For research use only. Not for therapeutic Use.
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 (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].
KP372-1(10, 20 mg/kg; i.v.; single daily for 33 days) induces NADH oxidation and impairs tumor growth in vivo without apparent toxicity[2].
| Catalog Number | I011437 |
| CAS Number | 1374996-60-7 |
| Synonyms | 10,11,12,13,14,16-hexazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(16),2,4,6,9,12,14-heptaen-8-one;10,12,13,14,15,16-hexazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(16),2,4,6,9,11,13-heptaen-8-one |
| Molecular Formula | C20H8N12O2 |
| Purity | ≥95% |
| InChI | InChI=1S/2C10H4N6O/c17-9-6-4-2-1-3-5(6)7-8(9)11-10-12-14-15-16(10)13-7;17-9-6-4-2-1-3-5(6)7-8(9)13-16-10(11-7)12-14-15-16/h2*1-4H |
| InChIKey | CWFOAASSUQIXOW-UHFFFAOYSA-N |
| SMILES | C1=CC=C2C(=C1)C3=NC4=NN=NN4N=C3C2=O.C1=CC=C2C(=C1)C3=NN4C(=NN=N4)N=C3C2=O |
| Reference | [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. [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. [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. |
