K02288

製品コードS7359 バッチS735903

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

C20H20N2O4

分子量 352.38 CAS No. 1431985-92-0
Solubility (25°C)* 体外 DMSO 70 mg/mL (198.64 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 K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
in vitro K02288 dose-dependently inhibits BMP4- and BMP6- induced Smad1/5/8 phosphorylation in C2C12 cells without affecting TGF-β-BMP signaling. [1]
in vivo In Zebrafish Embryos, K02288 induces a dorsalized phenotype in a dose dependent manner without effect om intersomitic vessel (ISV) formation. [1]
特徴 A chemical probe for BMP signaling in cells.

プロトコル(参考用のみ)

キナーゼアッセイ In vitro Kinase Assay for ALK1-6
Kinase reactions for ALK1-6 are performed at room temperature for 45 minutes in 96-well plates mixing 2.5 nM kinase, 0.5 mg/mL dephosphorylated casein, 6 µM ATP, 0.05 µCi/µL [γ-32P]ATP, 10 mM MnCl2 and 0.2% BSA in kinase buffer. Inhibitors are added at concentrations between 0 and 10 µM in kinase reaction buffer and tested in triplicate. Reactions are quenched with phosphoric acid, bound to 96-well P81 phosphocellulose filter plates and assayed with Microscint 20 scintillation fluid using a Spectramax L luminometer. Data are normalized to untreated controls at 100% enzyme activity and negative controls subtracted as background. IC50 values are calculated using GraphPad.
動物実験 動物モデル Zebrafish Embryos
投薬量 ~10 µM
投与方法 --

カスタマーフィードバック

, , Cancer Invest, 2017, 35(9):601-609

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:

Defects of the spliceosomal gene SNRPB affect osteo- and chondro-differentiation [ FEBS J, 2024, 291(2):272-291] PubMed: 37584444
Inhibition of BMP signaling pathway induced senescence and calcification in anaplastic meningioma [ J Neurooncol, 2024, 10.1007/s11060-024-04625-2] PubMed: 38446374
BMP9-ID1 Signaling Activates HIF-1α and VEGFA Expression to Promote Tumor Angiogenesis in Hepatocellular Carcinoma [ Int J Mol Sci, 2022, 23(3)1475] PubMed: 35163396
Low-Dose-Rate Radiation-Induced Secretion of TGF-β3 Together with an Activator in Small Extracellular Vesicles Modifies Low-Dose Hyper-Radiosensitivity through ALK1 Binding [ Int J Mol Sci, 2022, 23(15)8147] PubMed: 35897723
Electrochemically induced in vitro focal hypoxia in human neurons [ Front Cell Dev Biol, 2022, 10:968341] PubMed: 36247014
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
Clonal hematopoiesis with JAK2V617F promotes pulmonary hypertension with ALK1 upregulation in lung neutrophils [ Nat Commun, 2021, 12(1):6177] PubMed: 34702814
BMP9-ID1 signaling promotes EpCAM-positive cancer stem cell properties in hepatocellular carcinoma [ Mol Oncol, 2021, 10.1002/1878-0261.12963] PubMed: 33834612
Hemodynamic Forces Regulate Cardiac Regeneration-Responsive Enhancer Activity during Ventricle Regeneration [ Int J Mol Sci, 2021, 22(8)3945] PubMed: 33920448
GATA3 Mediates a Fast, Irreversible Commitment to BMP4-Driven Differentiation in Human Embryonic Stem Cells. [ Cell Stem Cell, 2020, 7;26(5):693-706] PubMed: 32302522

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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