| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
The primary targets of Dyrk1B/1A-IN-9 are the kinases Dyrk1B (Mirk) and Dyrk1A. Dyrk1B is a nuclear kinase that plays a role in the cell cycle, particularly in promoting the G0/G1 phase and maintaining cells in a quiescent state. It is also involved in the regulation of apoptosis and DNA repair. Overexpression of Dyrk1B has been observed in several cancers, including ovarian, colon, and pancreatic cancers, where it contributes to tumor cell survival and chemoresistance. Dyrk1A is a kinase implicated in neurodevelopmental processes, including neurogenesis and synaptic plasticity. Its overexpression is linked to Down syndrome and is associated with cognitive deficits. By potently and selectively inhibiting these two kinases, Dyrk1B/1A-IN-9 allows researchers to probe their functions.
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| ln Vitro |
Dyrk1B/1A-IN-9 is a highly potent inhibitor of Dyrk1B and Dyrk1A, with IC₅₀ values of 68 nM and 22 nM, respectively. This indicates that it is a very effective inhibitor at nanomolar concentrations. It is described as a highly selective inhibitor. Its mode of action is reversible, meaning it binds to the kinase in a non-covalent manner. This reversibility is a key feature for a research tool, as it allows for the study of the effects of acute inhibition. Its in vitro activity is typically characterized using kinase assays.
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| ln Vivo |
Specific in vivo data for Dyrk1B/1A-IN-9 is not detailed in the provided search results. However, as a potent and selective inhibitor, it would be a valuable tool for in vivo studies to validate Dyrk1B and Dyrk1A as drug targets. In cancer models, inhibition of Dyrk1B could potentially sensitize tumors to chemotherapy or reduce tumor growth. In neurological models, inhibition of Dyrk1A could potentially ameliorate cognitive deficits.
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| Enzyme Assay |
The in vitro kinase assay for Dyrk1B/1A-IN-9 typically measures its ability to inhibit the kinase activity of Dyrk1B and Dyrk1A. In these assays, purified recombinant Dyrk1B or Dyrk1A enzyme is incubated with a peptide substrate and ATP (the phosphate donor). The transfer of a phosphate group from ATP to the substrate is measured. This can be done using radioactive ATP (³³P-ATP) and measuring the incorporation of radioactivity into the substrate, or using non-radioactive methods such as fluorescence-based assays or ELISA. The assay is performed in the presence of varying concentrations of Dyrk1B/1A-IN-9. A control without the inhibitor defines 100% enzyme activity. By plotting the percent inhibition versus the compound concentration, an IC₅₀ value can be determined.
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| Cell Assay |
In vitro cell-based assays for Dyrk1B/1A-IN-9 evaluate its effects on cellular signaling and phenotypes. Cells are treated with the compound, and the phosphorylation of known Dyrk1B or Dyrk1A substrates is assessed by Western blotting using phospho-specific antibodies. This confirms target engagement in a cellular context. Additionally, the compound's effects on cell proliferation, cell cycle progression, and apoptosis can be studied, particularly in cancer cell lines where Dyrk1B is overexpressed. These assays are crucial for understanding the functional consequences of Dyrk1B/1A inhibition.
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| Animal Protocol |
Specific in vivo animal study protocols for Dyrk1B/1A-IN-9 are not described in the provided literature. However, based on its mechanism as a Dyrk1B/1A inhibitor, typical studies would involve administering the compound to mouse models of cancer (e.g., xenograft models) to evaluate its antitumor activity or to mouse models of Down syndrome to evaluate its effects on cognitive function.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for Dyrk1B/1A-IN-9 is not available in the provided search results. Its molecular weight is 498.32. As a research compound, its ADME properties would be characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Dyrk1B/1A-IN-9 is not publicly available. As a kinase inhibitor, its selectivity is a key determinant of its toxicity profile. It is classified as a research tool and is not intended for human use.
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| References | |
| Additional Infomation |
Dyrk1B/1A-IN-9 is a valuable research tool for studying the roles of Dyrk1B and Dyrk1A in cell biology and disease. Its high potency and selectivity make it a preferred compound for studying these kinases. The compound has not received FDA approval for any indication.
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| Molecular Formula |
C23H17CL2N5O4
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|---|---|
| Molecular Weight |
498.32
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| Exact Mass |
497.065
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| CAS # |
1386979-55-0
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| PubChem CID |
57523919
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.678
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| LogP |
4.21
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
812
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=NC=C2C=C(C(=O)NC2=N1)C(=O)NC3=C(C=CC(=C3)C(=O)NCC4=CC(=CC=C4)Cl)Cl
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| InChi Key |
CQKBSRPVZZLCJE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H17Cl2N5O4/c1-34-23-27-11-14-8-16(22(33)29-19(14)30-23)21(32)28-18-9-13(5-6-17(18)25)20(31)26-10-12-3-2-4-15(24)7-12/h2-9,11H,10H2,1H3,(H,26,31)(H,28,32)(H,27,29,30,33)
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| Chemical Name |
N-[2-chloro-5-[(3-chlorophenyl)methylcarbamoyl]phenyl]-2-methoxy-7-oxo-8H-pyrido[2,3-d]pyrimidine-6-carboxamide
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| Synonyms |
1A-IN-9; Dyrk1B inhibitor; Dyrk1B/1A-IN-9
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~10.03 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.5 mg/mL (1.00 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 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. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0067 mL | 10.0337 mL | 20.0674 mL | |
| 5 mM | 0.4013 mL | 2.0067 mL | 4.0135 mL | |
| 10 mM | 0.2007 mL | 1.0034 mL | 2.0067 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.
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