2. PI3K/Akt/mTOR
  3. PI3K
  4. MIPS-9922

MIPS-9922 是一种强效且选择性的 PI3Kβ 抑制剂，IC50 为 63 nM。MIPS-9922 抑制 PI3Kβ 的效力比 PI3Kδ 高 30 倍以上。MIPS-9922 阻断 PI3K 介导的血小板糖蛋白 αIIbβ3 活化和血小板粘附。MIPS-9922 具有抗血小板和抗血栓活性。

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MIPS-9922 Chemical Structure

MIPS-9922 Chemical Structure

CAS No. : 1416956-33-6

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MIPS-9922 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MIPS-9922 is a potent and selective PI3Kβ inhibitor with an IC50 of 63 nM. MIPS-9922 inhibits PI3Kβ with >30-fold higher potency than PI3Kδ. MIPS-9922 blocks PI3K mediated activation of platelet glycoprotein αIIbβ3 activation and platelet adhesion in vitro. MIPS-9922 shows anti-platelet and anti-thrombotic activities[1].

IC50 & Target[1]

PI3Kβ

63 nM (IC50)

PI3Kδ

2200 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MDA-MB-468 IC50
< 10 nM
Compound: 21
Inhibition of IGF-1 induced Akt phosphorylation in PTEN-deficient human MDA-MB-468 cells pretreated for 2 hrs before IGF1 induction measured after 15 mins by Western blot analysis
Inhibition of IGF-1 induced Akt phosphorylation in PTEN-deficient human MDA-MB-468 cells pretreated for 2 hrs before IGF1 induction measured after 15 mins by Western blot analysis
[PMID: 23795239]
MDA-MB-468 EC50
4.6 μM
Compound: 21
Cytotoxicity against PTEN-deficient human MDA-MB-468 cells assessed as inhibition of cell growth after 48 hrs by Cell Titer 96 assay
Cytotoxicity against PTEN-deficient human MDA-MB-468 cells assessed as inhibition of cell growth after 48 hrs by Cell Titer 96 assay
[PMID: 23795239]
Sf21 IC50
6000 nM
Compound: 21
Inhibition of recombinant PI3K-beta D862Q mutant (unknown origin) expressed in baculovirus infected Sf21 cells assessed as decrease in ATP consumption using phosphatidylinositol bisphosphate and 100 uM ATP as substrate measured after 60 mins by luminescen
Inhibition of recombinant PI3K-beta D862Q mutant (unknown origin) expressed in baculovirus infected Sf21 cells assessed as decrease in ATP consumption using phosphatidylinositol bisphosphate and 100 uM ATP as substrate measured after 60 mins by luminescen
[PMID: 23795239]
Sf21 IC50
8100 nM
Compound: 21
Inhibition of recombinant PI3K-alpha Q589D mutant (unknown origin) expressed in baculovirus infected Sf21 cells assessed as decrease in ATP consumption using phosphatidylinositol bisphosphate and 100 uM ATP as substrate measured after 60 mins by luminesce
Inhibition of recombinant PI3K-alpha Q589D mutant (unknown origin) expressed in baculovirus infected Sf21 cells assessed as decrease in ATP consumption using phosphatidylinositol bisphosphate and 100 uM ATP as substrate measured after 60 mins by luminesce
[PMID: 23795239]
体外研究
(In Vitro)

MIPS-9922 可有效抑制 ADP 诱导的洗涤性血小板聚集。MIPS-9922 还可抑制整合素 αIIbβ3 活化和 αIIbβ3 依赖性血小板在高剪切下粘附于固定的血管性血友病因子 (vWF)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MIPS-9922 相关抗体:
体内研究
(In Vivo)

MIPS-9922 (2.5 mg/kg，颈静脉推注；一次) 可防止体内电解血栓小鼠模型中动脉血栓形成，而不会引起长时间出血或过度失血[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice bearing electrolytic injury[1]
Dosage: 2.5 mg/kg
Administration: Bolus jugular vein injection; once
Result: Prevented arterial thrombus formation in the in vivo electrolytic mouse model of thrombosis.
分子量

563.60

Formula

C28H31F2N9O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MIPS-9922 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MIPS-99221416956-33-6MIPS9922MIPS 9922PI3KPhosphoinositide 3-kinaseAnti-platelet activityplatelet aggregationAnti-thrombotic activityPI3Kβ inhibitorInhibitorinhibitorinhibit

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目录号：
HY-120265
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