质量水平
检测方案
≥98% (HPLC)
形式
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
运输
wet ice
储存温度
−20°C
SMILES字符串
[H]C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCc1ccccc1
InChI
1S/C26H41N3O5/c1-17(2)12-21(15-30)27-24(31)22(13-18(3)4)28-25(32)23(14-19(5)6)29-26(33)34-16-20-10-8-7-9-11-20/h7-11,15,17-19,21-23H,12-14,16H2,1-6H3,(H,27,31)(H,28,32)(H,29,33)/t21-,22-,23-/m0/s1
InChI key
TZYWCYJVHRLUCT-VABKMULXSA-N
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Amino Acid Sequence
Z-Leu-Leu-Leu-al
一般描述
高效、可逆和细胞可透过性蛋白酶体抑制剂（(Ki = 4 nM）。可通过26S复合物降低哺乳动物细胞和酵母可渗透菌株中泛素结合蛋白的降解，而不会影响其ATP酶或异肽酶的活性。可激活c-Jun N端激酶（JNK1）、抑制NF-κB的活化（IC50 = 3 µM）。
生化/生理作用
产品不与ATP竞争。
可逆性：是
细胞渗透性：是
靶标IC50：3 µM抑制NF-κB活化
靶标Ki：4 nM作为蛋白酶体抑制剂
包装
用惰性气体包装
警告
毒性：刺激性（B）
外形
10 mM（1 mg/210 µl）或（5 mg/1050 l）MG-132 DMSO溶液（货号474790）提供。
其他说明
Meriin, A.B., et al. 1998.J. Biol. Chem.273, 6373.
Adams, J., and Stein, R. 1996.Ann.Rep.Med. Chem.31, 279.
Lee, D.H., and Goldberg, A.L.1996.J. Biol. Chem.271, 27280.
Wiertz, E.J.H.J., et al. 1996.Cell84, 769.
Read, M.A., et al. 1995.Immunity2, 493.
Rock, K.L., et al. 1994.Cell78, 761.
Adams, J., and Stein, R. 1996.Ann.Rep.Med. Chem.31, 279.
Lee, D.H., and Goldberg, A.L.1996.J. Biol. Chem.271, 27280.
Wiertz, E.J.H.J., et al. 1996.Cell84, 769.
Read, M.A., et al. 1995.Immunity2, 493.
Rock, K.L., et al. 1994.Cell78, 761.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
闪点(°F)
188.6 °F
闪点(°C)
87 °C
D H Lee et al.
The Journal of biological chemistry, 271(44), 27280-27284 (1996-11-01)
We have studied whether various agents that inhibit purified yeast and mammalian 26 S proteasome can suppress the breakdown of different classes of proteins in Saccharomyces cerevisiae. The degradation of short-lived proteins was inhibited reversibly by peptide aldehyde inhibitors of
E J Wiertz et al.
Cell, 84(5), 769-779 (1996-03-08)
Human cytomegalovirus (HCMV) down-regulates expression of MHC class I products by selective proteolysis. A single HCMV gene, US11, which encodes an endoplasmic reticulum (ER) resident type-I transmembrane glycoprotein, is sufficient to cause this effect. In US11+cells, MHC class I molecules
Clarissa Braun et al.
Cell stress, 5(12), 176-182 (2021-12-18)
Programmed cell death protein 4 (PDCD4) exerts critical functions as tumor suppressor and in immune cells to regulate inflammatory processes. The phosphoinositide 3-kinase (PI3K) promotes degradation of PDCD4 via mammalian target of rapamycin complex 1 (mTORC1). However, additional pathways that
A B Meriin et al.
The Journal of biological chemistry, 273(11), 6373-6379 (1998-04-16)
Inhibition of the major cytosolic protease, proteasome, has been reported to induce programmed cell death in several cell lines, while with other lines, similar inhibition blocked apoptosis triggered by a variety of harmful treatments. To elucidate the mechanism of pro-
Jackie Cheng et al.
Antibodies (Basel, Switzerland), 9(3) (2020-09-24)
Amplification and overexpression of HER2 (human epidermal growth factor receptor 2), an ErbB2 receptor tyrosine kinase, have been implicated in human cancer and metastasis. A bispecific tetravalent anti-HER2 antibody (anti-HER2-Bs), targeting two non-overlapping epitopes on HER2 in domain IV (trastuzumab)
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