662140 Sigma-AldrichDUB Inhibitor IV, b-AP15 - CAS 1009817-63-3 - Calbiochem
The DUB Inhibitor IV, b-AP15 controls the biological activity of DUB. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.
More>> The DUB Inhibitor IV, b-AP15 controls the biological activity of DUB. This small molecule/inhibitor is primarily used for Protease Inhibitors applications. Less<<Synonyms: USP14 Inhibitor III, UCH-L5/UCH37 Inhibitor II, NSC687852, 3,5-bis((4-Nitrophenyl)methylidene)-1-prop-2-enoylpiperidin-4-one, (3E,5E)-1-Acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one
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Overview
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Key Spec Table
CAS # | Empirical Formula |
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1009817-63-3 | C₂₂H₁₇N₃O₆ |
Description | |
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Overview | A cell-permeable bis-nitrobenzylidene-piperidinone that inhibits 19S deubiquitinase (DUB) activity (IC50 = 2.1 µM against Ub-AMC hydrolysis) in a reversible manner by directly targeting UCH37/UCH-L5 and USP14, while exhibiting little or no activity toward BAP1, UCH-L1, UCH-L3, USP2, USP7, USP8 (IC50 >100 µM), or POH1/PRN11. Dual UCH37 and USP14 inhibition by a-AP15 results in increased bulk cellular protein ubiquitination level and a blockage of protein proteasomal degradation (Effective conc. ≥770 nM in HCT-116 cells), exactly opposite to the effects seen with USP14 inhibition alone by IU1 (Cat. No. 662210). Effectively suppresses the growth of various tumors in mice (2.5 to 5 mg/kg, i.p. or s.c.) in vivo. |
Catalogue Number | 662140 |
Brand Family | Calbiochem® |
Synonyms | USP14 Inhibitor III, UCH-L5/UCH37 Inhibitor II, NSC687852, 3,5-bis((4-Nitrophenyl)methylidene)-1-prop-2-enoylpiperidin-4-one, (3E,5E)-1-Acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one |
References | |
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References | D'Arcy, P., et al. 2011. Nat. Med. 17, 1636. |
Product Information | |
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CAS number | 1009817-63-3 |
Form | Yellow powder |
Hill Formula | C₂₂H₁₇N₃O₆ |
Chemical formula | C₂₂H₁₇N₃O₆ |
Structure formula Image | |
Quality Level | MQ100 |
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Biological Information | |
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Purity | ≥97% by HPLC |
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Packaged under inert gas | Packaged under inert gas |
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Specifications |
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Global Trade Item Number | |
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Catalogue Number | GTIN |
662140 | 0 |
Documentation
DUB Inhibitor IV, b-AP15 - CAS 1009817-63-3 - Calbiochem Certificates of Analysis
Title | Lot Number |
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662140 |
References
Reference overview |
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D'Arcy, P., et al. 2011. Nat. Med. 17, 1636. |
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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