PI3K/AKT-IN-1
Based on 16 publication(s) in Google Scholar
PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.64%
- CAS No.: 3033069-84-7
- Formule: C23H23N5O4S
- Masse moléculaire:465.52
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) PI3K/AKT-IN-1
More- Nat Aging. 2026 Jul;6(7):1395-1416.
- Drug Resist Updat. 2025 Jan:78:101179. [Abstract]
- Nat Commun. 2025 May 22;16(1):4779. [Abstract]
- Gut Microbes. 2025 Dec;17(1):2449095. [Abstract]
- Adv Sci (Weinh). 2024 Jun;11(23):e2308986. [Abstract]
- Adv Sci (Weinh). 2022 Jul 28;e2200546. [Abstract]
- Cell Death Discov. 2025 Nov 7;11(1):511. [Abstract]
- Acta Pharmacol Sin. 2024 Apr;45(4):844-856. [Abstract]
- Sci China Life Sci. 2025 Mar;68(3):746-763. [Abstract]
- Int J Mol Sci. 2023 Nov 21;24(23):16552. [Abstract]
- Toxicology. 2023 Feb:485:153426. [Abstract]
- Neuropharmacology. 2026 Jul 1:292:110950. [Abstract]
- Curr Issues Mol Biol. 2025 Jun 20;47(7):478. [Abstract]
- Aquac Rep. 2025 Sep 15.
- Exp Ther Med. 2023 Sep 14;26(5):507. [Abstract]
- Biomed Pharmacother. 2024 Jan:170:116012. [Abstract]
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Activité biologique
Description
IC50 & Target
[1]|
PI3Kγ 6.99 μM (IC50) |
PI3Kδ 4.01 μM (IC50) |
In Vitro
PI3K/AKT-IN-1 (compound 7f) (0.04-100 µM; 48 hours) has high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 µM) than on the breast cancer cell line (MCF-7 IC50=3.22 µM)[1].
PI3K/AKT-IN-1 (2.62 µM) can promote S-phase cell cycle arrest and apoptosis induction in K562 cells[1].
PI3K/AKT-IN-1 (2.62 µM; 48 hours) causes an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage[1].
PI3K/AKT-IN-1 (2.62 µM; 48 hours) markedly reduces the expression of PI3K, AKT, Cyclin D1 and NF-κB[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 and K562 cells[1]
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Concentration:0.04-100 µM
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Incubation Time:48 hours
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Result:Demonstrated high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 µM) than on the breast cancer cell line (MCF-7 IC50=3.22 µM).
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Cell Line:K562 cells[1]
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Concentration:2.62 µM
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Incubation Time:
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Result:Promoted S-phase cell cycle arrest and apoptosis induction.
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Cell Line:K562 cells[1]
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Concentration:2.62 µM
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Incubation Time:48 hours
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Result:Caused an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage.
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Cell Line:K562 cells[1]
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Concentration:2.62 µM
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Incubation Time:48 hours
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Result:Markedly reduced the expression of PI3K, p-PI3K, AKT, p-AKT, Cyclin D1 and NF-κB.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female rats (180-200g)[1]
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Dosage:2000 mg/kg
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Administration:p.o.; single
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Result:The median lethal dose (LD50) was greater than the test dose (2000 mg/kg).
Chemical Information
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CAS No. 3033069-84-7
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Appearance Solid
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Masse moléculaire 465.52
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Formule C23H23N5O4S
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Color Off-white to light yellow
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SMILES
N#CC1=C(N/N=C/C2=CC(OC)=C(OC)C(OC)=C2)N=C(SC)N=C1C3=CC=C(OC)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (16)
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Journal Impact Factor
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Most Recent
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Drug Resist Updat
CEA-induced PI3K/AKT pathway activation through the binding of CEA to KRT1 contributes to oxaliplatin resistance in gastric cancer. [Abstract]2025 Jan:78:101179. PMID: 39644827 -
Nat Commun
NNMT/1-MNA protects against hepatic ischemia-reperfusion injury through the AKT/FOXO1/ANGPT2/JNK axis. [Abstract]2025 May 22;16(1):4779. PMID: 40404636
PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 22;16(1):4779. [Abstract]
We treated primary hepatocytes with the PI3K/AKT specific inhibitor PI3K/AKT-IN-1 (10 μM) and found that the inhibitory effect of NNMT/1-MNA on FOXO1 and ANGPT2 was partially reduced.
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Gut Microbes
Maternal milk fat globule membrane enriched gut L. murinus and circulating SCFAs to improve placental efficiency and fetal development in intrauterine growth restricted mice model. [Abstract]2025 Dec;17(1):2449095. PMID: 39762283
PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec;17(1):2449095. [Abstract]
Amino acid shortage model (AAS) for placental BeWo cells was established by mixing basic and amino acid-free DMEM/F12 medium (7:1), and supplemented with/without SCFAs cocktail and/or PI3K/AKT-IN-1 for 24 h. Relative gene expressions of inflammatory cytokines.
