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Akt &GSK-3

AZD2858 (486424-20-8)

AZD2858 is a potent and GSK-3 inhibitor with an IC50 of 68 nM. AZD-2858 inhibits tau phosphorylation at the S396 site, and it activates Wnt signaling pathway. AZD2858 has a substantial impact on fracture healing. The fractures healed with a bony callus without an obvious endochondral component, suggesting that AZD2858 drives mesenchymal cells into the osteoblastic pathway.

Not Intended for Therapeutic Use. For research use only.

CAS: 486424-20-8 Category

AZD2858 (486424-20-8) Description:

Glycogen synthase kinase 3β (GSK3β) was originally identified for its ability to constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.1 It can also phosphorylate proteins that are relevant to osteogenesis and Alzheimer’s disease, the latter for which it has earned the moniker, tau phosphorylating kinase.2,3,4 AZD 2858 is a pyrazine analog that inhibits GSK3β with a Ki value of 4.9 nM.5 It crosses the blood brain barrier and inhibits tau phosphorylation in vitro with an IC50 value of 76 nM.5 AZD 2858 has also been shown to increase bone mass (via Wnt activation) in rats after a two-week treatment with a maximum effective oral dose of 20 mg/kg once daily.6 Furthermore, by inhibiting GSK3β, AZD 2858 can stabilize β-catenin in rat mesenchymal stem cells (EC50 = 234 nM), spurring osteoblast differentiation.7

AZD2858 (486424-20-8) Specifications:

Product Name AZD2858
Synonym AZD-2858; AZD 2858; AZD2858.
Chemical Name 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-2-pyrazinecarboxamide
Drug Class Potent and GSK-3 inhibitor
Purity ≥98% (HPLC)
CAS Number 486424-20-8
Molecular Formula C21H23N7O3S
Molecular Weight 453.5
Monoisotopic Mass 453.5g/mol
MDL number MFCD26397072
InChIKey FHCSBLWRGCOVPT-UHFFFAOYSA-N
InChi Code InChI=1S/C21H23N7O3S/c1-27-9-11-28(12-10-27)32(30,31)17-6-4-15(5-7-17)18-14-24-20(22)19(26-18)21(29)25-16-3-2-8-23-13-16/h2-8,13-14H,9-12H2,1H3,(H2,22,24)(H,25,29)
SMILES NC1=NC=C(C2=CC=C(S(N3CCN(C)CC3)(=O)=O)C=C2)N=C1C(NC4=CC=CN=C4)=O
Form A crystalline solid
Color White to off-white
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application A potent and GSK-3 inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Asuni, A.A., Hooper, C., Reynolds, C.H., et al. GSK3α exhibits β-catenin and tau directed kinase activities that are modulated by Wnt European Journal of Neuroscience 24(12), 3387-3392 (2006).

[2]. Guerrero, F., Herencia, C., Almadén, Y., et al. TGF-β prevents phosphate-induced osteogenesis through inhibition of BMP and Wnt/β-catenin pathwaysPLoS One 9(2),e89179 (2014).

[3]. Gilmour, P.S., O’Shea, P.J., Fagura, M., et al. Human stem cell osteoblastogenesis mediated by novel glycogen synthase kinase 3 inhibitors induces bone formation and a unique bone turnover biomarker profile in rats Toxicology and Applied Pharmacology 272(2),399-407 (2013).

[4].Sisask G, Marsell R, Sundgren-Andersson A, Larsson S, Nilsson O, Ljunggren O,  Jonsson KB. Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone. 2013 May;54(1):126-32. doi: 10.1016/j.bone.2013.01.019. Epub 2013 Jan 19. PubMed PMID: 23337038.

[5]. Marsell R, Sisask G, Nilsson Y, Sundgren-Andersson AK, Andersson U, Larsson S, Nilsson O, Ljunggren O, Jonsson KB. GSK-3 inhibition by an orally active small molecule increases bone mass in rats. Bone. 2012 Mar;50(3):619-27. doi: 10.1016/j.bone.2011.11.007. Epub 2011 Nov 25. PubMed PMID: 22142634.

1 review for AZD2858 (486424-20-8)

  1. Cofttek

    Never had such good experience before,The AZD2858 (486424-20-8) is high purity,also customer service is pretty nice !gotta try!!

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