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Submit ReviewPIK 90 is a potent inhibitor of PI 3-K α/γ/δ kinases (IC50 = 11, 18, 47, 58 and 64 nM against p110α, p110γ, PI 3-KC2α, p110δ and PI 3-KC2α, respectively) as well as PIKKs (IC50 = 13 nM against DNA-PK). It inhibits the fMLP-stimulated phosphorylation of Akt and impairs polarity and chemotaxis in dHL60 cells. It suppresses insulin-stimulated phosphorylation of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in vitro and prevents insulin-induced blood glucose reduction in mice in vivo. PIK 90 can be used in combination with other small molecules and proteins for mesendoderm induction in protocols to differentiate iPSCs into organ-specific mesenchyme.
分子量 | 351.36 |
公式 | C18H17N5O3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 677338-12-4 |
PubChem ID | 135398491 |
InChI Key | ZJAVHOMVDCMAMF-UHFFFAOYSA-N |
Smiles | O=C(NC1=NC=2C(OC)=C(OC)C=CC2C3=NCCN13)C=4C=NC=CC4 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 3.51 | 10 温和加热 |
以下数据基于产品分子量 351.36。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 28.46 mL | 142.3 mL | 284.61 mL |
0.5 mM | 5.69 mL | 28.46 mL | 56.92 mL |
1 mM | 2.85 mL | 14.23 mL | 28.46 mL |
5 mM | 0.57 mL | 2.85 mL | 5.69 mL |
参考文献是支持产品生物活性的出版物。
Fan et al (2006) A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer cell 9 341 PMID: 16697955
Knight et al (2006) A pharmacological map of the PI3-K family defines a role for p110a in insulin signaling. Cell 125 733 PMID: 16647110
Kishimoto et al (2022) Directed differentiation of human pluripotent stem cells into diverse organ-specific mesenchyme of the digestive and respiratory systems. Nat.Protoc. 17 2699 PMID: 35978039
Keymeulen et al (2006) To stabilize neutrophil polarity, PIP3 and Cdc42 augment RhoA activity at the back as well as signals at the front. J.Cell Biol. 174 437 PMID: 16864657
If you know of a relevant reference for PIK 90, please let us know.
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