KG-501

製品コードS8409 バッチS840901

印刷

化学情報

Chemical Structure Synonyms 2-naphthol-AS-E-phosphate Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C17H13ClNO5P
分子量 377.72 CAS No. 18228-17-6
Solubility (25°C)* 体外 DMSO 20 mg/mL (52.94 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 KG-501 is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay.
in vitro

KG-501 inhibits induction of cAMP-responsive genes, at least in part, by blocking the CREB:CBP interaction[1]. The inhibition of the CREB pathway using KG-501, induces an inhibition of neurite outgrowth and synaptogenesis, as well as a decrease of MAP2+ neuronal cells[2].
in vivo

KG-501 inhibits CREB, CCL2 expression and ERK phosphorylation, also significantly lowers the cAMP level. CREB might contribute to the neuroprotection opposed neuroinflammation through cAMP/ERK adjustment pathway. KG-501 significantly promots the neurological outcomes of AOM-treated mice, reduces phosphorylation of ERK and the concentration of cAMP in cortex[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK293T cells
濃度 5, 10, 25 μM
反応時間 20 min
実験の流れ

EVX-1 luciferase reporter plasmid was transfected into HEK293T cells. At 24 h posttransfection, cells were pretreated with the indicated amount of KG-501 or DMSO vehicle for 20 min followed by coincubation with forskolin or DMSO. Cells were harvested at 4 h, and luciferase activity was measured.
動物実験 動物モデル Murine azoxymethane (AOM) model of hepatic encephalopathy (Adult male C57BL/6 mice)
投薬量 10, 20, or 50 μM
投与方法 intracerebroventricular infusion

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

LIM1 contributes to the malignant potential of endometrial cancer [ Front Oncol, 2023, 13:1082441] PubMed: 36969081
Sirt3 mediates the benefits of exercise on bone in aged mice [ Cell Death Differ, 2022, 10.1038/s41418-022-01053-5] PubMed: 36153410
Targeting ADRB2 enhances sensitivity of non-small cell lung cancer to VEGFR2 tyrosine kinase inhibitors [ Cell Death Discov, 2022, 8(1):36] PubMed: 35075132
The chemerin-CMKLR1 axis limits thermogenesis by controlling a beige adipocyte/IL-33/type 2 innate immunity circuit [ Sci Immunol, 2021, 6(61)eabg9698] PubMed: 34330814
Conjugated secondary 12α-hydroxylated bile acids promote liver fibrogenesis [ EBioMedicine, 2021, 66:103290] PubMed: 33752128
FKBP10 promotes proliferation of glioma cells via activating AKT-CREB-PCNA axis [ J Biomed Sci, 2021, 28(1):13] PubMed: 33557829
Long non-coding RNA Lnc-408 promotes invasion and metastasis of breast cancer cell by regulating LIMK1 [ Oncogene, 2021, 10.1038/s41388-021-01845-y] PubMed: 34079084
Recombinant Annexin A2 Administration Improves Neurological Outcomes After Traumatic Brain Injury in Mice [ Front Pharmacol, 2021, 12:708469] PubMed: 34400908
Cathepsin D deficiency in mammary epithelium transiently stalls breast cancer by interference with mTORC1 signaling [ Nat Commun, 2020, 11(1):5133] PubMed: 33046706
Cynandione A Alleviates Neuropathic Pain Through α7-nAChR-Dependent IL-10/β-Endorphin Signaling Complexes [ Front Pharmacol, 2020, 11:614450] PubMed: 33584292

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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