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7-(N-Benzyloxycarbonylglycyl-glycyl-leucyl)amino-4-methylcoumarin is a fluorogenic substrate for the chymotrypsin-like activity of the 20S proteasome. Synonyms: 7-Z-Gly-gly-leu-ME; L-Leucinamide, N-[ (phenylmethoxy)carbonyl]glycylglycyl-N- (4-methyl-2-oxo-2H-1-benzopyran-7-yl)-; Z-GGL-AMC. Grades: ≥98%. CAS No. 97792-39-7. Molecular formula: C28H32N4O7. Mole weight: 536.58.
Ac-Arg-Leu-Arg-AMC
Ac-Arg-Leu-Arg-AMC is a fluorogenic substrate for the determination of the trypsin-like activity of purified proteasomes (Km = 78 μM). Synonyms: Ac-RLR-AMC; N2-Acetyl-L-arginyl-L-leucyl-N-(4-methyl-2-oxo-2H-chromen-7-yl)-L-argininamide; L-Argininamide, N2-acetyl-L-arginyl-L-leucyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-. Grades: ≥95%. CAS No. 929903-87-7. Molecular formula: C30H46N10O6. Mole weight: 642.76.
Ac-Nle-Pro-Nle-Asp-AMC
Ac-Nle-Pro-Nle-Asp-AMC is a substrate for proteasomes. It can be cleaved by the caspase-like site of proteasome, also known as postglutamyl peptide hydrolase (PGPH). AMC (7-amino-4-methylcoumarin) is released and produces the fluorescence utilized to quantify the caspase-like site activity. Ac-Nle-Pro-Nle-Asp-AMC also inhibits the chymotrypsin-like activity of the proteasome allosterically when bound to the caspase-like site. Synonyms: Ac-Nle-Pro-Nle-Asp-7-amido-4-Methylcoumarin; Ac-nLPnLD-AMC; N-acetyl-L-norleucyl-L-prolyl-L-norleucyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-L-α-asparagine; L-α-Asparagine, N-acetyl-L-norleucyl-L-prolyl-L-norleucyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-; (3S) -4-Hydroxy-3- ({ (2S) -1-hydroxy-2-[ (hydroxy{ (2S) -1-[N- (1-hydroxyethylidene) -L-norleucyl]-2-pyrrolidinyl}methylene) amino]hexylidene}amino) -4-[ (4-methyl-2-oxo-2H-chromen-7-yl) imino]butanoic acid. Grades: ≥98%. CAS No. 355140-49-7. Molecular formula: C33H45N5O9. Mole weight: 655.74.
Ac-RLR-AMC trifluoroacetate salt
Ac-RLR-AMC is a fluorogenic substrate for the 26S proteasome. Ac-RLR-AMC is cleaved to release the fluorescent moiety 7-amino-4-methylcoumarin (AMC), which can be used to quantify the trypsin-like activity of 26S proteasomes. Synonyms: Ac-Arg-Leu-Arg-7-amino-4-methylcoumarin; (S)-2-acetamido-5-guanidino-N-((S)-1-(((S)-5-guanidino-1-((4-methyl-2-oxo-2H-chromen-7-yl)amino)-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)pentanamide, 2,2,2-trifluoroacetate salt. Grades: ≥98%. Molecular formula: C30H46N10O6·CF3COOH. Mole weight: 756.8.
Ac-WLA-AMC
Ac-WLA-AMC is a fluorogenic substrate for the β5c subunit of the 20S proteasome. Ac-WLA-AMC is cleaved to release the fluorescent moiety 7-amino-4-methylcoumarin (AMC), which can be used to quantify the β5c subunit activity. Synonyms: Acetyl-Trp-Leu-Ala-7-amino-4-Methylcoumarin; N-acetyl-L-tryptophyl-L-leucyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-L-alaninamide. Grades: ≥95%. CAS No. 1104011-59-7. Molecular formula: C32H37N5O6. Mole weight: 587.7.
Boc-Leu-Ser-Thr-Arg-AMC
Boc-Leu-Ser-Thr-Arg-AMC is a good fluorescent substrate for activated protein C (Km = 3.3·10-4 M, kcat = 8.4 s-1) and is commonly used to measure tryptic activity of proteasome. Synonyms: Boc-LSTR-AMC; Boc-leucyl-seryl-threonyl-arginine-4-methylcoumaryl-7-amide; Boc-Leu-Ser-Thr-Arg-7-amido-4-methylcoumarin. Grades: ≥95%. CAS No. 73554-93-5. Molecular formula: C34H52N8O10. Mole weight: 732.82.
ML241
ML241 is a selective p97 ATPase inhibitor and IC50 value is 100 nM. It can inhibit degradation of a p97-dependent but not a p97-independent proteasomesubstrate in a dual-reporter cell line. ML241 may be a novel agent for the treatment of cancer. Uses: Anticancer. Synonyms: 2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine; ML241; ML-241; ML 241. Grades: 98%. CAS No. 1346528-06-0. Molecular formula: C23H24N4O. Mole weight: 372.46.
ML241 HCl
ML241 is identified as a potent and selective inhibitors of p97 ATPase (IC(50)= 100 nM). ML241 inhibits degradation of a p97-dependent but not a p97-independent proteasomesubstrate in a dual-reporter cell line. ML241 could impair the endoplasmic-reticulum-associated degradation (ERAD) pathway. Synonyms: 2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine hydrochloride; ML241; ML-241; ML 241; ML241 HCl; ML241 hydrochloride. CAS No. 2070015-13-1. Molecular formula: C23H25ClN4O. Mole weight: 408.93.
