KT 5823 |
| Katalog-Nr.GC17346 |
KT 5823, ein selektiver Inhibitor der cGMP-abhängigen Proteinkinase (PKG) mit einem Ki-Wert von 0,23 μM, hemmt auch PKA und PKC mit Ki-Werten von 10 μM bzw. 4 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 126643-37-6
Sample solution is provided at 25 µL, 10mM.
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The activity of cGMP-dependent protein kinase (PKG) is controlled by factors that elevate cellular cGMP, like nitric oxide (NO), and by those that reduce cGMP levels, like certain phosphodiesterases. KT 5823 is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC50 = 234 nM).1 KT 5823 is cell-permeable and is often used in intact cells to assess the role of PKG in signaling, although there are cases where it poorly inhibits PKG in cells.[2] KT 5823 is a weak inhibitor of PKC (Ki = 4 µM) and PKA (Ki >10 µM).[1]
Reference:
[1]. Hidaka, H., and Kobayashi, R. Pharmacology of protein kinase inhibitors. Annu. Rev. Pharmacol. Toxicol. 32, 377-397 (1992).
[2]. Burkhardt, M., Glazova, M., Gambaryan, S., et al. KT5823 inhibits cGMP-dependent protein kinase activity in vitro but not in intact human platelets and rat mesangial cells. J. Biol. Chem. 275(43), 33536-33541 (2000).
| Cas No. | 126643-37-6 | SDF | |
| Chemical Name | (5S,6S,8S)-methyl 6-methoxy-5,14-dimethyl-13-oxo-6,7,8,13,14,15-hexahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate | ||
| Canonical SMILES | O=C([C@@]([C@]1(C)O[C@@H]2N3C4=C5N1C6=CC=CC=C6C5=C(CN(C)C7=O)C7=C4C8=CC=CC=C38)(C2)OC)OC | ||
| Formula | C29H25N3O5 | M.Wt | 495.53 |
| Löslichkeit | 1mg/mL in ethyl acetate or 20mg/mL in DMSO | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.018 mL | 10.0902 mL | 20.1804 mL |
| 5 mM | 0.4036 mL | 2.018 mL | 4.0361 mL |
| 10 mM | 0.2018 mL | 1.009 mL | 2.018 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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