide, is a potent, species selective, and noncovalent Plasmodium falciparum (Pf20S) inhibitor. TDI-8304 shows highly selective for Pf20S over humanproteasomes .
BC-05 is an orally active and potent inhibitor of CD13 and proteasome. BC-05 has an IC50 value of 0.13 μM for human CD13 and an IC50 value of 1.39 μM for the 20S proteasome. BC-05 can be used in multiple myeloma research .
(E)-Ferulic acid (Standard) is the analytical standard of (E)-Ferulic acid. This product is intended for research and analytical applications. (E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.
Aloin (mixture of A&B) (Standard) is the analytical standard of Aloin (mixture of A&B) (HY-N6013). This product is intended for research and analytical applications. Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticumcollagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma .
20S Proteasome-IN-4 (Compound 7) is a brain-penetrant, parasite-selective, orally active 20S proteasome inhibitor with an IC50 of 6.3 nM against T. b. brucei 20S proteasome. 20S Proteasome-IN-4 can be used for the research of human African trypanosomiasis (HAT) .
20S Proteasome-IN-2 is a human20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M .
RID-F (Ridaifen-F), a Tamoxifen (HY-13757A) derivative, is a nonpeptidic proteasome inhibitor. RID-F inhibits human 20S proteasome activity, with IC50s of 0.64, 0.34, and 0.43 μM for CT-L, T-L, and PGPH, respectively .
Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruziproteasome, with an pIC50 of 7.4 and <4 for T. cruzi and humanproteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study .
JBIR-22 is a protein-protein interaction inhibitor of proteasome assembly factor 3 homodimer, which has the activity of inhibiting this interaction and exerting long-term cytotoxicity against human cervical cancer cell lines, and its stereochemical structure has been determined by total synthesis.
FV-162 is a potent, orally active and irreversible proteasome inhibitor. FV-162 exhibits cytotoxic to human myeloma cell lines and primary myeloma cells. FV-162 inhibits tumor growth in a myeloma xenograft mouse model. FV-162 can be used for myeloma research .
HT1171 is a potent and selective inhibitor of mycobacterium tuberculosis proteasome. HT1171 shows strong anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv with an MIC90 of 2 μg/mL and an MIC of 4 μg/mL. When HT1171 concentration is 100 μM, the inhibition rate of human normal hepatocytes L02 is 53.8%. HT1171 can be used in the research of antitubercular agent .
YSY01A is a proteasome inhibitor that can suppress cancer cell survival by inducing apoptosis (Apoptosis). Its IC50 values are 51.0 nM for HEK293T, 9.2 nM for A549, 5.2 nM for MCF-7, 8.9 nM for MGC-803, and 35.4 nM for PC-3M cells. Additionally, YSY01A eliminates constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A holds promise for research in the field of cancer therapy .
Pf20S-IN-1 is a selective inhibitor of the 20S proteasome β5 subunit of Plasmodium falciparum. Pf20S-IN-1 exhibits antiparasitic activity against Plasmodium falciparum, with an EC50 of 20.1 nM against the Plasmodium falciparum W2 strain. Pf20S-IN-1 shows weak inhibitory effect on human 20S proteasome, has no obvious toxicity to human foreskin fibroblasts (HFF), and has a selectivity index > 25000. Pf20S-IN-1 can be used in malaria research .
PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with an IC50 of 185.7 nM against humanPRMT1. PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma .
Ixazomib citrate (Standard) is the analytical standard of Ixazomib citrate (HY-10452). This product is intended for research and analytical applications. 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 .
Isomoreollic acid is a cage xanthonoid. Isomoreollic acid exhibits cytotoxicity against colon cancer cells, with an IC50 > 10 μM for proteasome inhibition. Isomoreollic acid is present in the stem bark of Garcinia lateriflora. Isomoreollic acid can be used in colon cancer research .
SD-965 is a selective STAT3PROTAC degrader with a DC50 of 0.14 μM. SD-965 promotes the ubiquitination and degradation of STAT3. SD-965 induces rapid, complete and persistent depletion of STAT3 protein. SD-965 induces tumor regression in mouse xenograft models of leukemia and lymphoma .
PROTAC BRD9 Degrader-11 is a VHL-based BRD9PROTAC degraderwith an IC50 of 0.66 μM. PROTAC BRD9 Degrader-11 induces selective, proteasome-dependent degradation of BRD9 via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-11 impairs cell viability, suppresses proliferation, and arrests growth of acute myeloid leukemia cells. PROTAC BRD9 Degrader-11 can be used for the research of acute myeloid leukemia .