Ubiquitin-conjugating enzymes perform the second step in the ubiquitination reaction that targets a protein for degradation via the proteasome. The ubiquitination process covalently attaches ubiquitin, a short protein of 76 amino acids, to a lysine residue on the target protein. Once a protein has been tagged with one ubiquitin molecule, additional rounds of ubiquitination form a polyubiquitin chain that is recognized by the proteasome's 19S regulatory particle, triggering the ATP-dependent unfolding of the target protein that allows passage into the proteasome's 20S core particle, where proteases degrade the target into short peptide fragments for recycling by the cell. Applications: Ubiquitin conjugating enzyme fractions mammalian may be used in transferring the activated ubiquitin from e1 to the substrate through an additional high energy thiol ester intermediate e2-s-ubiquitin. ubiquitin-conjugating enzymes, also known as e2 enzymes and more rarely as ubiquitin-carrier enzymes, perform the second step in the ubiquitination reaction that targets a protein for degradation via the proteasome. Group: Enzymes. Synonyms: Ubiquitin con. Ubiquitin Conjugating Enzyme. Storage: -70°C. Source: Mammalian. Ubiquitin conjugating enzymes; Ubiquitin Conjugating Enzyme Fractions; E2 enzymes; ubiquitin-carrier enzymes. Cat No: NATE-0727.
proteasome endopeptidase complex
A 20-S protein composed of 28 subunits arranged in four rings of seven. The outer rings are composed of α subunits, but the β subunits forming the inner rings are responsible for peptidase activity. In eukaryotic organisms there are up to seven different types of β subunits, three of which may carry the N-terminal threonine residues that are the nucleophiles in catalysis, and show different specificities. The molecule is barrel-shaped, and the active sites are on the inner surfaces. Terminal apertures restrict access of substrates to the active sites. There is evidence that catalytic subunits are replaced by others under some conditions so as to alter the spec...atalytic proteinase; proteasome organelle; alkaline protease; 26S protease; tricorn proteinase; tricorn protease. Enzyme Commission Number: EC 3.4.25.1. CAS No. 140879-24-9. Alkaline Protease. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-4374; proteasome endopeptidase complex; EC 3.4.25.1; 140879-24-9; ingensin; macropain; multicatalytic endopeptidase complex; prosome; multicatalytic proteinase (complex); MCP; proteasome; large multicatalytic protease; multicatalytic proteinase; proteasome organelle; alkaline protease; 26S protease; tricorn proteinase; tricorn protease. Cat No: EXWM-4374.
Suc-Leu-Leu-Val-Tyr-AMC
Suc-Leu-Leu-Val-Tyr-AMC is a fluorogenic substrate of calpains and 20S proteasome. Synonyms: Suc-LLVY-AMC; Proteasomesubstrate (fluorogenic); Calpain substrate (fluorogenic). Grades: >97%. CAS No. 94367-21-2. Molecular formula: C40H53N5O10. Mole weight: 763.89.
Suc-Leu-Leu-Val-Tyr-pNA
Suc-Leu-Leu-Val-Tyr-pNA is a chromogenic substrate analogue to the proteasomesubstrate Suc-LLVY-AMC. Synonyms: Suc-LLVY-pNA; N-(3-Carboxypropanoyl)-L-leucyl-L-leucyl-L-valyl-N-(4-nitrophenyl)-L-tyrosinamide; L-Tyrosinamide, N-(3-carboxy-1-oxopropyl)-L-leucyl-L-leucyl-L-valyl-N-(4-nitrophenyl)-. Grades: ≥90%. CAS No. 1926163-44-1. Molecular formula: C36H50N6O10. Mole weight: 726.83.
Z-Leu-Leu-Glu-AMC
Z-Leu-Leu-Glu-AMC is a substrate peptide, and can be used for determination of postacidic-like hydrolysing activity of 20S proteasome [1]. Uses: Scientific research. Group: Peptides. Alternative Names: Z-LLE-AMC. CAS No. 348086-66-8. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-123053.
Z-LLE-AMC
Z-LLE-AMC is a fluorogenic substrate for the caspase-like post-glutamate peptide hydrolase of the 26S proteasome or 20S proteolytic core. AMC (7-amino-4-methylcoumarin) is released to quantify the caspase-like hydrolase activity. Synonyms: ProteasomeSubstrate III, Fluorogenic. Grades: >95%. CAS No. 348086-66-8. Molecular formula: C35H44N4O9. Mole weight: 664.76.
A cell-permeable bis-nitrobenzylidene-piperidinone compound that acts as a potent, reversible and selective inhibitor of 19S regulatory-particle-associated deubiquitylating enzymes (DUBs) UCH-L5 and USP-14 (IC50=2.1uM against Ub-AMC substrate), with no effect on UCH-L1, UCH-L3, USP2, USP7, USP8 and BAP1 and on the proteasomal proteolytic activities. Shown to prevent proteasomal degradation (IC50=0.8uM in MelJuSo-UbG76V-YFP cells), and cause accumulation of higher molecular weights polyubiquitinated proteins in HCT-116 cells. Preferentially induces cell-cycle arrest and apoptosis in several colon cancer and in CNS cells, and effectively suppresses tumor growth in various mouse model (5mg/kg, i.p.). Group: Biochemicals. Grades: Highly Purified. CAS No. 1009817-63-4. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?, Molecular Weight: 419.4. US Biological Life Sciences.
Worldwide
Golcadomide
Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL) [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: CC-99282. CAS No. 2379572-34-4. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-146237.
A potent, reversible proteasome inhibitor with Ki of 21nM for 20S proteasome and 35nM for 26S proteasome. The inhibition of proteasome was through specific inhibition of chymotrypsin-like activity of the proteasome. Also shown to induce apoptosis in Rat-1 and PC12 cells via a p3-independent pathway. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
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