LDN-27219 |
رقم الكتالوجGC13015
One-Click Copy Product Info
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LDN-27219 هو مثبط عكسي للربط البطيء لـ TGase
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 312946-37-5
Sample solution is provided at 25 µL, 10mM.
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LDN-27219 is a reversible and slow-binding inhibitor of tissue transglutaminase (TGases) with IC50 value of 250nM for TGase 2 [1, 2].
LDN-27219 is discovered as a moderately potent inhibitor of TGase. It shows inhibitory activity against hTGase with IC50 value of 0.6μM. LDN-27219 is also a selective inhibitor. It has no effect on Factor XIIIa or caspase 3 at concentration up to 50μM. Besides that, LDN-27219 is found to be mutually exclusive inhibitors with GTP which is an allosteric inhibitor of TGase. It binds at sites other than the GTP site or the active site of the enzyme. The mechanism of LDN-27219 is also not similar with GTP. It has a modest effect on the binding of calcium. Moreover, it is found that LDN-27219 is a competitive inhibitor of the hTGase-catalyzed hydrolysis of Z-Pro-Gln-Ala-Trp [1].
References:
[1] Case A, Stein R L. Kinetic analysis of the interaction of tissue transglutaminase with a nonpeptidic slow-binding inhibitor. Biochemistry, 2007, 46(4): 1106-1115.
[2] Duval E, Case A, Stein R L, et al. Structure–activity relationship study of novel tissue transglutaminase inhibitors. Bioorganic & medicinal chemistry letters, 2005, 15(7): 1885-1889.
| Cas No. | 312946-37-5 | SDF | |
| Chemical Name | (Z)-2-((4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio)acetohydrazonic acid | ||
| Canonical SMILES | N/N=C(O)/CSC1=NC2=C(C(N1C3=CC=CC=C3)=O)C(C4=CC=CC=C4)=CS2 | ||
| Formula | C20H16N4O2S2 | M.Wt | 408.5 |
| الذوبان | DMSO: 100 mM | Storage | Store 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 | 2.448 mL | 12.2399 mL | 24.4798 mL |
| 5 mM | 489.6 μL | 2.448 mL | 4.896 mL |
| 10 mM | 244.8 μL | 1.224 mL | 2.448 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)