PIK-294

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Chemical Structure| 900185-02-6 同义名 : -
CAS号 : 900185-02-6
货号 : A326767
分子式 : C28H23N7O2
纯度 : 99%+
分子量 : 489.528
MDL号 : MFCD17019338
存储条件：

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(214.49 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • p110γ

    p110γ, IC50:160 nM

  • p110β

    p110β, IC50:490 nM

  • p110δ

    p110δ, IC50:10 nM
描述 The phosphoinositide 3-kinase (PI3K)/Akt/mTOR signaling pathway is one of the most frequently dysregulated signaling cascades in human malignancies, it displays oncogenic potential and it is implicated in a wide variety of different neoplasms[3]. The PI3-K family comprises 15 kinases with distinct substrate specificities, expression patterns, and modes of regulation. The class I PI3-Ks (p110α, p110β, p110δ, and p110γ) are activated by tyrosine kinases or G protein-coupled receptors to generate PIP3, which engages downstream effectors such as the Akt/PDK1 pathway, the Tec family kinases, and the Rho family GTPases. PIK-294 is one of the most potent p110δ-selective inhibitors with IC50s of 0.01 μM for p110δ and 10 μM ,0.49 μM, 0.16 μM for p110α, p110β and p110γ[4]. In a vitro experiment, pretreatment with the PI3kinase p110δ inhibitor PIK-294 10 μM can significantly inhibited GM-CSF mediated phosphorylation in Neutrophils. The involvement of PI3Kδ in chemotaxis as pre-treatment of the cells with the PI3Kδ selective inhibitor PIK-294 significantly reduced migration in response to stimulation with CXCL8[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.21mL

2.04mL

1.02mL

20.43mL

4.09mL

2.04mL
参考文献

[1]Bobrovnikova-Marjon E, Pytel D, et al. PERK utilizes intrinsic lipid kinase activity to generate phosphatidic acid, mediate Akt activation, and promote adipocyte differentiation. Mol Cell Biol. 2012 Jun;32(12):2268-78.

[2]Knight ZA, Gonzalez B, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

[3]Chang KY, Tsai SY, Wu CM, Yen CJ, Chuang BF, Chang JY. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin Cancer Res. 2011 Nov 15;17(22):7116-26. doi: 10.1158/1078-0432.CCR-11-0796. Epub 2011 Oct 5. PMID: 21976531.

[4]Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B, Balla T, Weiss WA, Williams RL, Shokat KM. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. doi: 10.1016/j.cell.2006.03.035. Epub 2006 Apr 27. PMID: 16647110; PMCID: PMC2946820.

[5]Martin KJ, Muessel MJ, Pullar CE, Willars GB, Wardlaw AJ. The role of phosphoinositide 3-kinases in neutrophil migration in 3D collagen gels. PLoS One. 2015 Feb 6;10(2):e0116250. doi: 10.1371/journal.pone.0116250. Erratum in: PLoS One. 2015;10(7):e0134924. PMID: 25659107; PMCID: PMC4320071.