1. NF-κB Apoptosis Immunology/Inflammation
  2. NF-κB TNF Receptor Interleukin Related
  3. CAY10512

CAY10512 (5 μM, 0-96 h) 可有效抑制 AD-ECF 刺激的 HNG 细胞中 miRNA-9、miRNA-125b、miRNA146a 和 miRNA-155 的上调。
CAY10512 (0.15 μM, 1-7 h) 通过抑制促炎因子的增加和组织因子 TF 的表达,显著保护胰岛活力,有效减轻胰岛细胞损伤。
CAY10512 (0.25 μM, 25 h) 可显著抑制 MR 激动剂 (Aldosterone (HY-113313)、11-dehydrocorticosterone (HY-113447)) 在 BV-2 细胞中。

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.

CAY10512

CAY10512 Chemical Structure

CAS No. : 139141-12-1

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Description

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[1][2][3].

IC50 & Target[1][2][3]

NF-κB

 

IL-6

 

IL-8

 

Cellular Effect
Cell Line Type Value Description References
HepG2 EC50
5.4 μM
Compound: 1; LD55
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]
In Vitro

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.

ELISA Assay[2]

Cell Line: Primary human islets
Concentration: 0.15 μM
Incubation Time: Pre-treat for one hour, then mix with autologous blood and incubate for another 1, 3, 6 h
Result: Prevented the increase of TNF-α, MCP-1, IL-8 and IL-6.

RT-PCR[3]

Cell Line: BV-2 cells
Concentration: 0.25 μM
Incubation Time: Pre-treatment for 1 hour, then add the stimulus and incubate for 24 hours
Result: Completely blocked the upregulation of IL-6 mRNA induced by Aldosterone and the upregulation of TNFR2 mRNA induced by 11-dehydrocorticosterone.

Western Blot Analysis[3]

Cell Line: BV-2 cells
Concentration: 0.25 μM
Incubation Time: Pre-treatment for 1 hour, then add the stimulus and incubate for 24 hours
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.
Molecular Weight

228.26

Formula

C15H13FO

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC(C=C1)=CC=C1/C=C/C2=C(C=CC=C2)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 97.0%

References
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CAY10512
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HY-120269
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