Batimastat (BB-94)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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
- 1. Georg Jocher , Vincent Grass, et al. "ADAM10 and ADAM17 promote SARS‐CoV‐2 cell entry and spike protein‐mediated lung cell fusion." EMBO Rep. 2022 Jun 7;23(6):e54305. PMID: 35527514
- 2. Miri Morgulis, Mark R Winter, et al. "VEGF signaling activates the matrix metalloproteinases, MmpL7 and MmpL5 at the sites of active skeletal growth and MmpL7 regulates skeletal elongation." Dev Biol. 2021 May;473:80-89. PMID: 33577829
- 3. Zhijun Liu, Himani Nailwal, et al. "A class of viral inducer of degradation of the necroptosis adaptor RIPK3 regulates virus-induced inflammation." Immunity. 2021 Feb 9;54(2):247-258.e7. PMID: 33444549
- 4. Chan ZC, Kwan HR, et al. "Site-directed MT1-MMP trafficking and surface insertion regulate AChR clustering and remodeling at developing NMJs." Elife. 2020;9:e54379. PMID: 32208136
- 5. Xi Y, Huang H, et al. "Tissue inhibitor of metalloproteinase 1 suppresses growth and differentiation of osteoblasts and differentiation of osteoclasts by targeting the AKT pathway." Exp Cell Res. 2020;111930. PMID: 32113948
- 6. Karpova D, Rettig MP, et al. "Targeting VLA4 integrin and CXCR2 mobilizes serially repopulating hematopoietic stem cells." J Clin Invest. 2019 May 14;130:2745-2759. PMID: 31085833
- 7. Clarke C, Gallagher C, et al. "Transcriptomic analysis of IgG4 Fc-fusion protein degradation in a panel of clonally-derived CHO cell lines using RNASeq."Biotechnol Bioeng. 2019 Jun;116(6):1556-1562. PMID: 30802296
- 8. Lin CC, Kurashige M, et al. "A cleavage product of Polycystin-1 is a mitochondrial matrix protein that affects mitochondria morphology and function when heterologously expressed." Sci Rep. 2018 Feb 9;8(1):2743. PMID: 29426897
- 9. Lertudomphonwanit C, Mourya R, et al. "Large-scale proteomics identifies MMP-7 as a sentinel of epithelial injury and of biliary atresia." Sci Transl Med. 2017 Nov 22;9(417). PMID: 29167395
- 10. Kidacki M, Lehman HL, et al. "p120-Catenin Downregulation and PIK3CA Mutations Cooperate to Induce Invasion through MMP1 in HNSCC." Mol Cancer Res. 2017 Oct;15(10):1398-1409. PMID: 28637905
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| Physical Appearance | A solid |
| Storage | Store at 4°C |
| M.Wt | 477.64 |
| Cas No. | 130370-60-4 |
| Formula | C23H31N3O4S2 |
| Synonyms | Batimastat, BB-94 |
| Solubility | ≥23.88 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | (2S,3R)-N1-hydroxy-3-isobutyl-N4-((S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl)-2-((thiophen-2-ylthio)methyl)succinamide |
| SDF | Download SDF |
| Canonical SMILES | CNC([C@@H](NC([C@@H]([C@H](CSC1=CC=CS1)C(NO)=O)CC(C)C)=O)CC2=CC=CC=C2)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 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. |
|
| 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 | |
质量控制和MSDS
- 批次：
化学结构
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