| Identification | Back Directory | [Name]
DBIBB | [CAS]
1569309-92-7 | [Synonyms]
DBIBB
Benzoic acid, 2-[[[4-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)butyl]amino]sulfonyl]- | [Molecular Formula]
C23H20N2O6S | [MOL File]
1569309-92-7.mol | [Molecular Weight]
452.48 |
| Hazard Information | Back Directory | [Uses]
DBIBB is a non-lipid agonist of LPA2 (lysophosphatidic acid receptor 2), protecting rat intestinal crpyt epithelium-like IEC-6 cells against caspase 3/7 activation and apoptosis. | [Biological Activity]
dbibb, a butylsulfamoyl benzoic acid analog, is a non-lipid agonist of lpa2 with an ec50 of 0.10 μm. dbibb has no effect at other lpa receptor subtypes [1]. the bioactive phospholipid lysophosphatidic acid (lpa) has been involved in stimulating cell proliferation, migration and survival by acting on its cognate g-protein-coupled receptors. aberrant lpa production, receptor expression and signalling probably contribute to cancer initiation, progression and metastasis [2]. | [in vitro]
dbibb treatment postirradiation significantly (p< 0.01) increased the clonogenic survival of iec-6 cells in the 2-6 gy dose range. dbibb reduced dna fragmentation 4hr after irradiation in a dose dependent manner. dbibb also reduced caspase 3/7 activity and dna fragmentation in lpa2mef treated with adriamycin. in purified cd34+ progenitor cells, dbibb significantly increased the total number of colonies and specifically enhanced the survival of the granulocyte/macrophage lineages [1]. | [in vivo]
using a murine gi-ars mice model of partial-body irradiation (pbi) with shielding of the bone marrow contained in the tibiae, fibulae, and paws, administrations of up to 10 mg/kg of dbibb for 10 days showed no visually observable adverse effects and pathological findings at necropsy, indicating the lack of toxicity. the group that received 10 mg/kg dbibb showed a significant increase in survival. in c57bl/6 mice, dbibb showed a dose-dependent increase in the number of surviving crypts compared with the vehicle control [1]. | [storage]
Store at -20°C | [References]
[1] patil r, szabó e, fells j i, et al. combined mitigation of the gastrointestinal and hematopoietic acute radiation syndromes by an lpa 2 receptor-specific nonlipid agonist[j]. chemistry & biology, 2015, 22(2): 206-216.
[2] mills g b, moolenaar w h. the emerging role of lysophosphatidic acid in cancer[j]. nature reviews cancer, 2003, 3(8): 582-591. |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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