KP372-1
Based on 3 publication(s) in Google Scholar
KP372-1 is an Akt inhibitor that inhibits proliferation and induces apoptosis and anoikis. KP372-1 is also an NQO1 redox cycling agent that causes DNA damage (including DNA breakage) by generating ROS. KP372-1 can be used in cancer research (such as head and neck squamous cell carcinoma (HNSCC) and pancreatic cancer).
For research use only. We do not sell to patients.
- Purity : 99.5%
- CAS No.: 1374996-60-7
- Formula: C20H8N12O2
- Molecular Weight:448.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) KP372-1
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Biological Activity
Description
In Vitro
KP372-1 (0.0625, 0.125, 0.25, 0.5, 1.0 μM; 48 h) inhibits growth of JMARc42 and Tu167c2 cells with IC50s of 200 and 100 nM, respectively[1].
KP372-1 (125 nM; 24 h) induces Tu167c2 cells apoptosis and induces anoikis in the JMARc42 cells[1].
KP372-1 (125 nM; 30 min) blocks Akt, thereby decreasing the phosphorylation of the S6 ribosomal protein in both Tu167 and JMAR cells[1].
KP372-1 (0.250, 0.5, 1.0 μM; 30 min) inhibits Akt kinase activity with an IC50 of 250 nM in JMAR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:JMARc42 and Tu167c2 cells
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Concentration:0.0625, 0.125, 0.25, 0.5, 1.0 µM
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Incubation Time:48 h
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Result:Showed antiproliferative activity.
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Cell Line:Tu167c2 and JMARc42 cells
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Concentration:125 nM
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Incubation Time:24 h
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Result:Induced approximately 90% of cells apoptosis.
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Cell Line:Tu167 and JMAR cells
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Concentration:125 nM
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Incubation Time:30 min
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Result:Induced a small but consistent decrease in Akt phosphorylation with a concomitant marked decrease in S6 phosphorylation.
Inhibited the EGF induced phosphorylation of Aktser473 in Tu167 and AktThr308 in JMAR.
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Cell Line:JMAR cells
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Concentration:0.250, 0.5, 1.0 µM
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Incubation Time:30 min
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Result:Significantly blocked Akt kinase activity in a dose-dependent fashion, with an IC50 of 250 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice (H1299 xenografts model)[2].
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Dosage:10, 20 mg/kg
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Administration:intragastric injection; single daily for 33 days
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Result:Affected tumor metabolism and suppressed tumor growth.
Chemical Information
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CAS No. 1374996-60-7
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Appearance Solid
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Molecular Weight 448.36
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Formula C20H8N12O2
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Color Light yellow to yellow
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SMILES
O=C1C2=C(C3=NC4=NN=NN4N=C31)C=CC=C2.O=C5C6=NC7=NN=NN7N=C6C8=C5C=CC=C8
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Biomaterials
Nano-sensitizer with self-amplified drug release and hypoxia normalization properties potentiates efficient chemoradiotherapy of pancreatic cancer. [Abstract]2024 Oct:310:122634. PMID: 38823195 -
J Control Release
Bladder cancer selective chemotherapy with potent NQO1 substrate co-loaded prodrug nanoparticles. [Abstract]2022 May 31;347:632-648. PMID: 35618186 -
J Biochem Mol Toxicol
Heme Oxygenase-1 Regulates the JAK/STAT Pathway to Inhibit Ferroptosis in Metabolic Dysfunction-Associated Steatotic Liver Disease. [Abstract]2026 Jan;40(1):e70661. PMID: 41486516
Solvent & Solubility
In Vitro:
DMSO : 17.86 mg/mL (39.83 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (288 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Mandal M, et al. The Akt inhibitor KP372-1 inhibits proliferation and induces apoptosis and anoikis in squamous cell carcinoma of the head and neck. Oral Oncol. 2006 Apr;42(4):430-9. [Content Brief]
[2]. Zhao Y, et al. SoNar, a Highly Responsive NAD+/NADH Sensor, Allows High-Throughput Metabolic Screening of Anti-tumor Agents. Cell Metab. 2015 May 5;21(5):777-89. [Content Brief]
[3]. Viera T, et al. DNA damage induced by KP372-1 hyperactivates PARP1 and enhances lethality of pancreatic cancer cells with PARP inhibition. Sci Rep. 2020 Nov 19;10(1):20210. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2304 mL | 11.1518 mL | 22.3035 mL | 55.7588 mL |
| 5 mM | 0.4461 mL | 2.2304 mL | 4.4607 mL | 11.1518 mL | |
| 10 mM | 0.2230 mL | 1.1152 mL | 2.2304 mL | 5.5759 mL | |
| 15 mM | 0.1487 mL | 0.7435 mL | 1.4869 mL | 3.7173 mL | |
| 20 mM | 0.1115 mL | 0.5576 mL | 1.1152 mL | 2.7879 mL | |
| 25 mM | 0.0892 mL | 0.4461 mL | 0.8921 mL | 2.2304 mL | |
| 30 mM | 0.0743 mL | 0.3717 mL | 0.7435 mL | 1.8586 mL |