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product name
乳胞素，合成, 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.
质量水平
检测方案
≥99% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
white
溶解性
DMSO: 50 mg/mL
water: soluble
运输
ambient
储存温度
−20°C
一般描述
一种不可逆的蛋白酶体抑制剂。一种链霉菌代谢物，可作为20S蛋白酶体（MCP；多催化蛋白酶复合物）的高度特异性抑制剂（20S蛋白酶体的IC50 =500 nM）。通过靶向催化β-亚基阻断蛋白酶体活性。作为蛋白酶体的胰凝乳蛋白酶和胰蛋白酶样活性的共价抑制剂。诱导Neuro 2A小鼠神经母细胞瘤细胞中的神经突生长超出细胞周期G1期。据报告可诱导人原单核细胞U937细胞发生凋亡。也抑制NF-κB的活化（IC50 = 10 µM）
一种不可逆的蛋白酶体抑制剂。一种链霉菌代谢物，可作为20S蛋白酶体（MCP；多催化蛋白酶复合物）的高度特异性抑制剂（20S蛋白酶体的IC50 =500 nM）。通过靶向催化β-亚基阻断蛋白酶体活性。作为蛋白酶体的胰凝乳蛋白酶样和胰蛋白酶样活性的共价抑制剂。诱导Neuro 2A小鼠神经母细胞瘤细胞中的神经突生长，并抑制同步Neuro 2A细胞和MG-63人骨肉瘤细胞的进程超过细胞周期G1期。据报告可诱导人原单核细胞U937细胞发生凋亡。也抑制NF-κB的活化（IC50 = 10 µM）。
生化/生理作用
主要靶标
20S蛋白酶体（MCP；多催化蛋白酶复合物）
20S蛋白酶体（MCP；多催化蛋白酶复合物）
产物不与ATP竞争。
可逆：否
细胞渗透性：否
靶标IC50：20S蛋白酶体为500 nM；NF-κB活化为10 µM
警告
毒性：标准处理（A）
重悬
在DMSO中复溶后，等分并冷冻保存（-20°C）。DMSO贮备液在-20°C可稳定保存长达 1 个月。在水溶液中不稳定；使用前在H₂O中复溶。
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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