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Purity: ≥98%
Cytosporone B (Dothiorelone G; Csn-B) is a naturally occurring octaketide isolated from an endophytic fungus Cytospora sp, acting as an agonist for the nuclear orphan receptor Nur77 (EC50 = 0.278 nM) with antitumor activity. Nuclear orphan receptor Nur77 has important roles in many biological processes. Csn-B binds specifically to the ligand-binding domain of Nur77 with high affinity (IC50=0.278 nM) and stimulates Nur77-dependent transactivational activity towards target genes including Nr4a1 (Nur77) itself, which contains multiple consensus response elements allowing positive autoregulation in a Csn-B-dependent manner. Csn-B also elevates blood glucose levels in fasting C57 mice, an effect that is accompanied by induction of multiple genes involved in gluconeogenesis.
| ln Vitro |
Cytosporone B specifically enhances Nur77's transactivational activity by targeting the ligand binding region of Nur77. Luciferase activity is induced in cells cotransfected with GAL4-LBD or GAL4-Nur77 by cytosporone B. Cytosporone B's EC50 for Nur77 is 0.278 nM. Cytosporone B exhibits strong pro-apoptotic effects in BGC-823 gastric cancer cells. In 48 hours, cytosporone B treatment causes 63.5% of the cells to undergo apoptosis. Cytosporone B exhibits a targeted action on malignant cells. Cytosporone B has a minor effect on human lung cancer H1299 cells and human hepatoma HepG2 cells, however it reduces the proliferation of human gastric cancer BGC-823 cells and human colon cancer SW620 cells by 470%[1].
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| ln Vivo |
Treatment with cytosporone B increases the transcriptional activity of the reporter five-fold in the hepatocytes of wild-type mice. When cytosporone B is administered to wild-type mice, blood glucose levels rise noticeably from 3.2 to 11.4 mM in the first 30 minutes[1]. After that, blood glucose levels progressively dropped until they returned to the starting point after 300 minutes.
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| References |
[1]. Zhan Y, et al. Cytosporone B is an agonist for nuclear orphan receptor Nur77. Nat Chem Biol. 2008 Sep;4(9):548-56
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| Molecular Formula |
C18H26O5
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| Molecular Weight |
322.4
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| CAS # |
321661-62-5
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| SMILES |
O=C(OCC)CC1=CC(O)=CC(O)=C1C(CCCCCCC)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1017 mL | 15.5087 mL | 31.0174 mL | |
| 5 mM | 0.6203 mL | 3.1017 mL | 6.2035 mL | |
| 10 mM | 0.3102 mL | 1.5509 mL | 3.1017 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
(a) Structures of Csn-B (1) and Csn-C (2). (b) Csn-B stimulates Nur77-dependent transcriptional activity in BGC-823 cells.Nat Chem Biol.2008 Sep;4(9):548-56. |
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(a) Schematic representations of Nur77 and its truncation mutants. (b) Effect of Csn-B on fluorescence quenching of GST-Nur77 and its truncation and site mutants. (c,d) Analysis of Csn-B binding to Nur77 and its LBD by CD spectroscopy (c) and sedimentation equilibrium assay (d) as described inSupplementary Methods.Nat Chem Biol.2008 Sep;4(9):548-56. |
(a) Csn-B stimulates the transactivational activity of GAL4-Nur77 and GAL4-LBD in BGC-823 cells.(b) Effect of siRNA against Nur77 or RXRα on Csn-B–induced transactivational activity.Nat Chem Biol.2008 Sep;4(9):548-56. |
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