| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
The primary target of (E/Z)-GO289 is casein kinase 2 (CK2), a serine/threonine protein kinase involved in various cellular processes including cell cycle regulation, apoptosis, and circadian rhythm control. By inhibiting CK2, (E/Z)-GO289 significantly extends the circadian period and demonstrates cell type-dependent inhibition of cancer cell growth. The compound has an IC₅₀ of 13 µM against PM2, which is >1000 times greater than that of CK2, indicating high selectivity.
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| ln Vitro |
(E/Z)-GO289 is a strong and incredibly specific CK2 inhibitor that controls the proliferation of cancer cells as well as circadian cycles. (E/Z)-GO289 has an IC50 of 13 μM against PIM2, which is >1000 times greater than that of CK2[1]. Caki-2, A498 and 769-P cells are strongly inhibited by (E/Z)-GO289 (3-9 μM; 2 days) [1]. Cancer cell proliferation and clock protein phosphorylation are both regulated by (E/Z)-GO289 [1].
In vitro, (E/Z)-GO289 demonstrates potent and selective inhibition of CK2 with an IC₅₀ of 7 nM. It significantly extends the circadian period in cellular models and shows cell type-dependent inhibition of cancer cell growth that correlates with cellular clock function. The compound is a strong and incredibly specific CK2 inhibitor that controls the proliferation of cancer cells as well as circadian cycles. |
| ln Vivo |
In vivo activity of (E/Z)-GO289 has not been extensively characterized. As a CK2 inhibitor, it has potential for studying the role of CK2 in circadian rhythm regulation and cancer cell proliferation. However, detailed in vivo efficacy and pharmacokinetic data are limited in the available literature. The compound's cell type-dependent inhibition of cancer cell growth suggests it may have in vivo activity.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for (E/Z)-GO289 typically involve CK2 kinase activity studies. The enzyme is incubated with varying concentrations of (E/Z)-GO289 (0.1-1000 nM) in appropriate buffer at 37°C. Kinase activity is measured using radioactive or fluorescent substrates, and the IC₅₀ value is calculated from the dose-response curve. Selectivity against other kinases is assessed by testing the compound against a panel of kinases.
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| Cell Assay |
In vitro cellular assays for (E/Z)-GO289 involve testing its effects on circadian rhythm and cancer cell proliferation. Cells are treated with varying concentrations of (E/Z)-GO289 (0.01-10 µM) for 24-72 hours. Circadian period length is measured using bioluminescent reporters. Cell proliferation and viability are assessed using MTT or CCK-8 assays. The compound demonstrates concentration-dependent inhibition of CK2 activity and extension of the circadian period.
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| Animal Protocol |
In vivo animal studies for (E/Z)-GO289 are limited, as the compound is primarily used in research to study CK2 function. For efficacy testing, animal models of cancer or circadian rhythm disorders could be used. Animals would be treated with (E/Z)-GO289 via oral or intraperitoneal administration at various doses. However, detailed in vivo protocols are not well established in the available literature.
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| ADME/Pharmacokinetics |
(E/Z)-GO289 has a molecular formula of C₁₇H₁₅BrN₄O₂S and a molecular weight of 419.29. The compound is intended for research use only and has not been approved for clinical use. Detailed pharmacokinetic parameters such as half-life, oral bioavailability, and tissue distribution are not well characterized in the available literature. The compound is typically stored at -20°C and is stable under recommended conditions.
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| Toxicity/Toxicokinetics |
The toxicity profile of (E/Z)-GO289 has not been extensively characterized. As a research compound, standard toxicity studies would include assessment of acute oral toxicity, repeated-dose toxicity, and genotoxicity in animal models. The compound is intended for research use only and is not approved for clinical use. Further toxicological studies would be needed to fully establish its safety profile for therapeutic applications.
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| References | |
| Additional Infomation |
(E/Z)-GO289 (CAS 694522-87-7) is a potent and selective inhibitor of casein kinase 2 (CK2) with an IC₅₀ of 7 nM. It has a molecular formula of C₁₇H₁₅BrN₄O₂S and a molecular weight of 419.29. This compound significantly extends the circadian period and demonstrates cell type-dependent inhibition of cancer cell growth. It is intended for research use only and is not approved for clinical use.
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| Molecular Formula |
C17H15BRN4O2S
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|---|---|
| Molecular Weight |
419.295601129532
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| Exact Mass |
418.01
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| Elemental Analysis |
C, 48.70; H, 3.61; Br, 19.06; N, 13.36; O, 7.63; S, 7.65
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| CAS # |
694522-87-7
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| PubChem CID |
135401714
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| Appearance |
White to off-white solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
452
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C=C(C(=C1)/C=N/N2C(=NN=C2SC)C3=CC=CC=C3)Br)O
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| InChi Key |
DARDDBZKGVEVKB-VXLYETTFSA-N
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| InChi Code |
InChI=1S/C17H15BrN4O2S/c1-24-15-8-12(13(18)9-14(15)23)10-19-22-16(20-21-17(22)25-2)11-6-4-3-5-7-11/h3-10,23H,1-2H3/b19-10+
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| Chemical Name |
5-bromo-2-methoxy-4-[(E)-(3-methylsulfanyl-5-phenyl-1,2,4-triazol-4-yl)iminomethyl]phenol
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| Synonyms |
GO289; GO 289; GO-289
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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 (39.76 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (3.98 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 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 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. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.98 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 16.7 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 | 2.3849 mL | 11.9246 mL | 23.8493 mL | |
| 5 mM | 0.4770 mL | 2.3849 mL | 4.7699 mL | |
| 10 mM | 0.2385 mL | 1.1925 mL | 2.3849 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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