Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
50mg |
|
||
Other Sizes |
|
Targets |
IC50: 55 nM (haspin kinase) IC50: 9.9 μM (DYRK2)[1]
|
---|---|
ln Vitro |
Serine/threonine kinase Haspin, also known as Haploid Germ Cell-Specific Nuclear Protein Kinase, is expressed in a number of different tissues, including the testis, bone marrow, thymus, and spleen. Furthermore, haspin is crucial during mitosis, where it phosphorylates histone H3 at Thr-3 (H3T3) in G2/early prophase, reaches its peak in prometaphase/metaphase, and then starts to decline in anaphase[1]. DYRKs are ePKs that are a part of the CMGC family. They are further classified into two classes: class 2 kinases (DYRK2, 3, and 4) and class 1 kinases (DYRK1A and 1B). During synthesis, a critical activation loop tyrosine is autophosphorylated, which is necessary for DYRK activity[1].
|
References |
[1]. Gregory D Cuny, et al. Structure-activity Relationship Study of Acridine Analogs as Haspin and DYRK2 Kinase Inhibitors. Bioorg Med Chem Lett
[2]. Katrin Kestav, et al. Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin. Curr Med Chem. 2017;24(21):2276-2293. |
Molecular Formula |
C17H19CL3N2OS
|
---|---|
Molecular Weight |
405.77
|
CAS # |
1784281-97-5
|
SMILES |
ClC1C=CC2=C(C=1)C(=C1C=C(C=CC1=N2)OC)SCCCN.Cl.Cl
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : 33.33 mg/mL (82.14 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4645 mL | 12.3223 mL | 24.6445 mL | |
5 mM | 0.4929 mL | 2.4645 mL | 4.9289 mL | |
10 mM | 0.2464 mL | 1.2322 mL | 2.4645 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.