MedChemExpress LLC (MCE)

MedChemExpress - Model KP372-1 - 1374996-60-7

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)[1][2][3].

KP372-1

MCE China：KP372-1

Brand：MedChemExpress (MCE)

Cat. No.HY-15673

CAS：1374996-60-7

Purity：99.75%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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).

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].

In Vivo：KP372-1(10, 20 mg/kg; p.o.; single daily for 33 days) induces NADH oxidation and impairs tumor growth in vivo without apparent toxicity[2].

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]

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