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Adv Sci (Weinh)
Mgp High-Expressing MSCs Orchestrate the Osteoimmune Microenvironment of Collagen/Nanohydroxyapatite-Mediated Bone Regeneration. [Abstract]2024 Jun;11(23):e2308986. PMID: 38588510 -
Adv Sci (Weinh)
Succinylation Inhibits the Enzymatic Hydrolysis of the Extracellular Matrix Protein Fibrillin 1 and Promotes Gastric Cancer Progression. [Abstract]2022 Jul 28;e2200546. PMID: 35901491 -
Cell Death Discov
Pregnane X receptor protects against age-related bone loss in males via PI3K/Akt-mediated inhibition of apoptosis. [Abstract]2025 Nov 7;11(1):511. PMID: 41203627
PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Nov 7;11(1):511. [Abstract]
We performed Pxr overexpression in these cells by using the plasmid containing the full-length coding sequence of Mus musculus Nr1i2 (PNr1i2) or empty vector as negative control (PNC), and used PI3K/AKT-IN-1 (5 μM), a specific inhibitor of the PI3K/Akt pathway, to assess the pathway’s role in mediating Pxr function in BMSCs.
PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Nov 7;11(1):511. [Abstract]
Pxr overexpression significantly enhanced PI3K/Akt pathway activity in aged BMSCs, while treatment with the inhibitor PI3K/AKT-IN-1 (5 μM) suppressed this Pxr overexpression-induced activation of the PI3K/Akt pathway.
PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Nov 7;11(1):511. [Abstract]
The promotional effect of Pxr overexpression on osteogenesis in aged BMSCs was significantly weakened by the addition of PI3K/AKT-IN-1 (5 μM).
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Acta Pharmacol Sin
SMAD4 endows TGF-β1-induced highly invasive tumor cells with ferroptosis vulnerability in pancreatic cancer. [Abstract]2024 Apr;45(4):844-856. PMID: 38057506
PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Apr;45(4):844-856. [Abstract]
Wound healing assay were used to evaluate cell motility, respectively, in PANC-1 cell lines treated with TGF-β1 (5 ng/ml, 24 h) and a MAPK1/ERK2-MAPK3/ERK1 inhibitor (U0126), MAPK/p38 inhibitor (SB203580), MAPK/JNK inhibitor (SP600125), PI3K/AKT-IN-1 (HY-144806), RAC1 inhibitor and CDC42 inhibitor.
PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Apr;45(4):844-856. [Abstract]
Transwell invasion were used to evaluate cell invasion, respectively, in PANC-1 cell lines treated with TGF-β1 (5 ng/ml, 24 h) and a MAPK1/ERK2-MAPK3/ERK1 inhibitor (U0126), MAPK/p38 inhibitor (SB203580), MAPK/JNK inhibitor (SP600125), PI3K/AKT-IN-1 (HY-144806), RAC1 inhibitor and CDC42 inhibitor.
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Sci China Life Sci
Integrating spatial transcriptomics and single-nucleus RNA-seq revealed the specific inhibitory effects of TGF-β on intramuscular fat deposition. [Abstract]2025 Mar;68(3):746-763. PMID: 39422812 -
Int J Mol Sci
Melatonin Inhibits Testosterone Synthesis in Rooster Leydig Cells by Targeting CXCL14 through miR-7481-3p. [Abstract]2023 Nov 21;24(23):16552. PMID: 38068875 -
Toxicology
Protective role of cezanne in doxorubicin-induced cardiotoxicity by inhibiting autophagy, apoptosis and oxidative stress. [Abstract]2023 Feb:485:153426. PMID: 36639017 -
Neuropharmacology
Novel mechanism of hypidone hydrochloride (YL-0919) in Parkinson's disease: inhibiting neuronal ferroptosis by targeting the Sigma1R-PI3K-AKT-ACSL4 axis. [Abstract]2026 Jul 1:292:110950. PMID: 41887568 -
Curr Issues Mol Biol
IGFBP2 Modulates Trophoblast Function and Epithelial-Mesenchymal Transition in Preeclampsia via the PI3K/AKT Signaling Pathway. [Abstract]2025 Jun 20;47(7):478. PMID: 40728947 -
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Exp Ther Med
Salidroside inhibits renal ischemia/reperfusion injury‑induced ferroptosis by the PI3K/AKT signaling pathway. [Abstract]2023 Sep 14;26(5):507. PMID: 37822587 -
Biomed Pharmacother
Berberine exerts antidepressant effects in vivo and in vitro through the PI3K/AKT/CREB/BDNF signaling pathway. [Abstract]2024 Jan:170:116012. PMID: 38113631
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (107.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1481 mL | 10.7407 mL | 21.4814 mL | 53.7034 mL |
| 5 mM | 0.4296 mL | 2.1481 mL | 4.2963 mL | 10.7407 mL | |
| 10 mM | 0.2148 mL | 1.0741 mL | 2.1481 mL | 5.3703 mL | |
| 15 mM | 0.1432 mL | 0.7160 mL | 1.4321 mL | 3.5802 mL | |
| 20 mM | 0.1074 mL | 0.5370 mL | 1.0741 mL | 2.6852 mL | |
| 25 mM | 0.0859 mL | 0.4296 mL | 0.8593 mL | 2.1481 mL | |
| 30 mM | 0.0716 mL | 0.3580 mL | 0.7160 mL | 1.7901 mL | |
| 40 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3426 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0741 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8951 mL | |
| 80 mM | 0.0269 mL | 0.1343 mL | 0.2685 mL | 0.6713 mL | |
| 100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5370 mL |
PI3K/AKT-IN-1 Related Classifications
HY-144806 Related Classifications
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