PROTAC HPK1 Degrader-7 (compound D02) is a potent and selective PROTAC HPK1 degrader with an DC50 of 3.07 nM. PROTAC HPK1 Degrader-7 exhibits selectivity over GLK. PROTAC HPK1 Degrader-7 induces HPK1 degradation in a CRBN- and proteasome-dependent manner. PROTAC HPK1 Degrader-7 inhibits SLP-76 phosphorylation, induces IL-2 and IFN-γ secretion in human primary T cells. PROTAC HPK1 Degrader-7 can be used for immunology research .
PROTAC SARS-CoV-2 Mpro degrader-5 is a SARS-CoV-2 main protease (Mpro) PROTAC. PROTAC SARS-CoV-2 Mpro degrader-5 engages CRBN E3 ubiquitin ligase to form a ternary complex with SARS-CoV-2 Mpro, induces K48-linked polyubiquitination of SARS-CoV-2 Mpro, and drives proteasome-dependent turnover of SARS-CoV-2 Mpro with a high selectivity index (CC50/DC50 > 10) in human embryonic kidney cells.PROTAC SARS-CoV-2 Mpro degrader-5 can be used for the research of COVID-19 .
Berberine-amide-m-PhBA chloride (Compound 8b) is a selective anti-breast cancer agent. Berberine-amide-m-PhBA chloride may inhibit the proteasome by interacting with the 20S proteasome β5 subunit. Berberine-amide-m-PhBA chloride can be used in the research of breast cancer .
PDL1 degrader-3 (comppund e24) is a CSN5-binding antitumor immunomodulator with a humanCSN5Kd of 4.53 μM. PDL1 degrader-3 inhibits CSN5 enzymatic activity, increases PD-L1 ubiquitination, and induces PD-L1 degradation via the ubiquitin-proteasome pathway, reducing PD-L1 expression on tumor cell membranes. PDL1 degrader-3 blocks PD-1/PD-L1 interaction, activates the tumor immune microenvironment, enhances tumor-infiltrating T-cell immunity, and inhibits activation of immunosuppressive MDSCs and Tregs. PDL1 degrader-3 exerts antitumor effects in mouse tumor models. PDL1 degrader-3 can be used for the research of colorectal cancer, lung cancer .
PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer .
Boc-LRR-AMC (Boc-Leu-Arg-Arg-AMC) is a fluorogenic substrate, which can be utilized for detecting the trypsin-like activity of the 26S proteasome or the 20S proteasome core .
Biotin-(Oaa)3-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)3-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain .
Z-GGF-CMK is an Antibacterial agent, an inhibitor of the ClpP1P2 serine protease complex (with an IC50 of 50 μM against intracellular ClpP1P2 protease activity in Mycobacterium bovis BCG), and a selective inhibitor of the mycobacterial Proteasome (with an IC50 of 50 μM against the proteasome in M. bovis BCG). Z-GGF-CMK inhibits the growth of mycobacteria. Z-GGF-CMK exhibits cytotoxic activity against liver cancer cells. Z-GGF-CMK can be used in the research of tuberculosis .
Daratumumab (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab has anti-multiple myeloma (MM) effect. Daratumumab impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
Daratumumab (PBS) (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab (PBS) has anti-multiple myeloma (MM) effect. Daratumumab (PBS) impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
(E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.
Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticumcollagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma .
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
(E)-Ferulic acid (Standard) is the analytical standard of (E)-Ferulic acid. This product is intended for research and analytical applications. (E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.
Aloin (mixture of A&B) (Standard) is the analytical standard of Aloin (mixture of A&B) (HY-N6013). This product is intended for research and analytical applications. Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticumcollagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma .
Isomoreollic acid is a cage xanthonoid. Isomoreollic acid exhibits cytotoxicity against colon cancer cells, with an IC50 > 10 μM for proteasome inhibition. Isomoreollic acid is present in the stem bark of Garcinia lateriflora. Isomoreollic acid can be used in colon cancer research .
