- 商品介绍
- 规格参数
- 包装参数
General description
A cell-permeable benzothiazolylchromenone compound that disrupts Skp2-Skp1 interaction via direct Skp2 affinity binding and selectively prevents Skp2-, but not Fbw7- or β-TrCP-, Skp1-Cullin-1-F-box (SFC) complex-mediated substrates ubiquitination both in cell-free systems and in cultures, effectively preventing ubiquitination-dependent activation (Akt) and degradation (p21 & p27) of Skp2 substrates with concomitant down-regulation of cellular Skp2 protein level (10 to 20 µM in HEK293T & PC3 cultures). Exhibits antiproliferation activity toward a panel of 8 cancer (IC50 from 1.22 to 10.5 µM), but not normal PNT1A epithelial or IMR90 fibroblast, lines and effectively reduces ALDH+ cancer stem cell (CSC; Cancer Initiating Cell) population in prostate cancer PC3 cultures (10 to 20 µM) by promoting p53-independent senescence and blocking Akt-dependent aerobic glycolysis. Exhibits good pharmacokinetic property (tmax = 1 h; t1/2 >6 h; Cmax >1 µM/plasma and >4 µM/tumor in 200 mm3 PC3 tumor-bearing mice; 80 mg/kg i.p.) and is efficacious in suppressing A549 and PC3 tumor growth in mice (40 to 80 mg/kg/d i.p.) in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Skp2
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Use only fresh DMSO for reconstitution.
Other Notes
Chan, C.H., et al. 2013 Cell154, 556.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥98% (HPLC) |
| Quality Segment | 100 |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | beige |
| solubility | DMSO: 5 mg/mL |
| storage temp. | 2-8°C |
| 长度(mm) | |
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| 重量(kg) |
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¥ 4862.67
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¥ 1125.70
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¥ 2757.88
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¥ 3408.16
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¥ 3254.04
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¥ 1756.15
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