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General description
A cell-permeable, active metabolite of Sulindac (Cat. No. 574100). Strongly inhibits Ras-induced malignant transformation and Ras/Raf-dependent transactivation. Also decreases the Ras-induced activation of c-Raf-1 kinase. Inhibits growth and induces apoptosis in prostate cancer cell lines. Selectively inhibits COX-1 (ID50 = 500 nM) compared to prostaglandin H synthase-2 (PGHS-2; COX-2; ID50 = 14 µM). Preferentially inhibits the secretion of Aβ42 in CHO cells stably transfected with both APP75, and the PS1 mutant M146L.
An active metabolite of the non-steroidal anti-inflammatory drug Sulindac (Cat. No. 574100). Inhibits Ras signaling. Strongly inhibits Ras-induced malignant transformation and Ras/Raf-dependent transactivation. Also decreases the Ras-induced activation of c-Raf-1 kinase. Inhibits cell growth and induces apoptosis in a time-and dose-dependent manner. Selectively inhibits prostaglandin H synthase-1 (PGHS-1; COX-1; ID50 = 0.5 µM) relative to prostaglandin H synthase-2 (PGHS-2; COX-2; ID50 = 14 µM). Reduces Aβ42 production independently of COX inhibition.
Biochem/physiol Actions
Cell permeable: yes
ID50 = 500 nM against COX-1
Product does not compete with ATP.
Reversible: no
Other Notes
Weggen, S., et al. 2001. Nature414, 212.
Lim, J.T., et al. 1999. Biochem. Pharmacol. 58, 1097.
Herrmann, C., et al. 1998. Oncogene 17, 1769.
Picariello, L., et al. 1998. Eur. J. Pharmacol. 360, 105.
Arber, N., et al. 1997. Gastroenterology 113, 1892.
Meade, E.A., et al. 1993. J. Biol. Chem. 268, 6610.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful & Carcinogenic / Teratogenic (E)
| Quality Segment | 100 |
| assay | ≥98% (TLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze |
| color | yellow-orange |
| solubility | DMSO: 25 mg/mL,ethanol: 5 mg/mL |
| shipped in | ambient |
| storage temp. | 10-30°C |
| SMILES string | Fc1cc2c(cc1)\C(=C\c3ccc(cc3)SC)\C(=C2CC(=O)O)C |
| InChI | 1S/C20H17FO2S/c1-12-17(9-13-3-6-15(24-2)7-4-13)16-8-5-14(21)10-19(16)18(12)11-20(22)23/h3-10H,11H2,1-2H3,(H,22,23)/b17-9+ |
| InChI key | LFWHFZJPXXOYNR-RQZCQDPDSA-N |
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¥ 2707.32
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¥ 1259.40
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¥ 9207.92
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¥ 3372.68
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¥ 4968.78
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¥ 15214.65
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¥ 2268.97
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¥ 3319.60
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