The PSMD7 protein is a component of the 26S proteasome and promotes the ATP-dependent degradation of ubiquitinated proteins. It maintains protein homeostasis by eliminating misfolded or unnecessary proteins, thereby protecting cellular function. PSMD7 Protein, Human (sf9) is the recombinant human-derived PSMD7 protein, expressed by sf9 insect cells , with tag free.
Gankyrin/PSMD10 protein is a key partner in 26S proteasome assembly and contributes to the formation of the PA700/19S regulatory complex (RC). In basal subcomplex assembly, it engages PSMD10, PSMC4, PSMC5, and PAAF1, and possibly PSMD5, PSMC2, PSMC1, and PSMD2. Gankyrin/PSMD10 Protein, Human is the recombinant human-derived Gankyrin/PSMD10 protein, expressed by E. coli , with tag free.
The PSMG3 protein acts as a chaperone and actively promotes the assembly of the 20S proteasome. It involves potential cooperation with the PSMG1-PSMG2 heterodimer to ensure precise assembly of the proteasome. PSMG3 Protein, Human is the recombinant human-derived PSMG3 protein, expressed by E. coli , with tag free.
PSMG4 protein functions as a chaperone, facilitating the assembly of the 20S proteasome. In its role as a chaperone, PSMG4 interacts with PSMG3, forming a functional complex that contributes to the proper assembly of the 20S proteasome. Notably, PSMG4 associates specifically with the alpha subunits of the 20S proteasome, highlighting its involvement in the intricate process of proteasomal maturation and functionality. PSMG4 Protein, Human is the recombinant human-derived PSMG4 protein, expressed by E. coli , with tag free.
The PSMG3 protein acts as a chaperone and actively promotes the assembly of the 20S proteasome. It involves potential cooperation with the PSMG1-PSMG2 heterodimer to ensure precise assembly of the proteasome. PSMG3 Protein, Human (His, Strep) is the recombinant human-derived PSMG3 protein, expressed by E. coli , with N-Strep, N-6*His labeled tag.
PSMG4 protein functions as a chaperone, facilitating the assembly of the 20S proteasome. In its role as a chaperone, PSMG4 interacts with PSMG3, forming a functional complex that contributes to the proper assembly of the 20S proteasome. Notably, PSMG4 associates specifically with the alpha subunits of the 20S proteasome, highlighting its involvement in the intricate process of proteasomal maturation and functionality. PSMG4 Protein, Human (His, Strep) is the recombinant human-derived PSMG4 protein, expressed by E. coli , with N-Strep, N-6*His labeled tag.
PSMA3 is a protein involved in protein degradation. PSMA3 Protein, Human (His) is the recombinant human-derived PSMA3 protein, expressed by E. coli , with N-His labeled tag.
PSME3 is a subunit of the 11S REG-gamma proteasome modulator that forms a homoheptamer and is essential for activating the trypsin-like subunit of the proteasome and inhibiting the chymotrypsin-like and PGPH subunits. PSME3 promotes MDM2-p53 interaction, leading to p53 degradation and inhibiting apoptosis after DNA damage. PSME3 Protein, Human (His, solution) is the recombinant human-derived PSME3 protein, expressed by E. coli , with N-His labeled tag.
PSME3 is a subunit of the 11S REG-gamma proteasome modulator that forms a homoheptamer and is essential for activating the trypsin-like subunit of the proteasome and inhibiting the chymotrypsin-like and PGPH subunits. PSME3 promotes MDM2-p53 interaction, leading to p53 degradation and inhibiting apoptosis after DNA damage. PSME3 Protein, Human (N-His) is the recombinant human-derived PSME3 protein, expressed by E. coli , with N-His labeled tag.
The PSME1 protein is critical for immunoproteasome assembly and is essential for efficient antigen processing. As part of the PA28 activator complex, PSME1, together with PSME2, actively enhances the production of class I binding peptides by altering the cleavage pattern of the proteasome. PSME1 Protein, Human (His) is the recombinant human-derived PSME1 protein, expressed by E. coli , with N-6*His labeled tag.
PSME2 Protein, vital for immunoproteasome assembly, is crucial for efficient antigen processing. In collaboration with PSME1, the PA28 activator complex modifies the proteasome's cleavage pattern, actively contributing to class I binding peptide generation. The hexameric ring structure of this heterodimeric complex underscores its significance in orchestrating processes essential for immune responses and antigen presentation. PSME2 Protein, Human (His) is the recombinant human-derived PSME2 protein, expressed by E. coli , with N-His labeled tag.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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