Batimastat (BB-94)
(Synonyms: 巴马司他; BB94) 目录号 : GC16530
Batimastat (BB-94)是一种有效的广谱基质金属蛋白酶（MMPs）抑制剂，能够抑制MMP-1，MMP-2，MMP-9，MMP-7和MMP-3，IC50值分别为3nM，4nM，4nM，6nM和20nM。
Cas No.:130370-60-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Batimastat (BB-94) is a potent broad-spectrum inhibitor of matrix metalloproteinases (MMPs), capable of inhibiting MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, with IC50 values of 3nM, 4nM, 4nM, 6nM and 20nM, respectively[1]. Batimastat (BB-94) belongs to the hydroxamic acid class of compounds, which can chelate zinc ions, thereby inhibiting the activity of MMPs[2]. Batimastat (BB-94) can cause cell cycle disturbances in ovarian cancer cells[3].
In vitro, Batimastat (BB-94) (5μM) treatment of hematological tumor cell lines (HL-60, F36P, H929 cells) for 48h reduced cell viability and cell density, and significantly increased intracellular ERK1/2 phosphorylation[4].
In vivo, Batimastat (BB-94) (5, 10, 20mg/kg) treated with intraperitoneal injection in rats with colitis improved the inflammation score and reduced myeloperoxidase (MPO) activity in a dose-dependent manner[5]. Batimastat (BB-94) (30mg/kg) treated with intraperitoneal injection in rats with periodontal disease significantly increased periodontal bone destruction and had a deleterious effect on the progression of periodontal disease[6].
References:
[1] Yin Z, Sada A A, Reslan O M, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones[J]. American Journal of Physiology-Endocrinology and Metabolism, 2012, 303(1): E55-E70.
[2] Ferry G, Boutin J A, Hennig P, et al. A zinc chelator inhibiting gelatinases exerts potent in vitro anti-invasive effects[J]. European journal of pharmacology, 1998, 351(2): 225-233.
[3] Erba E, Ronzoni S, Bassano L, et al. The metalloproteinase inhibitor batimastat (BB-94) causes cell cycle phase perturbations in ovarian cancer cells[J]. Annals of Oncology, 1999, 10(5): 589-591.
[4] Alves R, Pires A, Jorge J, et al. Batimastat Induces Cytotoxic and Cytostatic Effects in In Vitro Models of Hematological Tumors[J]. International Journal of Molecular Sciences, 2024, 25(8): 4554.
[5] Di Sebastiano P, Di Mola F F, Artese L, et al. Beneficial effects of Batimastat (BB-94), a matrix metalloproteinase inhibitor, in rat experimental colitis[J]. Digestion, 2001, 63(4): 234-239.
[6] Björnsson M J, Havemose‐Poulsen A, Stoltze K, et al. Influence of the matrix metalloproteinase inhibitor batimastat (BB‐94) on periodontal bone destruction in Sprague‐Dawley rats[J]. Journal of periodontal research, 2004, 39(4): 269-274.
Batimastat (BB-94)是一种有效的广谱基质金属蛋白酶（MMPs）抑制剂，能够抑制MMP-1，MMP-2，MMP-9，MMP-7和MMP-3，IC50值分别为3nM，4nM，4nM，6nM和20nM[1]。Batimastat (BB-94)属于羟肟酸类化合物，能够螯合锌离子，从而抑制MMPs的活性[2]。Batimastat (BB-94)能够引起卵巢癌细胞的细胞周期扰动[3]。
在体外，Batimastat (BB-94)（5μM）处理血液肿瘤细胞系（HL-60, F36P, H929细胞）48h，降低了细胞活力和细胞密度，显著增加了细胞内ERK1/2磷酸化[4]。
在体内，Batimastat (BB-94)（5, 10, 20mg/kg）通过腹腔注射治疗结肠炎大鼠，以剂量依赖性方式改善了炎症评分，降低了髓过氧化物酶（MPO）活性[5]。Batimastat (BB-94)（30mg/kg）通过腹腔注射治疗牙周病大鼠，显著增加了牙周骨破坏，对牙周病的进展具有有害影响[6]。
| Cell experiment [1]: | |
Cell lines | HL-60, F36P, H929 cells |
Preparation Method | Cells were incubated with 5µM Batimastat (BB-94) for 48h, and the levels of phosphorylated ERK1/2 were measured by immunoblotting. |
Reaction Conditions | 5µM; 48h |
Applications | The exposure to 5µM of Batimastat (BB-94) leads to a significant increase in ERK1/2 phosphorylation in HL-60, F36P, and H929 cells. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Colitis was induced in 40 rats by intracolonic administration of trinitrobenzensulfonic acid (TNB). Animals were divided into four groups of ten rats each: group 1 received only intracolonic TNB, group 2 received TNB+5mg/kg intraperitoneal Batimastat (BB-94), group 3 TNB+10mg/kg Batimastat (BB-94) and group 4 TNB+20mg/kg Batimastat (BB-94). The MMP inhibitor was administered 30min before induction of colitis and twice daily until death. Ten rats receiving only intracolonic 0.9% saline served as controls. Animals were killed after seven days; segments of colon were removed and used for histological score of inflammation and myeloperoxidase (MPO) activity. |
Dosage form | 5, 10, 20mg/kg; i.p. |
Applications | Treatment with Batimastat (BB-94) has dose-dependent beneficial effects on the inflammatory alterations in rat experimental colitis. |
References: | |
| Cas No. | 130370-60-4 | SDF | |
| 别名 | 巴马司他; BB94 | ||
| 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 | ||
| 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 | ||
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0936 mL | 10.4681 mL | 20.9363 mL |
| 5 mM | 0.4187 mL | 2.0936 mL | 4.1873 mL |
| 10 mM | 0.2094 mL | 1.0468 mL | 2.0936 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet