426100
Lactacystin
≥99% (HPLC), solid, proteasome inhibitor, Calbiochem®
別名:
Lactacystin, Synthetic, Proteasome Inhibitor VI
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この商品について
実験式（ヒル表記法）:
C15H24N2O7S
CAS番号:
分子量:
376.43
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
製品名
Lactacystin, Synthetic, Lactacystin, Synthetic, CAS 1258004-00-0, is an irreversible inhibitor of 20S proteasome inhibitor (IC50 = 500 nM). A covalent inhibitor of the chymotrypsin & trypsin-like activities of proteasome.
Quality Level
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
DMSO: 50 mg/mL, water: soluble
shipped in
ambient
storage temp.
−20°C
SMILES string
S(C[C@H](NC(=O)C)C(=O)O)C(=O)[C@]1(NC(=O)[C@@H]([C@@H]1O)C)[C@@H](O)C(C)C
InChI
1S/C15H24N2O7S/c1-6(2)10(19)15(11(20)7(3)12(21)17-15)14(24)25-5-9(13(22)23)16-8(4)18/h6-7,9-11,19-20H,5H2,1-4H3,(H,16,18)(H,17,21)(H,22,23)/t7-,9+,10+,11+,15+/m1/s1
InChI key
DAQAKHDKYAWHCG-AFGIITKNSA-N
General description
An irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex) (IC50 = 500 nM for 20S proteasome). Blocks proteasome activity by targeting the catalytic β-subunit. Acts as a covalent inhibitor of the chymotrypsin- and trypsin-like activities of the proteasome. Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells and inhibits progression of synchronized Neuro 2A cells and MG-63 human osteosarcoma cells beyond the G1 phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC50 = 10 µM).
Biochem/physiol Actions
Cell permeable: no
Primary Target
20S proteasome (MCP; multicatalytic proteinase complex)
20S proteasome (MCP; multicatalytic proteinase complex)
Product does not compete with ATP.
Reversible: no
Target IC50: 500 nM against 20S proteasome; 10 µM against NF-κB activation
Preparation Note
Following reconstitution in DMSO, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Unstable in aqueous solutions; reconstitute in H₂O just prior to use.
Other Notes
Keyomarsi, K., et al. 2011. Cell. Biol. Toxicol.27, 123.
Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem.31, 279.
Dick, L.R., et al. 1996. J. Biol. Chem.271, 7273.
Oda, K., et al. 1996. Biochem. Biophys. Res.Commun.219, 800.
Fenteany, G., et al. 1995. Science268, 726.
Imajoh-Ohmi, S., et al. 1995. Biochem.Biophys. Res. Commun.217, 1070.
Jensen, T.J., et al. 1995. Cell 83, 129.
Katagiri, M.M., et al. 1995. J. Antibiot.48, 344.
Mori, S., et al. 1995. J. Biol. Chem.270, 29447.
Tanaka, H., et al. 1995. Biochem. Biophys. Res. Commun.216, 291.
Fenteany, G., et al. 1994. Proc. Natl. Acad.Sci. USA91, 3358.
Omura, S., et al. 1991. J. Antibiot.44, 117.
Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem.31, 279.
Dick, L.R., et al. 1996. J. Biol. Chem.271, 7273.
Oda, K., et al. 1996. Biochem. Biophys. Res.Commun.219, 800.
Fenteany, G., et al. 1995. Science268, 726.
Imajoh-Ohmi, S., et al. 1995. Biochem.Biophys. Res. Commun.217, 1070.
Jensen, T.J., et al. 1995. Cell 83, 129.
Katagiri, M.M., et al. 1995. J. Antibiot.48, 344.
Mori, S., et al. 1995. J. Biol. Chem.270, 29447.
Tanaka, H., et al. 1995. Biochem. Biophys. Res. Commun.216, 291.
Fenteany, G., et al. 1994. Proc. Natl. Acad.Sci. USA91, 3358.
Omura, S., et al. 1991. J. Antibiot.44, 117.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
Yue Qu et al.
Microbiology spectrum, 11(3), e0037823-e0037823 (2023-04-07)
Several viruses have been shown to modulate the transcription factor nuclear factor erythroid 2-related factor 2 (NRF2), the master regulator of redox homeostasis. The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), responsible for the COVID-19 pandemic, also seems to disrupt
Andrew M Pickering et al.
The Biochemical journal, 432(3), 585-594 (2010-10-06)
Oxidized cytoplasmic and nuclear proteins are normally degraded by the proteasome, but accumulate with age and disease. We demonstrate the importance of various forms of the proteasome during transient (reversible) adaptation (hormesis), to oxidative stress in murine embryonic fibroblasts. Adaptation
Yiming Lei et al.
Autophagy, 17(12), 4423-4441 (2021-04-20)
The hepatitis B virus X protein (HBx) is involved in the process of hepatocellular carcinoma via the activation of various oncogenes. Our previous study indicated that ARBB1 (arrestin beta 1) promotes hepatocellular carcinogenesis (HCC). However, the role of ARRB1 in
グローバルトレードアイテム番号
| カタログ番号 | GTIN |
|---|---|
| 426100-200UGCN | 04055977187328 |
| 426100-400UGCN | 04055977187335 |
| 426100-1MGCN | 04055977187311 |