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S6 kinase&PKD-1

GSK2334470 (1227911-45-6)

GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases.-PDK inhibitor.

Not Intended for Therapeutic Use. For research use only.

CAS: 1227911-45-6 Category

GSK2334470 (1227911-45-6) Description

3-Phosphoinositide-dependent protein kinase (PDK1) is a serine-threonine kinase that plays an important role in growth factor signaling by phosphorylating and activating a group of kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC. GSK2334470 is an inhibitor of PDK1 (IC50 = ~10 nM) that even at 100-fold higher concentrations does not affect the activity of 93 other protein kinases, including that of 13 closely related AGC kinase family members. In HEK293 cells, 30 nM – 1 µM GSK2334470 suppresses T-loop phosphorylation and activation of SGK, S6K1, and RSK, as well as the activation of Akt. GSK2334470 also inhibited T-loop phosphorylation and activation of Akt. GSK2334470 will be a useful tool for delineating the roles of PDK1 in biological processes.

GSK2334470 (1227911-45-6) Specifications

Product Name GSK2334470
Synonym GSK2334470; GSK 2334470; GSK-2334470
Chemical Name (3S,6R)-1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide
Drug Class 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor
Purity ≥98% (HPLC)
CAS Number 1227911-45-6
Molecular Formula C25H34N8O
Molecular Weight 462.6
Monoisotopic Mass 462.28556  g/mol
MDL number MFCD16660191
InChIKey QLPHOXTXAKOFMU-WBVHZDCISA-N
InChi Code InChI=1S/C25H34N8O/c1-15-8-9-17(24(34)28-18-6-4-3-5-7-18)14-33(15)22-13-20(29-25(27-2)30-22)16-10-11-19-21(12-16)31-32-23(19)26/h10-13,15,17-18H,3-9,14H2,1-2H3,(H,28,34)(H3,26,31,32)(H,27,29,30)/t15-,17+/m1/s1
SMILES NC1=NNC2=CC(C3=CC(N4C[[email protected]@H](C(NC5CCCCC5)=O)CC[[email protected]]4C)=NC(NC)=N3)=CC=C21
Form A crystalline solid
Color White
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application A potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor

 


RIDADR NONH for all modes of transport

References:

[1]. Knight ZA. For a PDK1 inhibitor, the substrate matters. Biochem J. 2011 Jan 15;433(2):e1-2. doi: 10.1042/BJ20102038. PubMed PMID: 21175429.

[2]. Najafov A, Sommer EM, Axten JM, Deyoung MP, Alessi DR. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem J. 2011 Jan 15;433(2):357-69. doi: 10.1042/BJ20101732. PubMed PMID: 21087210.

[3]. Najafov, A., Sommer, E.M., Axten, J.M., et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1 Biochemistry Journal433(2),357-369 (2011).

[4].Gutiérrez-Martínez; Rubio; Piedra-Quintero; Lopez-Mendez; Serrano; Reyes-Maldonado; Salinas-Lara; (…) Villegas-Sepúlveda; Nava – Translational Oncology 2019 vol. 12 # 1 p. 24 – 35

[5]. Li, Dong-Dong; Meng, Xiang-Feng; Wang, Qiang; Yu, Pan; Zhao, Lin-Guo; Zhang, Zheng-Ping; Wang, Zhen-Zhong; Xiao, Wei – Journal of Molecular Graphics and Modelling 2018 vol. 79 p. 81 – 87