Ubiquitination
Ubiquitination (or ubiquitylation) is an enzymatic post-translational modification in which a ubiquitin protein is attached to a substrate protein. This process most commonly binds the last amino acid of ubiquitin (glycine 76) to a lysine residue on the substrate.
Products for Ubiquitination
- Cat.No. Product Name Information
- BCC2092 MLN2238 Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
- BCC2091 MLN9708 Ixazomib Citrate (MLN9708) immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.
- BCC6420 Spautin-1 Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.
- BCC3596 Dihydroeponemycin
- BCC4383 Sulfacetamide Sodium Sulfacetamide Sodium is an anti-infective agent that is used topically to treat skin infections and orally for urinary tract infections.
- BCC7988 NSC 624206 NSC624206 is an inhibitor of ubiquitin E1 (UBA1), with an IC50 of ~9 μM. NSC624206 specifically blocks ubiquitin-thioester formation (IC50=13 μM) but has no effect on ubiquitin adenylation.
- BCC4200 CC0651 CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.
- BCN1841 Lactacystin Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces neurite outgrowth.
- BCC1227 MG-132 MG-132 (Z-Leu-leu-leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
- BCC1237 MG-115
- BCC1235 Epoxomicin Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
- BCC4977 NMS-873 NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with IC50 value of 30 nM.
- BCN2292 Vinblastine Sulfate Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
- BCC3943 MNS MNS is a potent and selective inhibitor of Src and Syk tyrosine kinases.
- BCC4006 SAR405 SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.
- BCC1224 Clasto-Lactacystin β-lactone
- BCC6528 CB-5083 CB-5083 is a potent, selective and orally bioavailable p97 inhibitor with an IC50 value of 11 nM.
- BCC1124 PSI
- BCC3916 DBeQ DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
- BCC1238 Bortezomib (PS-341) Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first therapeutic proteasome inhibitor to be used in humans. Anti-cancer activity.
- BCC3984 SBI-0206965 SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2 .
- BCC3874 Wortmannin Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.
- BCC8004 SZL P1-41 SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.
- BCC3627 PR-619 PR-619 is a broad-range DUB inhibitor with EC50 of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively.
- BCC7908 SMER 28 SMER28 is a positive regulator of autophagy acting via an mTOR-independent mechanism. SMER28 prevents the accumulation of amyloid beta peptide.
- BCC6354 PRT 4165 PRT4165 is a potent inhibitor of PRC1 (Polycomb-repressive complex 1)-mediated H2A ubiquitylation.
- BCC3826 Nocodazole Nocodazole is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
- BCC4960 STF-62247 STF-62247 is TGN inhibitor with IC50 of 0.625μM and 16μM in RCC4 and RCC4/VHL cells,respectively.
- BCN5986 Celastrol Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
- BCC4000 NSC697923 Selective UBE2N inhibitor,NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A.
- BCC4470 PYR-41 PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
- BCC2094 Salinosporamide A (NPI-0052, Marizomib) Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
- BCC4384 Trifluoperazine 2HCl Trifluoperazine dihydrochloride (TFP) is an antipsychotic phenothiazine agent and a selective α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is also a potent dopamine D2 receptor inhibitor.
- BCC1184 Dexamethasone (DHAP) Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18L expression on monocytes.
- BCC3915 Chloroquine diphosphate Chloroquine phosphate is a toll-like receptors (TLRs) and autophagy inhibitor. Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro.
- BCC2097 Aspirin (Acetylsalicylic acid) Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL.
- BCC3714 3-Methyladenine 3-Methyladenine is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.
- BCN5768 Xanthohumol Valosin-containing protein (VCP) inhibitor; impairs autophagosome maturation,Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities.
- BCC1232 Aclacinomycin A
- BCC3823 Nimodipine Nimodipine(Nimotop) is a dihydropyridine derivative and an analogue of the calcium channel blocker nifedipine, with antihypertensive activity.
- BCN3894 Gliotoxin Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
- BCC6152 SMER 3
- BCC3918 (±)-Bay K 8644 Ca2+ channel activator (L-type); aids generation of iPSCs from MEFs
- BCN5973 Artemether Artemether is an antimalarial for the treatment of resistant strains of falciparum malaria.
- BCC1254 Omeprazole Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.
- BCC4379 Divalproex Sodium Divalproex Sodium, consisting of a compound of sodium valproate and valproic acid in a 1:1 molar relationship in an enteric coated form, is a HDAC inhibitor, used in the treatment for epilepsy.
- BCC3919 Concanamycin A Concanamycin A (Antibiotic X 4357B) is a macrolide antibiotic and a specific vacuolar type H+-ATPase (V-ATPase) inhibitor.
- BCC2093 CEP-18770 Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.
- BCC3686 WP1130 Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
- BCC3589 AM 114
- BCC1145 Carfilzomib (PR-171) Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
- BCC3914 Bafilomycin A1 Bafilomycin A1, a macrolide antibiotic isolated from the Streptomyces species, is a specific inhibitor of vacuolar-type H+ ATPase (V-ATPase). Bafilomycin A1 inhibits autophagy and induces apoptosis.
- BCC1146 Oprozomib (ONX-0912) Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.
- BCC2095 ONX-0914 (PR-957) ONX-0914 (PR-957) is a potent and selective inhibitor of immunoproteasome subunit LMP7.