LDN-192960 |
| Catalog No.GC33086 |
LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 184582-62-5
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
LDN-192960 is a potent Haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase) inhibitor with an IC50 of 0.010 µM.
A comparison of the profiles of LDN-192960 (compound 3) and 42 suggests that only six kinases, including haspin, are inhibited by both compounds ≥90% at 10 µM[1]. LDN-192960 alone does not cause detectable mitotic exit in the mitotic (phospho)-protein monoclonal-2 (MPM-2) assay in HeLa cells. In the presence of 1 µM ZM447439, even concentrations as low as 0.1 µM LDN-192960 cause substantial loss of MPM-2 epitopes, and similar results are obtained in the presence of Hesperadin. However, 10 µM LDN-192960 does not cause mitotic exit in combination with Aurora B inhibition, which is consistent with off-target effects at this higher dose[2].
[1]. Cuny GD, et al. Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. Bioorg Med Chem Lett. 2012 Mar 1;22(5):2015-9. [2]. Fangwei Wang, et al. Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation. J Cell Biol. 2012 Oct 15; 199(2): 251-268.
| Cas No. | 184582-62-5 | SDF | |
| Canonical SMILES | NCCCSC1=C(C=C(OC)C=C2)C2=NC3=CC=C(OC)C=C31 | ||
| Formula | C18H20N2O2S | M.Wt | 328.43 |
| Solubility | Soluble in DMSO | 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 | 3.0448 mL | 15.2239 mL | 30.4479 mL |
| 5 mM | 0.609 mL | 3.0448 mL | 6.0896 mL |
| 10 mM | 0.3045 mL | 1.5224 mL | 3.0448 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *