MIPS-9922

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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.

For research use only. We do not sell to patients.

MIPS-9922 Chemical Structure

CAS No. : 1416956-33-6

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PI3Kβ

63 nM (IC₅₀)

PI3Kδ

2200 nM (IC₅₀)

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]

In Vitro

MIPS-9922 potently inhibits ADP-induced washed platelet aggregation. MIPS-9922 also inhibits integrin αIIbβ3 activation and αIIbβ3 dependent platelet adhesion to immobilized von Willebrand Factor (vWF) under high shear^[1].

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

In Vivo

MIPS-9922 (2.5 mg/kg, bolus jugular vein injection; once) prevents arterial thrombus formation in the in vivo electrolytic mouse model of thrombosis without inducing prolonged bleeding or excess blood loss^[1].

MedChemExpress (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.

Molecular Weight

563.60

Formula

C₂₈H₃₁F₂N₉O₂

CAS No.

1416956-33-6

SMILES

O=C(N1CCN(C2=NC(N3C4=CC=CC=C4N=C3C(F)F)=NC(N5CCOCC5)=N2)CC1)[C@@H](N)CC6=CC=CC=C6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhaohua Zheng, et al. Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922). Eur J Med Chem. 2016 Oct 21:122:339-351. [Content Brief]

MIPS-9922 Related Classifications

Cardiovascular Disease

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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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