PI3K-Akt-mTOR Signaling Pathway Inhibitor Kit

Catalog No. K1020

A unique collection of 9 inhibitors for studying the PI3K/Akt/mTOR signaling pathway

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  • Cooperative Effects of AR and mTOR Inhibition In Vitro and In Vivo (A) In vitro response of Pten null;Ar+ murine (CaP8) and human (LNCaP) prostate cancer cells to AR knockdown (sh-AR) or pharmacological inhibition of AR (MDV3100, 10 mM) with and without rapamycin (R: 1 nM) treatment (Sc, control sh oligo). (B and D) In vivo response to treatments with castration, MDV3100, rapamycin, or their combinations as measured by cell proliferation (Ki67+cells) and (C and D) tumor burden in Pb-Cre+;-PtenL/L and Pb-Cre+;PtenL/L:ArL/Y mutants. Scale bars represent 2 mm (C), 200 mm (D), and 75 mm (D, inset). Error bars represent mean ± SD.

    A, ANOVA of IC50 values of the dual PI3K/mTOR inhibitor NVP-BEZ235 in 23 melanoma cell lines showing no significant difference in sensitivity to this compound in B-Raf mutant and Braf wild-type cells. B, decreases in pAkt and pP70S6K in a dose and time-dependent fashion in 2 melanoma cell lines treated with NVP-BEZ235. pP70S6K levels are undetectable at all concentrations and time points studied, whereas levels of pAkt start rising again after 4 hours of drug exposure in a dose-dependent fashion. C, clonogenic assays in 2 melanoma cell lines (YUVON and YUSIK) treated with NVP-BEZ235 at different concentrations. NVPBEZ235 was effective in inhibiting colony formation at low nanomolar concentrations.

  • Confocal microscopy images of NO formation. DAF 2 DA-loaded washed platelets (1.0109 platelets/mL) were preincubated at 378C with saline (A), and then stimulated for 1min with 0.1 (B), 1.0 (C) or 10 (D) mM AEA. In Panel (E–F–G) washed platelets were preincubated with 1 mM SR1 (E), 1 Mm MK2206 (F) or 20 mM LY294002 (G), and then stimulated for 1min with 1.0 mM AEA. In panel (H) is reported the effect of 5 mg/mL collagen, used as a positive control. All the experiments were carried out in the presence of 100 mM L-arginine. NO formation was visualized by confocal microscropy as detailed in Methods.

    Effect of ATM inhibitor in etoposide-induced cell death. The cells were pretreated with KU55933 (2 M) for 1 h before etoposide treatment.

  • Mean IL-8 concentrations determined by ELISA of the supernatants of HeLa cells infected with wild-type Salmonella. Kinase inhibitors are indicated on the x axis, and the target families of the inhibitors are indicated above each column. CEC, chelerythrine; Pim Inh, Pim-1 inhibitor 2. Inhibitors that significantly affected IL-8 production relative to the control (P < 0.05, Bonferroni post hoc test from one-way ANOVA) are indicated with an asterisk. Relative cell viability is also shown, as determined by reduction of XTT by viable cells. A450, absorbance at 450 nm.

    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.

  • Rapamycin (RPM) inhibits OA-induced lipogenesis. Male SD rats were divided into three groups, and then treated as follows for seven days: group I (control; Ctrl), normal diet + vehicle; group II (OA), 1% OA diet + vehicle; group III (OA + RPM), 1% OA diet + RPM. (A) Hepatic TG concentrations were determined using the serum triglyceride determination kit. (B) Fixed liver sections were subjected to HE and Oil Red O staining as well as immunohistochemistry assays with SREBP-1 antibody. Representative microphotographs of liver specimens from all groups of rats are shown. (C) The levels of mRNA of the indicated genes involved in lipogenesis were determined by real-time PCR. Each bar represents the mean ± SE of the results obtained from six rats. * P < 0.05, ** P < 0.01, *** P < 0.001.

Contents

Cat.No. Product Name Targets and IC50s Suggested Solvent Amount Supplied
S2739 PKI-402 A selective, reversible and ATP-competitive Class I PI3K inhibitor. PI3Kα, IC50=1 nM; PI3Kβ, IC50=7 nM; PI3Kγ, IC50=16 nM; PI3Kδ, IC50=14 nM. DMSO <1 mg/mL
Water <1 mg/mL
5 mg
S1039 Rapamycin (Sirolimus) A specific mTOR inhibitor with an IC50 of 0.1 nM. DMSO 183 mg/mL 5 mg
S1009 BEZ235 (NVP-BEZ235) A dual ATP-competitive inhibitor of PI3K and mTOR. p110α, IC50=4 nM; p110β, IC50=75 nM; p110δ, IC50=7 nM; p110γ, IC50=5 nM. DMSO 7 mg/mL 50 mg
S1078 MK-2206 dihydrochloride A highly selective inhibitor of Akt. Akt1, IC50=8 nM; Akt2, IC50=12 nM; Akt3, IC50=65 nM. DMSO 96 mg/mL
Water 96 mg/mL
5 mg
S2924 CHIR-99021 (CT99021) HCl CHIR-99021 HCl (CT99021) is hydrochloride of CHIR-99021, which is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. DMSO 3 mg/mL 2 mg
S2638 NU7441 (KU-57788) A potent and selective DNA-PK inhibitor with an IC50 of 14 nM. DMSO 5 mg/mL 5 mg
S1092 KU-55933 A potent and specific ATM kinase inhibitor with an IC50 and a Ki of 13 nM and 2.2 nM, respectively. DMSO 50 mg/mL 5 mg
S1275 BX-912 A selective potent PDK-1 inhibitor with an IC50 of 12 nM. DMSO 94 mg/mL 2 mg
S1558 AT7867 A potent Akt inhibitor with an IC50 of 17 nM. AT7867 also inhibits structurally related AGC kinases p70S6K and PKA with IC50s of 20 nM and 85 nM, respectively. DMSO 68 mg/mL 10 mg

Chemical Information

Formulation A unique collection of 9 inhibitors for studying the PI3K/Akt/mTOR signaling pathway 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