BAMB-4

BAMB-4

Catalog Number:
L002370624APE
Mfr. No.:
APE-B4715
Price:
$426
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      • Overview
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          Background

          BAMB-4 is an inhibitor of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA) with an IC50 value of 20 µM [1].ITPKA is an InsP3 kinase. It binds to actin filaments and bundles them. This protein regulates actin dynamics as well as inositol phosphate signaling [1].BAMB-4 was almost completely taken up by H1299 cells. BAMB-4 did not belong to typical kinase inhibitors. Its relatively high specificity and high cellular uptake provide the possibility to effectively inhibit InsP3 kinase in vivo. Among InsP3Kinase inhibitors, BAMB-4 exhibit the lowest inhibition frequency. BAMB-4 showed an inhibitory effect only in 1 from 42 tested targets. There was no detected BAMB-4 target in kinase screens. These results indicated that BAMB-4 is not a typical kinase inhibitor. In vitro, data showed that BAMB-4 increased Km and reduced Vmax with respect to InsP3. BAMB-4 at the lowest concentration (10 µM) increased the Km-value for InsP3 by 160%. BAMB-4 at elevated concentrations did not further rise the Km-value for InsP3. BAMB-4 dose-dependently decreased Vmax from 75% to 50%. Decreased Vmax and increased Km in presence of inhibitor indicated that BAMB-4 might belong to mixed type inhibitors. Data showed that BAMB-4 also reduced Vmax and increased Km with respect to ATP [2].There is still no any available result of the application of BAMB-4 in animals.

          [1]. Schrder D, Tdter K, Gonzalez B, et al. The new InsP 3 Kinase inhibitor BIP-4 is competitive to InsP 3 and blocks proliferation and adhesion of lung cancer cells. Biochemical pharmacology, 2015, 96(2): 143-150.
          [2]. Schrder D, Rehbach C, Seyffarth C, et al. Identification of a new membrane-permeable inhibitor against inositol-1, 4, 5-trisphosphate-3-kinase A. Biochemical and biophysical research communications, 2013, 439(2): 228-234.

      • Properties
        • Alternative Name
          N-(benzo[d]isoxazol-3-yl)-4-methylbenzamide
          CAS Number
          891025-25-5
          Molecular Formula
          C15H12N2O2
          Molecular Weight
          252.27
          Appearance
          A solid
          Purity
          98.67%
          Solubility
          insoluble in H2O; insoluble in EtOH; ≥7.8 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Pan C, Jin L, et al. "Inositol-triphosphate 3-kinase B confers cisplatin resistance by regulating NOX4-dependent redox balance." J Clin Invest. 2019 May 13;129(6):2431-2445. PMID:31081803

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