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Batimastat (BB-94)MMP抑制剂

Batimastat (BB-94)

产品编号:A2577
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规格 单价 库存 订购数量
10mM (in 1mL DMSO) ¥1,050.00 现货
1mg ¥500.00 现货
5mg ¥1,000.00 现货
10mg ¥1,500.00 现货
25mg ¥2,500.00 现货

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Sample solution is provided at 25 µL, 10mM.

引用文献

质量控制

化学结构

Batimastat

相关生物数据

Batimastat

相关生物数据

Batimastat

相关生物数据

Batimastat

相关生物数据

Batimastat

相关生物数据

Batimastat

相关生物数据

Batimastat

相关生物数据

Batimastat

Batimastat (BB-94) Dilution Calculator

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化学性质

CAS号 130370-60-4 SDF Download SDF
别名 Batimastat,BB-94
化学名 (2S,3R)-N1-hydroxy-3-isobutyl-N4-((S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl)-2-((thiophen-2-ylthio)methyl)succinamide
SMILES CNC([C@@H](NC([C@@H]([C@H](CSC1=CC=CS1)C(NO)=O)CC(C)C)=O)CC2=CC=CC=C2)=O
分子式 C23H31N3O4S2 分子量 477.64
溶解度 ≥23.88mg/mL in DMSO 储存条件 Store at 4°C
物理性状 A solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 Batimastat (BB-94)是一种有效的广谱基质金属蛋白酶(matrix metalloprotease,MMP)抑制剂,作用于MMP-1、MMP-2、MMP-9、MMP-7和MMP-3,IC50值分别为3 nM、4 nM、4 nM、6 nM和20 nM。
靶点 MMP-1 MMP-2 MMP-9 MMP-7 MMP-3  
IC50 3 nM 4 nM 4 nM 6 nM 20 nM  

实验操作

细胞实验:

细胞系

C170HM2和AP5LV细胞系

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

96 h;3.0 μg/ml

应用

在batimastat存在时的细胞增殖实验用MTT吸光度法进行评估。在无血清和含scrum培养基中培养的C170HM2和AP5LV细胞中,batimastat对细胞生长没有显著影响。

动物实验:

动物模型

人结肠癌原位移植裸鼠模型

剂量

30 mg/kg;i.p.

应用

BB-94引起原发肿瘤的中位重量从对照组中的293 mg(范围: 1141~124 mg)减少到BB-94治疗组中的144 mg(范围: 424~38 mg)(P < 0.001),并显著减少肿瘤侵入邻近组织的发生率,从对照组中发生率为67%(12/18)减少到BB-94治疗组中的35%(7/20)。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Watson S A, Morris T M, Robinson G, et al. Inhibition of organ invasion by the matrix metalloproteinase inhibitor batimastat (BB-94) in two human colon carcinoma metastasis models[J]. Cancer research, 1995, 55(16): 3629-3633.

[2] Wang X, Fu X, Brown P D, et al. Matrix metalloproteinase inhibitor BB-94 (batimastat) inhibits human colon tumor growth and spread in a patient-like orthotopic model in nude mice[J]. Cancer research, 1994, 54(17): 4726-4728.

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研究更新

2. Matrix metalloproteinase inhibitor batimastat alleviates pathology and improves skeletal muscle function in dystrophin-deficient mdx mice. Am J Pathol. 2010 Jul;177(1):248-60. doi: 10.2353/ajpath.2010.091176. Epub 2010 May 14.
Abstract
The treatment of batimastat, an inhibitor of MMPs, in mdx mice resulted in increased muscle force production in isometric contraction, augmented levels of sarcolemmal protein beta-dystroglycan and neuronal nitric oxide and reduced necrosis, infiltratiom of macrophages, centronucleated fibers, expression of embryonic myosin heavy chain in skeletal muscle and activation of mitogen-activated protein kinases and activator protein-1 in myofibers.
3. [Protective role of MMP-9 inhibitor batimastat in acute lung injury after cardiopulmonary bypass]. Zhonghua Wai Ke Za Zhi. 2010 Jan 1;48(1):57-61.
Abstract
Batimastat, a MMP-9 inhibitor, was investigated for protective effect in CPB-induced dog lung injury.
4. Effect of the metalloproteinase inhibitor batimastat in the systemic toxicity induced by Bothrops asper snake venom: understanding the role of metalloproteinases in envenomation. Toxicon. 2004 Mar 15;43(4):417-24.
Abstract
Batimastat, a metalloproteinase inhibitor, inhibited lethality of low dose venom and concentration-dependently delayed death induced by high dose venom in mice, which also inhibited venom-induced in vitro coagulant, in vivo defibrinogenating and hemorrhagic effects.
5. Increased stromal expression of murine urokinase plasminogen activator in a human breast cancer xenograft model following treatment with the matrix metalloprotease inhibitor, batimastat. Breast Cancer Res Treat. 2001 Aug;68(3):225-37.
Abstract
Batimastat, a MMP inhibitor, caused retardation of tumor growth with no regression in a human breast cancer xenograft model and significantly increased expression of uPA in tumors.

产品描述

Batimastat (BB-94)是一种合成的有效MMPs抑制剂,作用于MMP-1(interstitial collagenase)、MMP-2(72 kDa type IV collagenase)、MMP-9(92 kDa type IV collagenase)、MMP-7(matrilysin)和MMP-3(Stromelysin 1),作用的IC50值分别为3 nM、4 nM、4 nM、6 nM和20 nM。Batimastat是一个低分子量(MW = 478)的多肽样胶原蛋白底物类似物,由一个多肽骨架和一个异羟肟酸基团组成,分别与MMPs和具催化活性的Zn原子结合。在包括卵巢癌异种移植肿瘤和人结肠癌在内的多个肿瘤模型中,Batimastat展示了抗肿瘤和抗血管生成的活性。

参考文献:
1.  Bernard Davies, Peter D. Brown, Nick East, Michael J. Crimmin, and Frances R. Balkwill. A synthetic matrix metalloproteinase inhibitor decreases tumor burden and prolongs survival of mice bearing human ovarian carcinoma xenografts. Cancer Research 1993; 53: 2087-2091
2.  X. Wang, X. Fu, P.D. Brown, M. J. Crimmin, and R. M. Hoffman. Matrix metalloproteinase inhibitor BB-94 (batimastat) inhibits human colon tumor growth and spread in a patient-like orthotopic model in nude mice. Cancer Research 1994; 54: 4726-4728
3.  Raffaella Giavazzi, Angela Garofalo, Cristina Ferri, Valeria Lucchini, Elisabeth A. Bone, Stefania Chiari, Peter D. Brown, M. Ines Nicoletti, and Giulia Taraboletti. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xgenografts. Clinical Cancer Research 1998; 4: 985-992