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Proteasome/Ubiquitin

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Cat. No. Product Name Field of Application Chemical Structure
DC11509 USP25 and 28 inhibitor AZ-2 USP25 and 28 inhibitor AZ-2 is a potent, selective, dual USP25/28 inhibitor with IC50 of 0.9/0.9 uM, respectively.
DC7525 USP7-USP47 inhibitor USP7/USP47 inhibitor is a potent and dual inhibitor of USP7/USP47 with IC50s of 0.42 uM(USP7) and 1.0 uM(USP47).
DC8299 VER155008 Featured VER-155008 is a novel, small molecule inhibitor of Hsc70/Hsp70 with GI50 of 5.3-14.4 uM in human breast and colon cancer cell lines.
DC7737 VER-50589 VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
DC10642 VLX1570 VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro.
DC8448 VR23 Featured VR-23 is a Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E–Mediated Centrosome Amplification
DC11876 XL 188 XL188 (XL-188) is a potent, selective, non-covalent active-site inhibitor of USP7 with IC50 of 90 nM and 193 nM for USP7 full length enzyme and catalytic domain, respectively.
DC6307 XL888 Featured XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.
DC8142 TAS-116 Featured TAS-116 is a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models.
DC11506 USP25 and 28 inhibitor AZ-1 Featured USP25 and 28 inhibitor AZ-1 (AZ1) is a potent, selective, dual USP25/28 inhibitor with IC50 of 0.7/0.6 uM, respectively; shows a high degree of selectivity over other deubiquitinases (USP4,7 etc.); demonstrates target engagement against both USP25 and USP28 in cells, elicits modulation of both the total levels and the half-life of the c-Myc oncoprotein in cells, and also induces apoptosis and inhibits cell viability in a range of cancer cell lines.
DC28551 USP7-IN-5 USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM.
DC28552 USP7-IN-6 USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM.
DC28734 6RK73 6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer.
DC28777 Ubiquitination-IN-1 Ubiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors.
DC28847 (1S,2S)-Bortezomib (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
DC29221 PTP1B-IN-9 Featured PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. PTP1B-IN-9 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. PTP1B-IN-9 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity.
DC31044 SJB3-019A A novel potent ubiquitin-specific protease USP1 inhibitor with IC50 of 78.1 nM, 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells.
DC31045 BC-1471 BC-1471 is a selective, small-molecule deubiquitinase STAM-binding protein (STAMBP) inhibitor (IC50=0.33 uM) that interrupts STAMBP-Ub-NALP7 interaction.
DC31046 P 217564 P 217564 is a potent, selective, irreversible second generation inhibitor of USP7 with IC50 of 0.48 uM, with similar potency against USP47 and no significant activity aginst other DUBs.
DC39084 Mezigdomide(CC-92480) Featured Mezigdomide is a cereblon E3 ubiquitin ligase modulating agent with potential immunomodulating and antineoplastic activities. Mezigdomide specifically binds to cereblon (CRBN), thereby affecting the ubiquitin E3 ligase activity, and targeting certain substrate proteins for ubiquitination. This induces proteasome-mediated degradation of certain transcription factors, some of which are transcriptional repressors in T cells. This leads to modulation of the immune system, including activation of T lymphocytes, and downregulation of the activity of other proteins, some of which play key roles in the proliferation of certain cancer cell types.
DC39096 MDL-28170 Featured MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.
DC40066 Arimoclomol citrate Arimoclomol citrate (BRX-220 citrate) is a co-inducer of heat shock proteins (HSP). Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.
DC40228 (Rac)-Calpain Inhibitor XII (Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM), with lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
DC40344 3-Phenyltoxoflavin Featured 3-Phenyltoxoflavin, a derivative of Toxoflavin, is an Hsp90 inhibitor, with a Kd of 585 nM for the interaction of Hsp90-TPR2A. 3-Phenyltoxoflavin has anti-cancer activity.
DC40452 17-GMB-APA-GA 17-GMB-APA-GA is an ADC Cytotoxin. 17-GMB-APA-GA is a potent HSP90 inhibitor and used for latent T. gondii infection research.
DC40629 17-AEP-GA 17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
DC40630 Aminohexylgeldanamycin Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activities.
DC40719 Geldanamycin-FITC Geldanamycin-FITC, a Geldanamycin fluorescent probe, can be used in a fluorescence polarization assay for HSP90 inhibitors. Geldanamycin-FITC also can be used for detection of cell surface HSP90.
DC41299 Eupalinolide A Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
DC41386 10,11-Dehydrocurvularin 10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
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