Date published: 2025-10-15

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GSK 429286 (CAS 864082-47-3)

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Alternate Names:
dihydropyridone indazole
Application:
GSK 429286 is a selective Rho-kinase inhibitor that reverses adrenalin-induced contraction
CAS Number:
864082-47-3
Molecular Weight:
432.37
Molecular Formula:
C21H16F4N4O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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GSK 429286 is a compound potent and selective inhibition of the enzyme phosphoinositide 3-kinase (PI3K). By precisely binding to the ATP-binding pocket of the PI3K enzyme, GSK 429286 effectively blocks the enzymatic activity necessary for the phosphorylation of phosphatidylinositol 4,5-bisphosphate (PIP2) into phosphatidylinositol 3,4,5-trisphosphate (PIP3). This action disrupts the PI3K/Akt signaling pathway, a conduit for regulating cellular functions such as growth, proliferation, and survival. The selectivity of GSK 429286 for PI3K over other kinases ensures minimal off-target effects, making it exemplary in molecular biology and biochemical for elucidating the complex roles of PI3K signaling. This inhibitor serves as a critical resource in various, facilitating detailed studies on the modulation of cellular processes and the investigation of PI3K′s involvement in diverse cellular states. Through these studies, GSK 429286 helps in advancing our understanding of cellular signaling networks, offering insights into the molecular dynamics that govern cell behavior under various physiological and pathophysiological conditions.


GSK 429286 (CAS 864082-47-3) References

  1. H1152 promotes the degradation of polyglutamine-expanded ataxin-3 or ataxin-7 independently of its ROCK-inhibiting effect and ameliorates mutant ataxin-3-induced neurodegeneration in the SCA3 transgenic mouse.  |  Wang, HL., et al. 2013. Neuropharmacology. 70: 1-11. PMID: 23347954
  2. The effect of Rho kinase inhibition on long-term keratinocyte proliferation is rapid and conditional.  |  Chapman, S., et al. 2014. Stem Cell Res Ther. 5: 60. PMID: 24774536
  3. Induction of oligodendrocyte differentiation and in vitro myelination by inhibition of rho-associated kinase.  |  Pedraza, CE., et al. 2014. ASN Neuro. 6: PMID: 25289646
  4. A Podocyte-Based Automated Screening Assay Identifies Protective Small Molecules.  |  Lee, HW., et al. 2015. J Am Soc Nephrol. 26: 2741-52. PMID: 25858967
  5. Rho-associated kinase 1 inhibition is synthetically lethal with von Hippel-Lindau deficiency in clear cell renal cell carcinoma.  |  Thompson, JM., et al. 2017. Oncogene. 36: 1080-1089. PMID: 27841867
  6. Targeting the RhoGTPase/ROCK pathway for the treatment of VHL/HIF pathway-driven cancers.  |  Thompson, JM., et al. 2020. Small GTPases. 11: 32-38. PMID: 28632992
  7. Neural Precursor-Derived Pleiotrophin Mediates Subventricular Zone Invasion by Glioma.  |  Qin, EY., et al. 2017. Cell. 170: 845-859.e19. PMID: 28823557
  8. Diverse signalling of the platelet P2Y1 receptor leads to a dichotomy in platelet function.  |  Amison, RT., et al. 2018. Eur J Pharmacol. 827: 58-70. PMID: 29534999
  9. Phospho-substrate profiling of Epac-dependent protein kinase C activity.  |  Goode, DJ. and Molliver, DC. 2019. Mol Cell Biochem. 456: 167-178. PMID: 30739223
  10. A high-throughput drug combination screen of targeted small molecule inhibitors in cancer cell lines.  |  Flobak, Å., et al. 2019. Sci Data. 6: 237. PMID: 31664030
  11. Strategies to Enhance Logic Modeling-Based Cell Line-Specific Drug Synergy Prediction.  |  Niederdorfer, B., et al. 2020. Front Physiol. 11: 862. PMID: 32848834
  12. Cardiac Safety of Kinase Inhibitors - Improving Understanding and Prediction of Liabilities in Drug Discovery Using Human Stem Cell-Derived Models.  |  Ziegler, R., et al. 2021. Front Cardiovasc Med. 8: 639824. PMID: 34222360
  13. Laminin-511-derived recombinant fragment and Rho kinase inhibitor Y-27632 facilitate serial cultivation of keratinocytes differentiated from human embryonic stem cells.  |  Takagi, R., et al. 2021. Regen Ther. 18: 242-252. PMID: 34409136

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

GSK 429286, 1 mg

sc-361200
1 mg
$39.00

GSK 429286, 5 mg

sc-361200B
5 mg
$123.00

GSK 429286, 10 mg

sc-361200A
10 mg
$230.00