Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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Targets |
DYRK1 DYRK2
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ln Vitro |
Protein kinase inhibitor 1 hydrochloride has IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2, making it a strong HIPK2 inhibitor. With an IC50 greater than 10 μM, protein kinase inhibitor 1 (compound A64) is ineffective as a Cdk1 inhibitor. With Kds of 3.7 nM (PIM3), 6.1 nM (CSNK2A2), 6.1 nM (CSNK2A2), 8.8 nM (DYRK1A), 9.5 nM (DAPK1), 31 nM (CSNK2A1), 37 nM (PIM1), 130 nM (DRAK2), 150 nM (CLK2), 190 nM (DRAK1), 220 nM (ULK2), 240 nM (CLK1), 250 nM (DYRK2), and 390 nM (ERK8), as well as IC50s of 19 nM (DYRK1A), 62 nM (DYRK1B), and 74 nM (HIPK2)[1].
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References |
[1]. Miduturu CV, et al. High-throughput kinase profiling: a more efficient approach toward the discovery of new kinaseinhibitors. Chem Biol. 2011 Jul 29;18(7):868-79.
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Molecular Formula |
C18H18CLN5O3S
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Molecular Weight |
419.89
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CAS # |
2321337-71-5
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Related CAS # |
Protein kinase inhibitor 1;1365986-44-2
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SMILES |
Cl.S1C(NC(/C/1=C\C1CNC(C(C2=CN=C(C=C2)N2CCNCC2)C1)=O)=O)=O
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Solubility (In Vitro) |
H2O: 9.09 mg/mL (21.65 mM)
DMSO: 8.33 mg/mL (19.84 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.3816 mL | 11.9079 mL | 23.8158 mL | |
5 mM | 0.4763 mL | 2.3816 mL | 4.7632 mL | |
10 mM | 0.2382 mL | 1.1908 mL | 2.3816 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.