KN-62

製品コードS7422 バッチS742201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C38H35N5O6S2
分子量 721.84 CAS No. 127191-97-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (138.53 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 KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM; also a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM). It is selective for CaMKII relative to PKA, PKC and MLCK, but inhibits CaMKI and CaMKIV equally well, The Ki value of KN-62 for CaMK V is 0.8 μM.
in vitro KN-62 suppresses the A23187-induced autophosphorylation of Ca2+/CaM kinase in PC12 D cells. [1] KN-62 (10 μM) inhibits carbachol and potassium-stimulated insulin secretion from rat pancreatic islets. [2] KN-62 also inhibits growth of K562 cells and blocks cell cycle progression. [3]
in vivo KN-62 inhibits seizure-induced expression of brain-derived neurotrophic factor mRNA in adult rat brain. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assay
Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin, and 10 μM [γ-33]ATP at 30 °C. The kinase reaction is halted by adding 1 mL of 10% trichloroacetic acid.
細胞アッセイ 細胞株 K562 cells
濃度 10 μM
反応時間 48 hours
実験の流れ

For cell growth analysis, K562 cells are plated in a 3-cm dish with 5 mL of culture medium containing various concentration of KN-62. After two days in these condition cell numbers are counted.
動物実験 動物モデル Sprague Dawley Rats
投薬量 2 pmol
投与方法 i.c.v.

カスタマーフィードバック

Data from [Data independently produced by , , Front Cell Neurosci, 2017, https://doi.org/10.3389/fncel.2017.00281]

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：

Single-cell transcriptomics of NRAS-mutated melanoma transitioning to drug resistance reveals P2RX7 as an indicator of early drug response [ Cell Rep, 2023, 42(7):112696] PubMed: 37379213
Capsaicin ameliorates intermittent high glucose-mediated endothelial senescence via the TRPV1/SIRT1 pathway [ Phytomedicine, 2022, 100:154081] PubMed: 35405615
Non-catalytic allostery in α-TAT1 by a phospho-switch drives dynamic microtubule acetylation [ J Cell Biol, 2022, 221-11e202202100] PubMed: 36222836
Terfenadine resensitizes doxorubicin activity in drug-resistant ovarian cancer cells via an inhibition of CaMKII/CREB1 mediated ABCB1 expression [ Front Oncol, 2022, 12:1068443] PubMed: 36439493
Derivation and Characterization of Murine and Amphibian Müller Glia Cell Lines [ Transl Vis Sci Technol, 2022, 11(4):4] PubMed: 35377941
TLR4 signalling via Piezo1 engages and enhances the macrophage mediated host response during bacterial infection [ Nat Commun, 2021, 12(1):3519] PubMed: 34112781
CAMK2/CaMKII activates MLKL in short-term starvation to facilitate autophagic flux [ Autophagy, 2021, 1-19] PubMed: 34282994
A phospho-regulated ensemble signal motif of α-TAT1 drives dynamic microtubule 1 acetylation 2 [ HAL open science, 2021, 10.1101/2020.09.23.310235] PubMed: None
Wnt ligands 3a and 5a regulate proliferation and migration in human fetal liver progenitor cells [ Transl Gastroenterol Hepatol, 2021, 6:56] PubMed: 34805578
The NLRP3 Inflammasome Regulates Corneal Allograft Rejection Through Enhanced Phosphorylation of STAT3 [ Am J Transplant, 2020, 10.1111/ajt.16071] PubMed: 32583615

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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