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MK-2206 dihydrochloride (CAS 1032350-13-2)

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Alternate Names:
MK-2206 dihydrochloride is also known as MK2206.
Application:
MK-2206 dihydrochloride is a highly selective pan-Akt inhibitor activated by the pleckstrin homology domain.
CAS Number:
1032350-13-2
Molecular Weight:
480.39
Molecular Formula:
C25H21N5O•2HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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MK-2206 dihydrochloride is a highly selective inhibitor of Akt1, Akt2 and Akt3 with IC50 values of 8 nM, 12 nM and 65 nM, respectively. It is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 dihydrochloride inhibits auto-phosphorylation of both Akt T308 and S473. It also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins. Additionally, it shows synergistic responses in combination with cytotoxic agents such as Erlotinib (sc-202154) or Lapatinib (sc-353658) in lung NCI-H460 or ovarian A2780 tumor cells. MK-2206 dihydrochloride inhibits the nasopharyngeal carcinoma (NPC) cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 proliferation in dose- and time-dependent manner. MK-2206 dihydrochloride is also known as MK2206, MK 2206, MK-2206 2HCl, and 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-onedihydrochloride.


MK-2206 dihydrochloride (CAS 1032350-13-2) References

  1. MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo.  |  Hirai, H., et al. 2010. Mol Cancer Ther. 9: 1956-67. PMID: 20571069
  2. Activation of phosphatidylinositol 3-kinase/Akt signaling pathway mediates acquired resistance to sorafenib in hepatocellular carcinoma cells.  |  Chen, KF., et al. 2011. J Pharmacol Exp Ther. 337: 155-61. PMID: 21205925
  3. eEF-2 kinase dictates cross-talk between autophagy and apoptosis induced by Akt Inhibition, thereby modulating cytotoxicity of novel Akt inhibitor MK-2206.  |  Cheng, Y., et al. 2011. Cancer Res. 71: 2654-63. PMID: 21307130
  4. Cytotoxic activity of the novel Akt inhibitor, MK-2206, in T-cell acute lymphoblastic leukemia.  |  Simioni, C., et al. 2012. Leukemia. 26: 2336-42. PMID: 22614243
  5. A novel PKB/Akt inhibitor, MK-2206, effectively inhibits insulin-stimulated glucose metabolism and protein synthesis in isolated rat skeletal muscle.  |  Lai, YC., et al. 2012. Biochem J. 447: 137-47. PMID: 22793019
  6. Inhibition of AKT with the orally active allosteric AKT inhibitor, MK-2206, sensitizes endometrial cancer cells to progestin.  |  Pant, A., et al. 2012. PLoS One. 7: e41593. PMID: 22911820
  7. Cigarette smoke-induced alveolar epithelial-mesenchymal transition is mediated by Rac1 activation.  |  Shen, HJ., et al. 2014. Biochim Biophys Acta. 1840: 1838-49. PMID: 24508121
  8. Lipid Emulsion Inhibits Apoptosis Induced by a Toxic Dose of Verapamil via the Delta-Opioid Receptor in H9c2 Rat Cardiomyoblasts.  |  Ok, SH., et al. 2017. Cardiovasc Toxicol. 17: 344-354. PMID: 27990618
  9. Peanut sprout extract attenuates cisplatin-induced ototoxicity by induction of the Akt/Nrf2-mediated redox pathway.  |  Youn, CK., et al. 2017. Int J Pediatr Otorhinolaryngol. 92: 61-66. PMID: 28012535
  10. Activation of phosphatidylinositol 3-kinase/AKT/snail signaling pathway contributes to epithelial-mesenchymal transition-induced multi-drug resistance to sorafenib in hepatocellular carcinoma cells.  |  Dong, J., et al. 2017. PLoS One. 12: e0185088. PMID: 28934275
  11. MicroRNA‑320a suppresses tumor cell growth and invasion of human breast cancer by targeting insulin‑like growth factor 1 receptor.  |  Guan, J., et al. 2018. Oncol Rep. 40: 849-858. PMID: 29989645
  12. [Corrigendum] Daily or weekly dosing with EGFR inhibitors, gefitinib and lapatinib, and AKT inhibitor MK2206 in mammary cancer models.  |  Lubet, RA., et al. 2019. Oncol Rep. 41: 718. PMID: 30365076
  13. Thiocoraline mediates drug resistance in MCF-7 cells via PI3K/Akt/BCRP signaling pathway.  |  Jin, J., et al. 2019. Cytotechnology. 71: 401-409. PMID: 30689149
  14. PEDF increases GLUT4-mediated glucose uptake in rat ischemic myocardium via PI3K/AKT pathway in a PEDFR-dependent manner.  |  Yuan, Y., et al. 2019. Int J Cardiol. 283: 136-143. PMID: 30819588
  15. MK-2206 Alleviates Renal Fibrosis by Suppressing the Akt/mTOR Signaling Pathway In Vivo and In Vitro.  |  Chen, M., et al. 2022. Cells. 11: PMID: 36359901

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

MK-2206 dihydrochloride, 5 mg

sc-364537
5 mg
$178.00

MK-2206 dihydrochloride, 10 mg

sc-364537A
10 mg
$325.00

How did you get this result "MK-2206 is a highly selective inhibitor of Akt1, Akt2, and Akt3 with IC50 values of 8 nM, 12 nM and 65 nM, respectively. "? Here, " IC50 values of 8 nM, 12 nM and 65 nM"?

Asked by: Suikoshin
Thank you for your inquiry. These values are taken from published literature on the compound, not tested in house. Please contact Technical Service by phone, (800)-457-3801 option 2, email <scbt@scbt.com>, or by live chat directly on our website, www.scbt.com if you have any further questions.
Answered by: Technical Service
Date published: 2017-04-11

What is this soluble in?

Asked by: SCM4
MK-2206 dihydrochloride is soluble in DMSO (14 mg/ml), water (1 mg/ml), and ethanol (<1 mg/ml) at 25°C.
Answered by: Tech Service 11
Date published: 2017-02-24
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Rated 5 out of 5 by from KongKong, X. et al. (PubMed 26167511) found that MK-2206, a highly selective inhibitor of Akt1, Akt2 and Akt3, completely abolished anti-glucotoxicity effect of FLZ. -SCBT Publication Review
Date published: 2015-07-16
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MK-2206 dihydrochloride is rated 5.0 out of 5 by 1.
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