Molecular structure of MK-2206 dihydrochloride, CAS Number: 1032350-13-2
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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SDS & Certificate of Analysis
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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- [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
- 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
- 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
- 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
Inhibitor of:
β-defensin 8, β-defensin 9, 1500010J02Rik, 1500012F01Rik, 1500016O10Rik, 1500035H01Rik, 1600002K03Rik, 1600012H06Rik, 1600014K23Rik, 1600016N20Rik, 1600023N17Rik, 3110007F17Rik, 9430016H08Rik, AI314180, AIDA, AKIP, Akt, Akt1, Akt2, Akt3, ALG-4, ANGEL2, AZI1, BRCAA1, BTBD10, BVES, C030030A07Rik, C030034I22Rik, C030037F17Rik, C030039L03Rik, C030048H21Rik, C12orf11, C12orf73, C130039O16Rik, C130074G19Rik, C130079G13Rik, C330006A16Rik, C330006K01Rik, C6orf130, C86695, CCDC150, CCDC151, CMTM7, CWH43, CYYR1, DIP2C, Dok-1, E2F-5, EG216818, EG330305, EG330513, EG330689, EG433365, EG622744, EG626215, ENPP5, FAM185A, FAM83B, FAM8A1, FARP1, FBXW18, FKHR, FKHRL1, FLJ35220, FLJ40125, FYTTD1, GAP-assoc p62, GIGYF2, GPBP, GRAMD4, GRB10, HPK1, IFIT1, ILKAP, IRS-1, IRS-4, KBTBD2, KIAA0195, LLGL2, LOC100041351, LOC100041356, LOC339047, LOC646864, LOC729974, Ly-55A, Ly-55B, MAGI-3, NICE-1, Olfr478, Olfr549, Olfr553, Olfr554, Olfr555, Olfr556, Olfr557, Olfr585, Olfr586, Olfr589, Olfr59, Olfr591, Olfr592, Olfr593, Olfr594, Olfr633, Olfr64, Olfr648, Olfr657, Olfr658, Olfr659, OTTMUSG00000012817, P1 Adhesion, p70 S6 kinase β, PCDH9_Pcdh9, Pecanex 1, PERQ1, PGs5, PHF14, PHLDA3, PIG11, PKB Kinase, PKNβ, PLEKHA6, PRAS40, PRR14, Ran BP-2, RAP1GDS1, RASAL2, RasGRP, RERGL, Ruvbl2, S-100A5, SAV1, Ser/Thr Protein Kinase, SIK2, SUR-5, Tap42, TAPP1, TAPT1, TBC1D1, TEF-4, UEV3, VGF, VRK2, WBSCR9, YadA, Ypk2, ZNF677, and ZPR1.Activator of:
4E-T, Atg4a, BJ-TSA-9, C030046E11Rik, Clm3, cyclin J, Dab2, DEPTOR, eIF3K, EVT-2, FTS, GABARAPL2, IL-20Rα, IL-3, IP6K2, JKTBP, KIAA0240, KIAA0317, LTβR, MK, MTMR15, NCoA-7, Nek11, NgR3, PFAAP5, PKM2, RBMXL2, Rif1, SGK, SGK3, SPRED1, UBE2C, and ZMAT2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
MK-2206 dihydrochloride, 5 mg | sc-364537 | 5 mg | $178.00 | |||
MK-2206 dihydrochloride, 10 mg | sc-364537A | 10 mg | $325.00 |