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Batimastat

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Chemical Structure| 130370-60-4 同义名 : BB94
CAS号 : 130370-60-4
货号 : A633905
分子式 : C23H31N3O4S2
纯度 : 99%+
分子量 : 477.64
MDL号 : MFCD00866533
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(52.34 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+40% PEG 300+2% Tween 80+water 2 mg/mL

生物活性
靶点

  • MMP

    MMP-1, IC50:3 nM

    MMP-7, IC50:4 nM
描述 Matrix metalloproteinases (MMPs) play important roles in tumor invasion, metastasis, and angiogenesis. Batimastat is a synthetic, low molecular weight, hydroxamate-based inhibitor of MMPs. It inhibited MMP-1, 2, 3, 9, 13, and 14 with IC50 values of 0.99, 0.73, 0.56, 0.60, 5.0, and 4.6 nM, respectively. It also blocked the activity of TNF-α converting enzyme with an IC50 value of 14.9 nM[3]. Batimastat showed less inhibitory effect on the processing of CD23, a low affinity IgE receptor, with an IC50 value of 100 nM[4]. In athymic mice inoculated with MDA435/LCC6 human breast cancer cells, daily injection of 50 mg/kg batimastat for 28 days significantly reduced tumor volumes relative to vehicle-treated controls[5].
作用机制 Batimastat inhibits the activity of MMPs via binding the zinc ion in the catalytic site of MMPs.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Sf9 insect cells Function assay Inhibition of human matrix metalloprotease-2 expressed in Sf9 insect cells, IC50=0.013 μM 15582436
Sf9 insect cells Function assay Inhibition of human matrix metalloprotease-9 expressed in Sf9 insect cells, IC50=0.025 μM 15582436
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.94mL

4.19mL

2.09mL
参考文献

[1]Yin Z, Sada AA, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70.

[2]Botos I, Scapozza L, et al. Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54.

[3]Fray MJ, Burslem MF, Dickinson RP. Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality. Bioorg Med Chem Lett. 2001 Feb 26;11(4):567-70. doi: 10.1016/s0960-894x(00)00719-8. PMID: 11229773.

[4]Bailey S, Bolognese B, Buckle DR, Faller A, Jackson S, Louis-Flamberg P, McCord M, Mayer RJ, Marshall LA, Smith DG. Selective inhibition of low affinity IgE receptor (CD23) processing. Bioorg Med Chem Lett. 1998 Jan 6;8(1):29-34. doi: 10.1016/s0960-894x(97)10149-4. PMID: 9871623.

[5]Low JA, Johnson MD, Bone EA, Dickson RB. The matrix metalloproteinase inhibitor batimastat (BB-94) retards human breast cancer solid tumor growth but not ascites formation in nude mice. Clin Cancer Res. 1996 Jul;2(7):1207-14. PMID: 9816289.