Fig. 1 · Structure

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PIK-294

Cat. No. A10728 CAS 900185-02-6

PI3K inhibitor

PIK-294 is a PI3 Kinase inhibitor that is 20- to 60-fold more potent than the parent compound, PIK-293. It is one of the most potent p110δ-selective inhibitors that has been reported.

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Biological Activity

Target & Activity

Target Activity Value
p110δ 10 nM
p110γ 160 nM
p110β 490 nM

In Vitro Studies

Pretreatment with 1 μM PIK-294 did not alter apoptosis in control, uninfected PMNs, as assessed by Annexin V-FITC/PI staining and flow cytometry. In LVS-infected PMNs, PIK-294 did not alter the rate of apoptosis, with the compound effect isolated by comparison with PMNs left in medium alone. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Apoptosis in control uninfected PMNs

Cell-based study · control, uninfected PMNs [1]

Control, uninfected PMNs were pretreated with 1 μM PIK-294. Apoptosis assessed by Annexin V-FITC/PI staining and flow cytometry was unaltered.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Apoptosis was quantified at 4, 10, 18, and 24 hours using Annexin V-FITC/PI staining and flow cytometry.Reported result 1 μM PIK-294: Neither of these drugs altered the rate of apoptosis of control or LVS-infected PMNs.[1]

Literature-Reported Treatment Conditions

Treatment concentration
1 μM
Exposure duration
60 min; 4, 10, 18, and 24 hours
Method
pretreated
Vehicle
dimethyl sulfoxide (DMSO)
Methods and source locations

Compound reported in the paper: PIK-294

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Assessment of Neutrophil Apoptosis (S21); Materials and Methods > Inhibition of Signaling Pathways (S28); Results > PI3K Activity Is Required for Survival of Both Infected and Uninfected Neutrophils (S78); Results > PI3Kα Plays a Specific Role in Extended Survival of F. tularensis-Infected Neutrophils (S89, S97, S98); Figure 5 legend (S169, S170); Table 1 (T1.h1, T1.r10)

Apoptosis was quantified at 4, 10, 18, and 24 hours using Annexin V-FITC/PI staining and flow cytometry.: Apoptosis was quantified at 4, 10, 18, and 24 hours using Annexin V-FITC/PI staining and flow cytometry.; comparator: medium alone — Results > PI3Kα Plays a Specific Role in Extended Survival of F. tularensis-Infected Neutrophils (S97, S98); Figure 5 legend (S170)

Apoptosis in LVS-infected PMNs

Cell-based study · LVS-infected PMNs [1]

PMNs were treated with PIK-294 prior to further incubation in the presence and absence of LVS. Neither of these drugs altered the rate of apoptosis of control or LVS-infected PMNs.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Apoptosis was quantified at 4, 10, 18, and 24 hours using Annexin V-FITC/PI staining and flow cytometry.Reported result 1 μM PIK-294: Neither of these drugs altered the rate of apoptosis of control or LVS-infected PMNs.[1]

Literature-Reported Treatment Conditions

Treatment concentration
1 μM
Exposure duration
60 min; 4, 10, 18, and 24 hours
Method
pretreated
Vehicle
dimethyl sulfoxide (DMSO)
Co-treatment
Other interventions in this design: F. tularensis LVS 20 bacteria/cell. Compound effect isolated by the comparison: PMNs were left in medium alone.
Methods and source locations

Compound reported in the paper: PIK-294

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Infection and Culture of Neutrophils (S12); Materials and Methods > Assessment of Neutrophil Apoptosis (S21); Materials and Methods > Inhibition of Signaling Pathways (S28, S29); Results > PI3Kα Plays a Specific Role in Extended Survival of F. tularensis-Infected Neutrophils (S89, S97, S98); Figure 5 legend (S169, S170); Table 1 (T1.h1, T1.r10)

Apoptosis was quantified at 4, 10, 18, and 24 hours using Annexin V-FITC/PI staining and flow cytometry.: Apoptosis was quantified at 4, 10, 18, and 24 hours using Annexin V-FITC/PI staining and flow cytometry.; comparator: medium alone — Results > PI3Kα Plays a Specific Role in Extended Survival of F. tularensis-Infected Neutrophils (S97, S98); Figure 5 legend (S170)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 900185-02-6
Applications PI3K inhibitor
Formula C28H23N7O2
Molecular Weight 489.5
SMILES
CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)CN4C5=C(C(=N4)C6=CC(=CC=C6)O)C(=NC=N5)N

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 91 mg/mL (185.89 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Kinkead LC, Krysa SJ, Allen LH. Neutrophil Survival Signaling During Francisella tularensis Infection. Front Cell Infect Microbiol (2022). PMID: 35873156 DOI: 10.3389/fcimb.2022.889290 Source material

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