DKFZ-251 |
Catalog No.GC79387
One-Click Copy Product Info
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DKFZ-251 is a kininogenase-related peptidase KLK6 inhibitor ( IC50 =0.47 μM), and also exhibits certain inhibitory activity against KLK5 and KLK7 ( IC50 values are 1.1 nM and 73 nM, respectively).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2222059-70-1
Sample solution is provided at 25 µL, 10mM.
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In Vitro, DKFZ-251 (compound 11) (200 μM; 1 h) forms a long-lived acyl-enzyme complex with recombinant triple-mutant KLK6, with a half-life of 6.43 h[1]. DKFZ-251 (100-500 nM; 48 h) induces a dose-dependent increase in BrdU incorporation and causes phenotypic changes in FaDu cells, which is consistent with the targeted inhibition of endogenous KLK6[1]. DKFZ-251 (2.5-10 μM; 30 min) specifically inhibits the labeling of recombinant KLK6 by the activity-based probe DKFZ-633[1].
References:
[1]. De Vita E, et al. Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity. J Med Chem. 2018;61(19):8859-8874.
| Cas No. | 2222059-70-1 | SDF | |
| Formula | C24H24N4O3 | M.Wt | 416.48 |
| Solubility | Storage | Store at -20°C | |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4011 mL | 12.0054 mL | 24.0108 mL |
| 5 mM | 480.2 μL | 2.4011 mL | 4.8022 mL |
| 10 mM | 240.1 μL | 1.2005 mL | 2.4011 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
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 saline, 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
- View current batch:
- Purity: >95.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)