CAY10512
Based on 1 Customer Validation
CAY10512 is a NF-κB inhibitor. CAY10512 can suppress the upregulation of NF-κB-sensitive proinflammatory miRNAs (miRNA-9, miRNA-125b, miRNA-146a, miRNA-155) in cerebrospinal fluid and extracellular fluid. CAY10512 significantly reduces the release of pro-inflammatory cytokines (such as TNF-α, MCP-1, IL-8, IL-6). CAY10512 can be used for researchs on neuroinflammation, islet transplantation and microRNA regulation.
For research use only. We do not sell to patients.
- Purity: 97.0%
- CAS No.: 139141-12-1
- Formula: C15H13FO
- Molecular Weight:228.26
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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NF-κB |
IL-6 |
IL-8 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
0.15 μM
Compound: 6p
|
Inhibition of TNF-alpha-induced NF-kappaB activation in HEK293T cells
Inhibition of TNF-alpha-induced NF-kappaB activation in HEK293T cells
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[PMID: 17125270] |
| HepG2 | EC50 |
5.4 μM
Compound: 1; LD55
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Activation of Nrf2 (unknown origin) expressed in human HepG2 cells after 5 hrs by ARE-driven luciferase reporter gene assay
Activation of Nrf2 (unknown origin) expressed in human HepG2 cells after 5 hrs by ARE-driven luciferase reporter gene assay
|
[PMID: 28126440] |
CAY10512 (5 μM, 0-96 h) effectively inhibits miRNA-9, miRNA-125b, miRNA146a and miRNA-155 upregulation in HNG cells stimulated by AD-ECF[1].
CAY10512 (0.15 μM, 1-7 h) significantly protects pancreatic islet viability and effectively alleviates pancreatic islet cell damage by inhibiting the increase of pro-inflammatory factors and the expression of tissue factor TF in primary human islets[2].
CAY10512 (0.25 μM, 25 h) significantly inhibits the gene and protein expressions of pro-inflammatory factor IL-6 and inflammatory receptor TNFR2 induced by MR agonists (Aldosterone (HY-113313), 11-dehydrocorticosterone (HY-113447)) in BV-2 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary human islets
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Concentration:0.15 μM
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Incubation Time:Pre-treat for one hour, then mix with autologous blood and incubate for another 1, 3, 6 h
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Result:Prevented the increase of TNF-α, MCP-1, IL-8 and IL-6.
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Cell Line:BV-2 cells
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Concentration:0.25 μM
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Incubation Time:Pre-treatment for 1 hour, then add the stimulus and incubate for 24 hours
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Result:Completely blocked the upregulation of IL-6 mRNA induced by Aldosterone and the upregulation of TNFR2 mRNA induced by 11-dehydrocorticosterone.
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Cell Line:BV-2 cells
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Concentration:0.25 μM
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Incubation Time:Pre-treatment for 1 hour, then add the stimulus and incubate for 24 hours
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Result:Completely blocked the phosphorylation of ILp65 induced by aldosterone and its translocation to the nucleus, as well as the upregulation of TNFR2 protein levels induced by 11-dehydrocorticosterone.
Chemical Information
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CAS No. 139141-12-1
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Appearance Solid
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Molecular Weight 228.26
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Formula C15H13FO
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Color White to off-white
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SMILES
COC(C=C1)=CC=C1/C=C/C2=C(C=CC=C2)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Alexandrov P N, et al. microRNA (miRNA) speciation in Alzheimer’s disease (AD) cerebrospinal fluid (CSF) and extracellular fluid (ECF)[J]. International journal of biochemistry and molecular biology, 2012, 3(4): 365. [Content Brief]
[2]. Kanak MA, et al. Alleviation of instant blood-mediated inflammatory reaction in autologous conditions through treatment of human islets with NF-κB inhibitors. Transplantation. 2014 Sep 15;98(5):578-84. [Content Brief]
[3]. Chantong B, et al. Mineralocorticoid and glucocorticoid receptors differentially regulate NF-kappaB activity and pro-inflammatory cytokine production in murine BV-2 microglial cells. J Neuroinflammation. 2012 Nov 28;9:260. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)