BI-D1870

製品コードS2843 バッチS284302

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₉H₂₃F₂N₅O₂

分子量

391.42

CAS No.

501437-28-1

Solubility (25°C)*

体外

DMSO

78 mg/mL (199.27 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.250mg/ml (3.19mM)	Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
in vitro	BI-D1870 inhibits RSK1, RSK2, RSK3 and RSK4 with an IC50 of 10–30 nM, but does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. This compound is cell permeant and prevents the RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in human embryonic kidney 293 cells and Rat-2 cells. It does not affect the agonist-triggered phosphorylation of substrates for six other AGC kinases. Moreover, this chemical does not suppress the phorbol ester- or EGF-induced phosphorylation of CREB. ^[1]

製品説明

BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.

in vitro

BI-D1870 inhibits RSK1, RSK2, RSK3 and RSK4 with an IC50 of 10–30 nM, but does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. This compound is cell permeant and prevents the RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in human embryonic kidney 293 cells and Rat-2 cells. It does not affect the agonist-triggered phosphorylation of substrates for six other AGC kinases. Moreover, this chemical does not suppress the phorbol ester- or EGF-induced phosphorylation of CREB. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	Protein kinase assays
キナーゼアッセイ	Purified His6–RSK1, His6–RSK2 or GST–RSK2^{1–389:S381E} (1–2 units/mL) are assayed for 10 min at 30 °C in a 50 μL assay mixture in Buffer A containing 30 μM substrate peptide (KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK), 10 mM magnesium acetate and 100 μM of [γ-³²P]ATP. Reactions are terminated and analysed as described previously. The amount of enzyme that catalysed the phosphorylation of 1 nmol of substrate peptide in 1 min is termed one unit. In order to assay RSK and MSK1 in HEK-293 or Rat-2 cell lysates, these kinases are immunoprecipitated from the cell lysates (0.1 mg of lysate protein for RSK and 0.3 mg for MSK1) and for RSK assays the immunoprecipitates are washed twice with Buffer A containing 1 mM ATP and twice with Buffer A prior to the assay, as a precaution to ensure dissociation of this compound from the RSK isoforms.
細胞アッセイ	細胞株	Cell-free assays
	濃度	IC50 of 31, 24, 18 and 15 nM for RSK1, 2, 3, & 4, respectively.
	反応時間
	実験の流れ
動物実験	動物モデル	C57/BL6J mice
	投薬量	0.5 mg/kg
	投与方法	i.p.

参考

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1698666/
https://pubmed.ncbi.nlm.nih.gov/17040210/
https://pubmed.ncbi.nlm.nih.gov/26386981/

カスタマーフィードバック

: Data from [Data independently produced by , , Mol Cancer Ther, 2017, 16(5):793-804]

: Data from [Data independently produced by , , Sci Rep, 2016, 6:36134.]

: Data from [Data independently produced by , , Mol Cell Biol, 2014, 34(13): 2517-32]

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：

The cytoplasmic domain of the pseudoprotease iRhom2 mediates distinct signaling mechanisms to control activation of the cell surface protease ADAM17 [ J Biol Chem, 2025, 301(10):110643]	PubMed: 40885391
Targeting the p90RSK/MDM2/p53 Pathway Is Effective in Blocking Tumors with Oncogenic Up-Regulation of the MAPK Pathway Such as Melanoma and Lung Cancer [ Cells, 2024, 13(18)1546]	PubMed: 39329730
Ribosomal S6 kinase 2-forkhead box protein O4 signaling pathway plays an essential role in melanogenesis [ Sci Rep, 2024, 14(1):9440]	PubMed: 38658799
p90RSK pathway inhibition synergizes with cisplatin in TMEM16A overexpressing head and neck cancer [ BMC Cancer, 2024, 24(1):233]	PubMed: 38373988
Multiplex single-cell chemical genomics reveals the kinase dependence of the response to targeted therapy [ Cell Genom, 2024, 4(2):100487]	PubMed: 38278156
The ribosomal protein S6 kinase alpha-1 (RPS6KA1) induces resistance to venetoclax/azacitidine in acute myeloid leukemia [ Leukemia, 2023, 37(8):1611-1625]	PubMed: 37414921
The ribosomal protein S6 kinase alpha-1 (RPS6KA1) induces resistance to venetoclax/azacitidine in acute myeloid leukemia [ Leukemia, 2023, 37(8):1611-1625]	PubMed: 37414921
Conjugated Bile Acids Promote Lymphangiogenesis by Modulation of the Reactive Oxygen Species-p90RSK-Vascular Endothelial Growth Factor Receptor 3 Pathway [ Cells, 2023, 12(4)526]	PubMed: 36831193
Conjugated Bile Acids Promote Lymphangiogenesis by Modulation of the Reactive Oxygen Species-p90RSK-Vascular Endothelial Growth Factor Receptor 3 Pathway [ Cells, 2023, 12(4)526]	PubMed: 36831193
LRG1 is a novel HER3 ligand to promote growth in colorectal cancer [ bioRxiv, 2023, PPR618443 ]	PubMed: none

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。