| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
Skepinone-L (CBS-3830; CBS3830) is a novel, potent, selective, and ATP-competitive p38-MAPK inhibitor that may have anti-inflammatory effects. With an IC50 of 5 nM, it inhibits p38α-MAPK.
| Targets |
p38α (IC50 = 5 nM)
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| ln Vitro |
Skepinone-L reduces TNF-α, IL-1β, and IL-10 concentrations, which are controlled by p38 MAPK, with an IC50 range of 30 to 50 nM and exhibits concentration-dependent inhibition of HSP27 (Ser82) phosphorylation through the p38 MAPK pathway.[1] Skepinone-L (1 μM) reduces platelet secretion and aggregation by inhibiting the phosphorylation of the platelet p38 MAPK substrate Hsp27 that is activated by stimulation with CRP, thrombin, or the thromboxane A2 analogue U-46619. [2]
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| ln Vivo |
Skepinone-L inhibits TNF-induced release from Gal/LPS by 77% in living organisms. [1]
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| Enzyme Assay |
Skepinone-L (CBS3830), the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, Skepinone-L (CBS3830) is a valuable probe for chem. biol. research, and it may foster the development of a unique class of kinase inhibitors.
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| Animal Protocol |
Mice
~3 mg/kg Oral administration |
| References |
| Molecular Formula |
C24H21F2NO4
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|---|---|---|
| Molecular Weight |
425.42
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| Exact Mass |
425.143
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| Elemental Analysis |
C, 67.76; H, 4.98; F, 8.93; N, 3.29; O, 15.04
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| CAS # |
1221485-83-1
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| Related CAS # |
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| PubChem CID |
45279963
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
629.0±55.0 °C at 760 mmHg
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| Flash Point |
334.2±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.646
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| LogP |
4.95
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
608
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C1C2=CC(OC[C@@H](CO)O)=CC=C2CCC3=C1C=CC(NC4=CC=C(C=C4F)F)=C3
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| InChi Key |
HXMGCTFLLWPVFM-GOSISDBHSA-N
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| InChi Code |
InChI=1S/C24H21F2NO4/c25-16-4-8-23(22(26)10-16)27-17-5-7-20-15(9-17)2-1-14-3-6-19(11-21(14)24(20)30)31-13-18(29)12-28/h3-11,18,27-29H,1-2,12-13H2/t18-/m1/s1
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| Chemical Name |
13-(2,4-difluoroanilino)-5-[(2R)-2,3-dihydroxypropoxy]tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-one
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| Synonyms |
CBS3830; CBS-3830; CBS 3830; Skepinone-L
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| HS Tariff Code |
2934.99.9001
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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 (5.88 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 (5.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. View More
Solubility in Formulation 3: 0.5% methylcellulose: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3506 mL | 11.7531 mL | 23.5062 mL | |
| 5 mM | 0.4701 mL | 2.3506 mL | 4.7012 mL | |
| 10 mM | 0.2351 mL | 1.1753 mL | 2.3506 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.
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