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작성일 : 14-03-07
[Chemdea] PI3K / mTOR Inhibitors (5)


PI3K / mTOR Inhibitors (5)


 

Product Name: TG100-115 - PI3Kγ/δ Inhibitor


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TG100-115 inhibited PI3Kγ and PI3Kδ (IC50 values of 83 and 235 nM, respectively), whereas both PI3Kα and PI3Kβ were

relatively unaffected (IC50 values >1 μM). In 133 protein kinase panel, TG100-115 did not show significant inhibition (IC50

values >1 μM). In a mouse murine asthma model, TG100-115 markedly reduced the pulmonary eosinophilia and the 

concomitant interleukin-13 and mucin accumulation. TG100-115 also inhibited inflammatory patterns in mouse smoke

model. In a rat and porcine model of myocardial infraction TG100-115 potently inhibited edema and inflammation in 

response to multiple mediators, including vascular endothelial growth factor and platelet-activating factor. By contrast,

endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage, was not disrupted.

   

Details


Chemical Formula:

 

C18H14N6O2

CAS No.:

 

677297-51-7

Molecular weight:

 

346.34.

Purity:

98% by HPLC

Appearance:

 

Yellow solid

Chemical name:

 

3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol  (6,7-Bis(3-hydroxyphenyl)pteridine-2,4-diamine)

Solubility:

 

DMSO (1 mg/mL)

Storage:

Protect from light. Packaged under inert gas


References


1. Doukas, J., et al.  J. Pharmacol. Exp. Ther. 2009, 328, 758;


 

Product Name: TGX-221 – PI3Kb Inhibitor VI


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A cell-permeable morpholino-pyrimidinone compound that acts as a reversible, ATP-competitive, selective, and highly 

potent inhibitor of PI 3-Kb (p110b IC50 = 0.005 µM, p110d IC50 = 0.1 µM, p110a IC50 = 5 µM, and p110b IC50 ≥3.5 µM)

with little activity against a panel of 15 commonly studied protein kinases even at concentrations as high as 10.0 µM. An 

excellent tool for studying p110b-dependent responses both in cells in vitro and in animals in vivo.


Details


Chemical Formula:

 

C21H24N4O2

CAS No.:

 

663619-89-4

Molecular weight:

 

364.44.

Purity:

98% by HPLC

Appearance:

 

White solid

Chemical name:

 

 (±)-7-Methyl-2-(morpholin-4-yl)-9-(1-phenylaminoethyl)-pyrido[1,2-a]-pyrimidin-4-one

Solubility:

 

DMSO (10 mg/mL), ethanol (5 mg/mL).

Storage:

Protect from light. Packaged under inert gas


References


1. Chaussade, C., et al. Biochem. J. 2007, 404, 449;

 


Product Name: Wortmannin (KY 12420)


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A cell-permeable, fungal metabolite that acts as a potent, selective, and irreversible inhibitor of phosphatidylinositol 3-

kinase in purified preparations and cytosolic fractions (IC50 = 5 nM). Blocks the catalytic activity of PI 3-kinase without

affecting the upstream signaling events. Preincubation of fibroblasts with Wortmannin abolishes PDGF-mediated Ins(3,4,5)

P3 formation (IC50 = 5 nM). Also blocks the metabolic effects of insulin in isolated rat adipocytes without affecting the

insulin receptor tyrosine kinase activity. Inhibits MAP kinase activation induced by platelet activating factor in guinea pig

neutrophils (200 - 300 nM). Also inhibits other kinases such as myosin light chain kinase (IC50 = 200 nM) and PI 4-kinase

at concentrations higher than that required for inhibition of PI 3-kinase. Also blocks phospholipase D.


Details


Chemical Formula:

 

C23H24O8

CAS No.:

 

19545-26-7

Molecular weight:

 

428.4

Purity:

99% by HPLC

Appearance:

 

White solid

Chemical name:

 

Wortmannin

Solubility:

 

DMSO (25 mg/mL), MeOH (5 mg/mL)

Storage:

Protect from light. Packaged under inert gas


References


1. Arcaro, A et al, Biochem. J. 1993, 296, 297; 



Product Name: ZSTK474 – PI3K a/b/g/d Inhibitor


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Cell permeable, reversible, potent and specific inhibitor of phosphoinositide 3-kinase (PI(3)K p110a IC50=6.7 nM,

p110b IC50=10.4 nM, p110g IC50=11.7 nM and p110δ Ki=1.8 nM). Blocks cellular PI(3)K/Akt (PKB) signalling in vitro and

inhibits Akt(PKB)-dependent tumor growth in mice in vivo without significant toxic effect. More effective than LY 294,002

in vitro and as in vivo.

   

Details


Chemical Formula:

 

C19H21F2N7O2

CAS No.:

 

475110-96-4

Molecular weight:

 

417.4.

Purity:

99% by HPLC

Appearance:

 

White solid

Chemical name:

 

2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine

Solubility:

 

DMSO (20mg/mL)

Storage:

Protect from light. Packaged under inert gas


References


1. Yaguchi, S. et al.; Proc. Am. Assoc. Cancer Res. 2005, 46, 1691;


    

Ordering informations


Catalog No.

Product Name

Size

CD0287

TG100-115 - PI3Kγ/δ Inhibitor

1mg, 5mg, 10mg, 25mg, 50mg,

100mg, 200mg, 500mg & 1g

CD0180

TGX-221 – PI3Kb Inhibitor VI

1mg, 5mg, 10mg, 25mg, 50mg,

100mg & 1g

CD0277

Wortmannin (KY 12420)

1mg, 5mg, 25mg

& 50mg

CD0237

ZSTK474 – PI3K a/b/g/d Inhibitor

10mg, 25mg, 50mg, 100mg,

250mg & 1g

 


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