| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CDK5 GSK3β
The primary targets of 7BIO are cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). CDK5 and GSK3β are key pharmacological targets in Alzheimer's disease and other neurodegenerative disorders. By inhibiting these kinases, 7BIO modulates tau phosphorylation and other downstream signaling pathways involved in neuroinflammation and synaptic function. The compound also inhibits Aβ oligomer-induced neuroinflammation and synaptic impairments. |
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| ln Vitro |
In SH-SY5Y cells, 7BIO (1 and 10 μM; 24 hours) exhibits neuroprotective properties and can stop Aβ1–42 oligomer-induced cell death, but not reverse it[1].
In vitro, 7BIO demonstrates potent inhibition of CDK5 and GSK3β. It inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, and the activation of astrocytes and microglia. In cellular assays, 7BIO has been shown to have antiproliferative activity against apoptosis-resistant human A549 cells with an IC50 of 13.9 μM. The compound shows concentration-dependent inhibition of CDK5 and GSK3β activity. |
| ln Vivo |
In mice, the effects of Aβ oligomer-induced impairment on recognition, spatial learning, and memory are dramatically reduced by 7Bio (2.3, 7.0, and 23.3 μg/kg; bilateral ventricle injection)[1]. In mice, Aβ oligomer-induced increases in TNF-α and IL-6 production in the brain and synapsin-1 and PSD-95 expression in the hippocampus are reduced by 7Bio (2.3, 7.0, and 23.3 μg/kg; bilateral ventricle injection)[1]. Activation of microglia, astrogliosis, and increased expression of pTau in the mouse brain caused by Aβ oligomer are attenuated by 7Bio (2.3, 7.0, and 23.3 μg /kg; bilateral ventricle injection)[1]. Preventing decreased expression of pSer9-GSK3β and having no significant influence on the level of Tau protein is possible with 7Bio (2.3, 7.0, and 23.3 μg/kg; bilateral ventricle injection)[1].
In vivo, 7BIO attenuates Aβ oligomer-induced cognitive impairments in mice. It has been shown to inhibit neuroinflammation, synaptic damage, and tau hyperphosphorylation in animal models of Alzheimer's disease. The compound demonstrates in vivo efficacy in reducing Aβ oligomer-induced neuroinflammation and cognitive deficits. However, detailed pharmacokinetic and pharmacodynamic data are limited in the available literature. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for 7BIO typically involve kinase inhibition studies against CDK5 and GSK3β. Kinases are incubated with varying concentrations of 7BIO (0.1-100 µM) in appropriate buffer at 37°C. Kinase activity is measured using radioactive or fluorescent substrates, and IC50 values are calculated from dose-response curves. The compound demonstrates concentration-dependent inhibition of CDK5 and GSK3β.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: SH-SY5Y cells Tested Concentrations: 1 and 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibit Aβ oligomer-induced neuronal death. 7BIO prevented, but did not rescue Aβ1 −42 oligomer-induced cell death in SH-SY5Y cells. In vitro cellular assays for 7BIO involve testing its effects on neuroinflammation, tau phosphorylation, and cell viability. Cells (e.g., neuronal cells, astrocytes, microglia) are treated with varying concentrations of 7BIO (0.1-50 µM) for 24-72 hours. Aβ oligomer-induced neuroinflammation and tau hyperphosphorylation are measured by Western blot or ELISA. Cell viability is assessed using MTT or CCK-8 assays. The compound demonstrates concentration-dependent inhibition of neuroinflammation and tau phosphorylation. |
| Animal Protocol |
Animal/Disease Models: 8 weeks mice (30 g)[1]
Doses: 2.3, 7.0, and 23.3 μg/kg Route of Administration: bilateral ventricle injection Experimental Results: Attenuates Aβ oligomer-induced impairment of recognition, spatial learning and memory in mice. In vivo animal studies for 7BIO involve efficacy testing in models of Alzheimer's disease. Mice are treated with 7BIO via intraperitoneal or oral administration at various doses. Cognitive impairment is assessed using behavioral tests such as the Morris water maze. Neuroinflammation, synaptic damage, and tau hyperphosphorylation are measured by immunohistochemistry or Western blot. The compound attenuates Aβ oligomer-induced cognitive impairments in mice. |
| ADME/Pharmacokinetics |
7BIO has a molecular formula of C16H10BrN3O2 and a molecular weight of 356.17. It appears as a solid powder with a purity of ≥98%. It is soluble in DMSO at 71 mg/mL (199.34 mM) but insoluble in water and ethanol. The compound should be stored as a powder at -20°C for up to 3 years. In solution, it is stable at -80°C for 6 months and at -20°C for 1 month. It is intended for research use only and is not for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of 7BIO 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. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
7BIO (CAS 916440-85-2) is a cell-permeable indirubin derivative that acts as a kinase inhibitor targeting CDK5 and GSK3β. It has a molecular formula of C16H10BrN3O2 and a molecular weight of 356.17. The compound inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, and activation of astrocytes and microglia. It attenuates Aβ oligomer-induced cognitive impairments in mice. 7BIO is a valuable tool for studying neurodegenerative diseases, particularly Alzheimer's disease, and is intended for research use only.
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| Molecular Formula |
C16H10BRN3O2
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|---|---|
| Molecular Weight |
356.17
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| Exact Mass |
354.996
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| CAS # |
916440-85-2
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| PubChem CID |
135423792
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| Appearance |
Brown to reddish brown solid powder
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| Density |
1.80±0.1 g/cm3 (20 °C, 760 mmHg)
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| Boiling Point |
565.5±50.0 °C (760 mmHg)
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| LogP |
3.692
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
22
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| Complexity |
438
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C(=C(N2)C3=C(NC4=C3C=CC=C4Br)O)N=O
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| InChi Key |
HYMACPDEJIEMST-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H10BrN3O2/c17-10-6-3-5-9-12(16(21)19-13(9)10)15-14(20-22)8-4-1-2-7-11(8)18-15/h1-7,18-19,21H
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| Chemical Name |
7-bromo-3-(3-nitroso-1H-indol-2-yl)-1H-indol-2-ol
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 250 mg/mL (701.91 mM)
Ethanol : 50 mg/mL (140.38 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.02 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH 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: ≥ 2.08 mg/mL (5.84 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 20.8 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 | 2.8076 mL | 14.0382 mL | 28.0765 mL | |
| 5 mM | 0.5615 mL | 2.8076 mL | 5.6153 mL | |
| 10 mM | 0.2808 mL | 1.4038 mL | 2.8076 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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