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Bestatin

CAS号

58970-76-6

分子式

C16H24N2O4

主要靶点

Aminopeptidase|Antibacterial|Antibiotic|LTR|Others

仅限科研使用

Cat No : CM00764

Print datasheet

Synonyms

Antibiotic|Aminopeptidase|APN|Bacterial|Bestatin|Ubenimex|乌苯美司|inhibit|Inhibitor|LTA(4)H-h

验证数据展示

  • CAS No.: 58970-76-6

    Bestatin
    CAS#: 58970-76-6

产品信息

CAS号 58970-76-6
分子式 C16H24N2O4
主要靶点 Aminopeptidase|Antibacterial|Antibiotic|LTR|Others
主要通路 微生物学|代谢|微生物学|免疫与炎症
分子量 308.37
纯度 100%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Antibiotic|Aminopeptidase|APN|Bacterial|Bestatin|Ubenimex|乌苯美司|inhibit|Inhibitor|LTA(4)H-h

体内活性

Bestatin对SN12M细胞侵入重组基底膜（基质胶）具有浓度依赖性的抑制作用。在非肿瘤条件培养基中,其还可浓度依赖性抑制肿瘤细胞IV型胶原退化。在U937细胞中,乌苯美司可使caspase-3的活性增强并诱导DNA梯和DNA片段化。在SN12M Bestatin抑制氨基肽酶底物的水解活性。Bestatin对人脐静脉内皮细胞中的管状形成具有抑制作用。通过固定在细胞表面的亮氨酸氨肽酶,Bestatin直接刺激淋巴细胞（和单核细胞）,而间接刺激则是通过氨基肽酶乙抑制吞噬作用激素的分解代谢发挥。

体外活性

在B16-BL6黑色素瘤细胞荷瘤的小鼠背部侧中,Bestatin使既定原发性肿瘤块血管的数量下降.在小鼠背部气囊测定中,Bestatin显著抑制黑色素瘤细胞诱导的血管生成. 在EGDA大鼠中,Bestatin可降低EAC的发病率（57.7％降至26.1％）.在EGDA大鼠的食管组织中,Bestatin对白三烯B4生物合成的抑制具有明显的统计学意义.

溶解度

1eq. NaOH:15.4 mg/mL (49.94 mM);DMSO:10 mg/mL (32.43 mM)

细胞实验

Growing cells (1×106 to 2×106 cells/mL) are diluted to 1.0×103 cells/mL and transferred (3 mL) into a well in a 12-well multiwell plate (2.5-cm diameter/well). Cells are treated with 0, 10, 50, 100, 300, or 600 μM Bestatin and allowed to grow at 21°C shaking at 180 rpm for 48 h. A hemocytometer is used to measure cell density after 0, 24, and 48 h.

参考文献

1.Sekine K, et al. Leukemia, 1999, 13(5), 729-734.
2.Yoneda J, et al. Clin Exp Metastasis, 1992, 10(1), 49-59.
3.Aozuka Y, et al. Cancer Lett, 2004, 216(1), 35-42.
4.Mathé G, et al. Biomed Pharmacother, 1991, 45(2-3), 49-54.
5.Chen X, et al. J Natl Cancer Inst, 2003, 95(14), 1053-1061.
6.Jiang T Y, Feng X F, Fang Z, et al. PTEN deficiency facilitates the therapeutic vulnerability to proteasome inhibitor bortezomib in gallbladder cancer[J]. Cancer Letters. 2020
7.Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma[J]. Science Translational Medicine. 2020, 12(562).

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2