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Ceranib 1

Ceramidase inhibitor; antiproliferative CAS# 328076-61-5

Ceranib 1

Catalog No. BCC6186----Order now to get a substantial discount!

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Ceranib 1: 5mg $69 In Stock
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Chemical structure

Ceranib 1

3D structure

Chemical Properties of Ceranib 1

Cas No. 328076-61-5 SDF Download SDF
PubChem ID 5761166 Appearance Powder
Formula C26H21NO3 M.Wt 395.45
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name 3-[(E)-3-(4-methoxyphenyl)prop-2-enoyl]-6-methyl-4-phenyl-1H-quinolin-2-one
SMILES CC1=CC2=C(C=C1)NC(=O)C(=C2C3=CC=CC=C3)C(=O)C=CC4=CC=C(C=C4)OC
Standard InChIKey OJMCCNQNCSCAJV-RVDMUPIBSA-N
Standard InChI InChI=1S/C26H21NO3/c1-17-8-14-22-21(16-17)24(19-6-4-3-5-7-19)25(26(29)27-22)23(28)15-11-18-9-12-20(30-2)13-10-18/h3-16H,1-2H3,(H,27,29)/b15-11+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Ceranib 1

DescriptionCeramidase inhibitor; inhibits proliferation in SKOV3 ovarian carcinoma cells (IC50 = 3.9 μM). Induces accumulation of ceramide species and decreases sphingosine and sphingosine-1-phosphate (S1P) levels in SKOV3 cells.

Ceranib 1 Dilution Calculator

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Ceranib 1 Molarity Calculator

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Preparing Stock Solutions of Ceranib 1

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5288 mL 12.6438 mL 25.2876 mL 50.5753 mL 63.2191 mL
5 mM 0.5058 mL 2.5288 mL 5.0575 mL 10.1151 mL 12.6438 mL
10 mM 0.2529 mL 1.2644 mL 2.5288 mL 5.0575 mL 6.3219 mL
50 mM 0.0506 mL 0.2529 mL 0.5058 mL 1.0115 mL 1.2644 mL
100 mM 0.0253 mL 0.1264 mL 0.2529 mL 0.5058 mL 0.6322 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Ceranib 1

Discovery and evaluation of inhibitors of human ceramidase.[Pubmed:21885864]

Mol Cancer Ther. 2011 Nov;10(11):2052-61.

The ceramide/sphingosine-1-phosphate (S1P) rheostat has been hypothesized to play a critical role in regulating tumor cell fate, with elevated levels of ceramide inducing death and elevated levels of S1P leading to survival and proliferation. Ceramidases are key enzymes that control this rheostat by hydrolyzing ceramide to produce sphingosine and may also confer resistance to drugs and radiation. Therefore, ceramidase inhibitors have excellent potential for development as new anticancer drugs. In this study, we identify a novel ceramidase inhibitor (Ceranib-1) by screening a small molecule library and describe the synthesis of a more potent analogue (Ceranib-2). In a cell-based assay, both compounds were found to inhibit cellular ceramidase activity toward an exogenous ceramide analogue, induce the accumulation of multiple ceramide species, decrease levels of sphingosine and S1P, inhibit the proliferation of cells alone and in combination with paclitaxel, and induce cell-cycle arrest and cell death. In vivo, Ceranib-2 was found to delay tumor growth in a syngeneic tumor model without hematologic suppression or overt signs of toxicity. These data support the selection of ceramidases as suitable targets for anticancer drug development and provide the first nonlipid inhibitors of human ceramidase activity.

Description

Ceranib1 is a ceramidase inhibitor. Ceranib1 inhibits ceramidase activity toward an exogenous ceramide analog, induces the accumulation of multiple ceramide species, decreases levels of sphingosine and S1P. Ceranib1 inhibits the proliferation of ovarian cancer cells.

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