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Batimastat sodium salt

Catalog No. T10461   CAS 130464-84-5
Synonyms: BB-94 sodium salt

Batimastat (BB-94) sodium salt is a broad-spectrum MMP inhibitor (IC50s: 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7, and MMP-3).

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Batimastat sodium salt Chemical Structure
Batimastat sodium salt, CAS 130464-84-5
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Batimastat (BB-94) sodium salt is a broad-spectrum MMP inhibitor (IC50s: 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7, and MMP-3).
Targets&IC50 MMP1:3 nM , MMP7:6 nM , MMP2:4 nM , MMP9:4 nM , MMP3:20 nM
In vitro Batimastat inhibits gelatinases A and B (IC50s: 4 nM and 10 nM). The IC50 with the structurally similar collagenase Ht-d is 6 nM, which is comparable with values for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM) [2]. CD30 shedding from the cell line Karpas299 can effectively be blocked by the hydroxamic acid-based metalloproteinase inhibitor Batimastat (IC50: 230 nM) [3].
In vivo Matrix density in animals treated with saline or Batimastat (40 mg/kg) is analyzed 4 hours post-E2 administration, a critical point when collagen density notably decreases following hormone treatment [6]. Batimastat intraperitoneally administers to restrict human ovarian carcinoma xenografts and murine melanoma metastasis, alongside delaying primary tumor growth in human breast cancer models without inducing cytotoxicity or affecting mRNA levels [2]. Exhibiting antineoplastic and antiangiogenic effects across tumor models, Batimastat's concomitant application with Cisplatin (60 mg/kg i.p. bi-daily for 8 injections and 4 mg/kg i.v. every 7 days for 3 injections, respectively) effectively halts growth and dissemination of xenografts, maintaining all subjects' health up to day 200 [4]. Furthermore, Kaplan-Meier survival analysis (48 hours) highlights a significant survival rate increase to 95.2% in Batimastat-treated animals versus 75% in controls, with statistical relevance nearing significance (p=0.064) [5].
Kinase Assay 6. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.
Cell Research http://www.ncbi.nlm.nih.gov/pubmed/19889233
Synonyms BB-94 sodium salt
Molecular Weight 500.63
Formula C23H31N3NaO4S2
CAS No. 130464-84-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Yin Z, 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, 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. Hansen HP, et al. Inhibition of metalloproteinases enhances the internalization of anti-CD30 antibody Ki-3 and the cytotoxic activity of Ki-3 immunotoxin. Int J Cancer. 2002 Mar 10;98(2):210-5. 4. Giavazzi R, et al. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xenografts. Clin Cancer Res. 1998 Apr;4(4):985-92. 5. Ricci S, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014 Dec 31;14:726.

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Keywords

Batimastat sodium salt 130464-84-5 Proteases/Proteasome MMP Batimastat sodium BB-94 sodium BB-94 sodium salt inhibitor inhibit

 

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