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[PI3K/Akt/mTOR]

AZD5363,1143532-39-1,IC-0197879

Price : $142.50Price : ￥1425.00

AZD5363 is a novel, potent phosphoinositide 3-kinase (PI3K)/Akt pathway inhibitor with IC50 value of ~200nM. [1] AZD5363 is proved to inhibit castrate resistant prostate cancer (CRPC) progression. Clusterin (CLU) and autophagy will be induced which may work as cytoprotective responses which can affect the downstream PI3K/Akt signaling. [2] AZD5363 inhibits the growth of a lot of human tumor cells in a dose dependent manner. The mode of action could be monotherapy as well as in combination with HER2 inhibitors in breast cancer models. [3] It is suggested to induce cell apoptosis by measuring the expression of PARP cleavage, the activity of Caspase 3, et al. [1] Most importantly, AZD5363 can target the PI3K/Akt-pathway in vivo significantly, thus reducing the serum PSA-levels and tumor volume, finally, it could postpone the progression to CRPC.[1]
[PI3K/Akt/mTOR]

GDC-0068 (RG7440),1001264-89-6,IC-0198068

Price : $97.50Price : ￥975.00

GDC-0068 (RG7440, Ipatasertib) is a novel highly selective ATP-competitive pan-Akt inhibitor that inhibits all three isoforms of Akt1, Akt2, and Akt3 at an IC50 of 5,18,8 nM, respectively [1,5]. GDC-0068 decreased cell viability, induced apoptosis, and inhibited phosphorylation of proline rich Akt substrate 40 kDa and p70 S6 kinase in a dose-dependent manner in PIK3CA-mutant breast cancer brain metastatic cell lines compared with PIK3CA-wildtype cell lines[6]. The combined treatment of GDC-0068 (RG7440) plus anti-microtubule chemotherapy, including vinorelbine, paclitaxel, eribulin, is contributed to anti-proliferative, pro-apoptotic, and anti-metastatic effect on human breast cancer cells[7]. GDC-0068 (RG7440) blocked Akt signaling both in cultured human cancer cell lines and in tumor xenograft models as evidenced by dose-dependent decrease in phosphorylation of downstream targets. Inhibition of Akt activity by GDC-0068 (RG7440) resulted in blockade of cell-cycle progression and reduced viability of cancer cell lines[2]. Preclinical Pharmacology demonstrates GDC-0068 (RG7440) exposure resulting in a dose-dependently pharmacodynamic effect and robust anti-tumor activi......
[PI3K/Akt/mTOR]

MK-2206 dihydrochloride,1032350-13-2,IC-0198257

Price : $127.50Price : ￥1275.00

MK-2206 dihydrochloride is an orally active allosteric Akt inhibitor used in treatment of solid tumors.[1] IIn vitro experiment it shown that MK-2206 is equally potent toward purified recombinant human Akt1 and Akt2 enzyme with IC50 of 5 nmol/L and 12 nmol/L, respectively; and approximately 5-fold less potent against human Akt3 (IC50, 65 nmol/L). MK-2206 potently inhibited the cell growth of Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292 with IC50s of 5.5, 4.3, and 5.2 μmol/L, respectively. The combination of 2.5 μmol/L erlotinib and 3 μmol/L MK-2206 or higher obviously activated the caspase.[1] In vitro, Akt inhibitor (MK 2206 dihydrochloride, 2.5 nM) reduces the effects of anti-microRNA-320a on the apoptosis of MDA-MB-231 cells.[2] In vitro, treatment with 0.1 and 1 μM for 48 h MK-2206 reduced the expression p-Akt in all pancreatic cancer cell lines suggesting that MK-2206 inhibited Akt phosphorylation in pancreatic cancer cells.[3] In vitro the colony formation assay confirmed that 1 μM of MK-2206 significantly inhibited the proliferation of SGC-7901 cells.[4] In vivo test displayed it that treatment with 120 mg/kg MK-2206 orally 2 hours after erlotinib ......
[PI3K/Akt/mTOR]

AICAR,2627-69-2,IC-0199013

Price : $129.00Price : ￥1290.00

AICAR (also called acadesine) is a purine nucleoside. Three pharmacological applications of AICAR were identified: i) stimulation under ischemic conditions of the cardiac production of the vasodilator, adenosine [1]; ii) inhibition of hepatic gluconeogenesis at the level of fructose-1,6-bisphosphatase [2], of therapeutic potential in diabetes; and iii) stimulation of AMP-activated protein kinase (AMPK), initially applied to inhibit the hepatic synthesis of triglycerides and cholesterol [3]. AICAR (treated 48 hours) inhibited cell proliferation of mantle cell lymphoma (MCL) cell lines, REC-1, JEKO-1, UPN-1, JVM-2, MAVER-1 and Z-138, with IC50s of 0.28, 0.59, 0.64, 0.98, 0.50, and 0.14 Mm respectively [4]. AICAR inhibited the growth and depletion of pyrimidine nucleotide pools in fibroblasts [5], accelerated repletion of purine nucleotide pools in heart [6], inhibition of fatty acid, sterol synthesis, and gluconeogenesis in hepatocytes, and increase in glucose uptake in muscle [7]. AICAR (500 mg/kg) injected intraperitoneally into C57BL/6J mice 1 hour before LPS administration. LPS induced the expression of TF mRNA in many major organs, including the lung and liver [8].......
[PI3K/Akt/mTOR]

Dorsomorphin (Compound C),866405-64-3,IC-0199202

Price : $97.70Price : ￥977.00

Dorsomorphin (Compound C) is an agent that used as a cell-permeable AMPK inhibitor. It could rescue the antiproliferative actions of AICAR and metformin. Moreover, dorsomorphin (Compound C) is also used as a selective inhibitor of the BMP pathway. Compound C could inhibit a number of kinases other than AMPK.[1] In vitro experiments indicate that Compound C inhibits AMPK activity and proliferation of human glioma cells. Dorsomorphin (Compound C) also reduces the apoptosis of cells induced by cisplatin, and decreases the expression of c-caspase3 and c-PARP in cisplatin treatment. In vivo study demonstrate compound C attenuates cisplatin-induced nephrotoxicity in mice, and alleviates c-caspase 3 and c-PARP induced by cisplatin in kidney tissues.[1][2]
[PI3K/Akt/mTOR]

Dorsomorphin 2HCl,1219168-18-9,IC-0199391

Price : $97.70Price : ￥977.00

IC50: Dorsomorphin inhibited BMP4-induced phosphorylation of BMP-responsive SMADs in a dose-dependent manner (half maximal inhibitory concentration (IC50) =0.47 mM). Bone morphogenetic protein (BMP) signals coordinate developmental patterning and have essential physiological roles in mature organisms. The first known small-molecule inhibitor of BMP signaling, dorsomorphin, were identified in a screen for compounds that perturb dorsoventral axis formation in zebrafish. In vitro: Previoius researchers found that dorsomorphin selectively inhibits the BMP type I receptors ALK2/ALK3/ALK6 leading to block BMP-mediated SMAD1/5/8 phosphorylation, osteogenic differentiation as well as target gene transcription. Using dorsomorphin, they examined the role of BMP signaling in iron homeostasis.dorsomorphin inhibited the systemic iron regulator hepcidin BMP-, hemojuvelin- and interleukin 6–stimulated expression, indicating that BMP receptors regulate hepcidin induction by all of these stimuli [1]. In vivo: The systemic challenge with iron rapidly induced SMAD1/5/8 phosphorylation and hepcidin expression in the liver, while dorsomorphin treatment could blocke SMAD1/5/8 phosphorylation......

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