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CCT128930 (CAS 885499-61-6)

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Alternate Names:
4-[(4-chlorophenyl)methyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amine
Application:
CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2
CAS Number:
885499-61-6
Purity:
≥98%
Molecular Weight:
341.84
Molecular Formula:
C18H20ClN5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 (IC50: 6 nM). CCT128930 may act to exhibit marked antiproliferative activity against PTEN-deficient human tumor cell lines including U87MG human glioblastoma cells, LNCaP human prostate cancer cells and PC3 human prostate cancer cells (GI50′s: U87MG = 6.3 muM, LNCaP = 0.35 mumol/L and PC3 = 1.9 mumol/L). Furthermore, CCT128930 causes a G1 arrest in PTEN-null U87MG human glioblastoma cells and Akt pathway blockade.


CCT128930 (CAS 885499-61-6) References

  1. Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930.  |  Yap, TA., et al. 2011. Mol Cancer Ther. 10: 360-71. PMID: 21191045
  2. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition.  |  Wang, FZ., et al. 2014. Biochimie. 103: 118-25. PMID: 24793486
  3. Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors.  |  Fang, Z., et al. 2015. ACS Chem Biol. 10: 279-88. PMID: 24959717
  4. Epigenetic changes of EGFR have an important role in BRAF inhibitor-resistant cutaneous melanomas.  |  Wang, J., et al. 2015. J Invest Dermatol. 135: 532-541. PMID: 25243790
  5. Inhibition of Phospho-S6 Kinase, a Protein Involved in the Compensatory Adaptive Response, Increases the Efficacy of Paclitaxel in Reducing the Viability of Matrix-Attached Ovarian Cancer Cells.  |  Choi, JI., et al. 2016. PLoS One. 11: e0155052. PMID: 27148873
  6. High-concentration hydrogen protects mouse heart against ischemia/reperfusion injury through activation of thePI3K/Akt1 pathway.  |  Chen, O., et al. 2017. Sci Rep. 7: 14871. PMID: 29093541
  7. Inhibitors of AKT kinase increase LDL receptor mRNA expression by two different mechanisms.  |  Bjune, K., et al. 2019. PLoS One. 14: e0218537. PMID: 31216345
  8. Neutrophils homing into the retina trigger pathology in early age-related macular degeneration.  |  Ghosh, S., et al. 2019. Commun Biol. 2: 348. PMID: 31552301
  9. Dual-Targeting AKT2 and ERK in cancer stem-like cells in neuroblastoma.  |  Kim, KW., et al. 2019. Oncotarget. 10: 5645-5659. PMID: 31608140
  10. CCT128930 induces G1-phase arrest and apoptosis and synergistically enhances the anticancer efficiency of VS5584 in human osteosarcoma cells.  |  Sun, JY., et al. 2020. Biomed Pharmacother. 130: 110544. PMID: 32721630
  11. Corrigendum to 'CCT128930 induces G1-phase arrest and apoptosis and synergistically enhances the anticancer efficiency of VS5584 in human osteosarcoma cells' [Biomed. Pharmacother. 130 (2020) 110544].  |  Sun, JY., et al. 2020. Biomed Pharmacother. 132: 110931. PMID: 33254436
  12. CCT128930 is a novel and potent antagonist of TRPM7 channel.  |  Guan, Z., et al. 2021. Biochem Biophys Res Commun. 560: 132-138. PMID: 33989904
  13. Modulators of TRPM7 and its potential as a drug target for brain tumours.  |  Ji, D., et al. 2022. Cell Calcium. 101: 102521. PMID: 34953296
  14. Repression of the iron exporter ferroportin may contribute to hepatocyte iron overload in individuals with type 2 diabetes.  |  Qiu, R., et al. 2022. Mol Metab. 66: 101644. PMID: 36436807
  15. PM2.5 induces cardiac malformations via PI3K/akt2/mTORC1 signaling pathway in zebrafish larvae.  |  Jiang, Y., et al. 2023. Environ Pollut. 323: 121306. PMID: 36804889

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

CCT128930, 5 mg

sc-364459
5 mg
$153.00

CCT128930, 10 mg

sc-364459A
10 mg
$286.00

Do you have an Akt specific inhibitor that is not covered by a patent or that it will be soon generic? thank you shoshi

Asked by: shoshi
Thank you for your question. We offer quite a few chemicals that are Akt Inhibitors. You can find them on our website. https://www.scbt.com/scbt/browse/Chemicals-Protein-Interacting-Inhibitors-Activators-and-Substrates-Protein-Inhibitors/_/N-70w8k?Ntt=akt+inhibitor If you have any further questions, please contact our European Technical Service team. You can reach them by phone at Toll Free: +49 6221 4503 0, by email at: europe@scbt.com or by live chat directly on our website, www.scbt.com
Answered by: Tech Service
Date published: 2017-06-27
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Rated 5 out of 5 by from Wang FZ; et alWang FZ; et al. (PubMed ID: 24793486) determined that higher doses of CCT128930 increased apoptosis and activation of caspase-3, caspase-9, and PARP. -SCBT Publication Review
Date published: 2015-02-11
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CCT128930 is rated 5.0 out of 5 by 1.
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