Product Details
Product Name:
3CAI |
CAS No.:
28755-03-5 |
Purity:
98.13% |
Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
Name | 3CAI |
Description | 3CAI is a potent and specific AKT1 and AKT2 inhibitor, demonstrating significant inhibition of AKT in an in vitro kinase assay. It suppressed the expression of AKT direct downstream targets (such as mTOR and GSK3β) and induced growth inhibition and apoptosis in colon cancer cells. |
In vitro | 3CAI, a potential AKT inhibitor, exhibits significantly higher potency in inhibiting AKT1 compared to PI3K (60% inhibition at 1 μM vs 10 μM, respectively). In experiments with HCT116 and HT29 colon cancer cells treated with 3CAI (4 μM), I3C, or an AKT inhibitor in 1% FBS/McCoy's 5A (for HCT116) over four days, 3CAI notably increased apoptotic cell numbers versus untreated controls. Additionally, 3CAI markedly reduced AKT-mediated phosphorylation of mTOR (Ser2448) and GSK3β (Ser9) in a time-dependent manner, while also elevating pro-apoptotic proteins p53 and p21 after 12 or 24 hours of treatment. In vitro kinase assays revealed that 3CAI solely inhibits AKT1 kinase activity without affecting the activities of MEK1, JNK1, ERK1, and TOPK at 1 μM. Its capability to suppress AKT1 and AKT2 activities indicates a dose-dependent effect, with a profound impact on downstream AKT targets and the induction of apoptosis. |
In vivo | To assess the in vivo antitumor efficacy of 3CAI, athymic nude mice with HCT116 cancer cell-induced tumors on their right flank were orally administered 3CAI at doses of 20 or 30 mg/kg, I3C at 100 mg/kg, or a vehicle control, five times weekly for a duration of 21 days. The higher dosage of 3CAI (30 mg/kg) was found to notably suppress the expression of AKT-target proteins in tumor tissues. Furthermore, this dosage significantly reduced tumor growth by 50% compared to the control group (p<0.05), without inducing noticeable side effects or substantial weight loss in the mice, suggesting a good tolerance to the treatment. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 246 mg/mL (1270.46 mM), Sonication is recommended.
|
Keywords | 3CAI | Inhibitor | inhibit | Akt | Protein kinase B | PKB |
Inhibitors Related | Ethyl gallate | Oridonin | Capivasertib | SKLB-163 | Scutellarin | Artemisinin | Honokiol | 2,3-Butanediol | MK-2206 dihydrochloride | AKT Kinase Inhibitor |
Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Antioxidant Compound Library | Inhibitor Library | Metabolism Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Neuronal Differentiation Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
|
$50.00/5mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |