| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Casein kinase 2 (CK2) and ERK8 (MAPK15, ERK7). CK2/ERK8-IN-1 inhibits CK2 with a Ki of 0.25 µM and ERK8 with an IC50 of 0.50 µM. It also binds to PIM1 (Ki 8.65 µM), HIPK2 (Ki 15.25 µM), and DYRK1A (Ki 11.9 µM).
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|---|---|
| ln Vitro |
Jurkat cells treated with CK2/ERK8-IN-1 (Compound K66; 0-50 µM; 24 hours) exhibited cytotoxic action [1].
CK2/ERK8-IN-1 inhibits CK2 with a Ki of 0.25 µM and ERK8 with an IC50 of 0.50 µM. It also binds to PIM1, HIPK2, and DYRK1A with Ki values of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. The compound has pro-apoptotic efficacy. |
| ln Vivo |
In vivo activity of CK2/ERK8-IN-1 has not been extensively reported in the available literature. The compound is primarily used for in vitro studies to investigate the roles of CK2 and ERK8 in apoptosis and cell signaling.
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| Enzyme Assay |
Kinase inhibition assays are performed using recombinant CK2 and ERK8 enzymes. CK2/ERK8-IN-1 is incubated with the enzymes and substrates, and the inhibition of kinase activity is measured. Ki and IC50 values are determined from dose-response curves.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Jurkat Cell Tested Concentrations: 0-50 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of cell growth in a dose-dependent manner. Cell-based assays are conducted using Jurkat cells to evaluate the pro-apoptotic activity of CK2/ERK8-IN-1. Cells are treated with the compound at concentrations ranging from 10 to 50 µM, and apoptosis is assessed by measuring markers such as caspase activation and DNA fragmentation. |
| Animal Protocol |
In vivo studies for CK2/ERK8-IN-1 are not extensively reported in the available literature. The compound is primarily used for in vitro research to study CK2 and ERK8 biology. Further in vivo studies would be needed to evaluate its therapeutic potential.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CK2/ERK8-IN-1 are not extensively reported in the available literature. The compound is primarily used for in vitro research. Further PK characterization would be required for in vivo applications.
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| Toxicity/Toxicokinetics |
Toxicity data for CK2/ERK8-IN-1 are not extensively detailed in the available literature. The compound is intended for research use only. Its pro-apoptotic activity suggests potential for cancer research, but further toxicological studies are needed.
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| References | |
| Additional Infomation |
CK2/ERK8-IN-1 is a research compound used to study the roles of CK2 and ERK8 in cell signaling and apoptosis. It is a valuable tool for investigating the therapeutic potential of targeting these kinases in cancer and other diseases. The compound is not approved for clinical use.
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| Molecular Formula |
C11H9BR4N3O2
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|---|---|
| Molecular Weight |
534.824059247971
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| Exact Mass |
534.738
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| CAS # |
1085822-09-8
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| PubChem CID |
46943415
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| Appearance |
White to off-white solid powder
|
| LogP |
4.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
387
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1=C(C(=C(C2=C1N(CC(=O)O)C(=N2)N(C)C)Br)Br)Br
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| InChi Key |
PHAOTASRLQMKBE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H9Br4N3O2/c1-17(2)11-16-9-7(14)5(12)6(13)8(15)10(9)18(11)3-4(19)20/h3H2,1-2H3,(H,19,20)
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| Chemical Name |
2-[4,5,6,7-tetrabromo-2-(dimethylamino)benzimidazol-1-yl]acetic acid
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| Synonyms |
CK2/ERK8IN1; CK2/ERK8 IN 1
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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 : ~16.67 mg/mL (~31.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (3.12 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 16.7 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: 1.67 mg/mL (3.12 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 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. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (3.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8698 mL | 9.3489 mL | 18.6979 mL | |
| 5 mM | 0.3740 mL | 1.8698 mL | 3.7396 mL | |
| 10 mM | 0.1870 mL | 0.9349 mL | 1.8698 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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