1. PI3K/Akt/mTOR
  2. PI3K
  3. IPI-3063


Cat. No.: HY-111510 Purity: 98.80%
Handling Instructions

IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM.

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

IPI-3063 Chemical Structure

IPI-3063 Chemical Structure

CAS No. : 1425043-73-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 220 In-stock
Estimated Time of Arrival: December 31
2 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
25 mg USD 720 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM.

IC50 & Target[1]


2.5 nM (IC50)


1170 nM (IC50)


1508 nM (IC50)


2187 nM (IC50)

In Vitro

IPI-3063 inhibits p110α, p110β, and p110γ with IC50s of 1171±533 nM, 1508±624 nM, and 2187±1529 nM, respectively. IPI-3063 potently reduces mouse B cell proliferation, survival, and plasmablast differentiation while increasing antibody class switching to IgG1. IPI-3063 is a p110δ selective compound with an IC50=0.1 nM in p110δ-specific cell-based assays and cellular IC50 values for the other class I PI3K isoforms are at least 1,000-fold higher (IC50=1901±1318 nM for p110α, IC50=102.8±35.7 nM for p110β, IC50=418.8±117.2 nM for p110γ). IPI-3063 is very potent in reducing p-AKT (significant effect at 1 nM). IPI-3063 also reduces p-ERK1/2 with a significant effect at 10 nM. IPI-3063 is very potent, achieving a significant decrease in B cell survival when present at 10 nM[1].

Molecular Weight







N#CC1=C(N[[email protected]](C2=CC3=C(C(N2C(C)C)=O)C(C(C=C4)=CN(C)C4=O)=CC=C3)C)N=CN=C1N


Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.33 mg/mL (182.94 mM)

*"≥" means soluble, but saturation unknown.

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1953 mL 10.9767 mL 21.9534 mL
5 mM 0.4391 mL 2.1953 mL 4.3907 mL
10 mM 0.2195 mL 1.0977 mL 2.1953 mL
*Please refer to the solubility information to select the appropriate solvent.
Kinase Assay

Human recombinant PI3K-α, PI3K-β, PI3K-δ, and PI3K-γ are used. Phosphatidylinositol 4,5 bis phosphate (diC8-PtdIns(4,5)P2) is used. PI3K-α, β, and δ are heterodimers consisting of full length p110α, p110β, or p110δ catalytic subunit and the p85α regulatory subunit. PI3K-γ is a monomer of the p110γ catalytic subunit. Samples of kinase (10 nM-α, β, and δ; 20 nM-γ) are incubated with IPI-3063 for 30 min at room temperature in reaction buffer (15 mM HEPES pH 7.4, 20 mM NaCl, 1 mM EGTA, 0.02% Tween 20, 10 mM MgCl2, 0.2 mg/mL bovine-γ-globulins) followed by addition of ATP/diC8-PtdIns(4,5)P2 mixture to give final concentrations of 3 mM ATP and 500 µM diC8-PtdIns(4,5)P2. Reactions are incubated at room temperature for 2 h, with PI3K activity is assessed. Plates are read on plate reader in luminescence mode[1].

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

Cell Assay

Peripheral blood mononuclear cells (PBMCs) are first purified from blood by density gradient centrifugation. Human B cells are then purified from PBMCs by negative selection. B-cell purity is increased from 4% to >70% as measured by FACS analysis using anti-CD19 PE conjugated antibody. Purified B cells are seeded at a final concentration of 0.1×106 cells/mL and cultured with 2 µg/mL human CD40L+5 µg/mL anti-human IgM/IgG+100 µg/mL hIL-2+100 µg/mL hIL-21. All B cells are cultured in RPMI 1640 supplemented with 10% (vol/vol) heat-inactivated FCS, 5 mM Hepes, 2 mM L-glutamine, 100 U/mL Penicillin, 100 µg/mL Streptomycin, 50 µM 2-mercaptoethanol. Purified human B cells are pretreated with IPI-3063 (0.1, 1, 10, and 100 nM) for 30 min, then stimulated with human CD40L+anti-human IgM/IgG+human IL-2+human IL-21 for 120 h[1].

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

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IPI-3063IPI3063IPI 3063PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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