PI3K Inhibitor Kits

Catalog No. K1010

A unique collection of 7 inhibitors for a range of PI3K subtypes

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1ea USD 490

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7 Customer Reviews

  • Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.

    (A) MCF7 cells pre-treated with 100 nM siRNA for 72 h were re-seeded with normal growth media and grown overnight, then further transfected by 100nM of fresh siRNA. Twenty-(A) four hours after transfection, the cells were further treated with PI-103 for 24 h and the cell lysates were immunoblotted with the indicated antibodies. (B) Breast cancer cells carrying BRCA1 mutations were treated with 1 mM of PI-103 for 24h (left) or increasing amounts of PI-103 for 24 h (right). Cell lysates were analyzed by Western blotting with the indicated antibodies.

  • After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of A66 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

    We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.

  • After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of AS-605240 for 3h,followed by 15-minute stimolation of 100ng/ml EGF

    After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of CAL-101 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

  • Knockdown of BRCA1 sensitizes cells to PI3K/AKT pathway inhibitors. MCF7 cells transfected with either BRCA1-siRNA or control-siRNA were treated with increasing amounts of inhibitors targeting the PI3K/AKT pathway for 48 h in triplicate. Viable cells were measured by MTT assay.

Contents

Cat.No. Product Name Feature Targets and IC50s Suggested Solvent Amount Supplied
p110α p110β p110γ p110δ C2β Vps34
S1009 BEZ235 (NVP-BEZ235) A dual ATP-competitive inhibitor of PI3K and mTOR. 4 nM 75 nM 5 nM 7 nM     DMSO 7mg/mL 50 mg
S2636 A66 A selective inhibitor of p110α, p110αE545K and p110αH1047R. 32 nM           DMSO 79mg/mL 5 mg
S1169 TGX-221 A potent, selective and cell permeable PI3K inhibitor of p110β.   8.5 nM         DMSO 17mg/mL 5 mg
S1410 AS-605240 A novel, potent and selective PI3Kγ inhibitor.     8 nM       DMSO 3mg/mL 5 mg
S2226 CAL-101 (GS-1101) A selective class I PI3K inhibitor of p110δ.       2.5 nM     DMSO 83mg/mL 10 mg
S1038 PI-103 A potent, cell-permeable and ATP-competitive PI3K family member inhibitor. 8 nM 88 nM 150 nM 48 nM 26 nM   DMSO 24mg/mL 5 mg
S2767 3-Methyladenine A selective autophagy and PI3K inhibitor of Vps34 and PI3Kγ.     60 µM     25 µM DMSO 3mg/mL 50 mg

Chemical Information

Formulation A unique collection of 7 inhibitors for a range of PI3K subtypes supplied as lyophilized powder
Container Screw Cap Micro Tubes of WATSON
Stability
Powder -20℃ 2 years
In DMSO -80℃ 6 months
Shipping Blue ice
Packaging Inert gas

Research Area

Other Inhibitor Kits