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작성일 : 14-06-14
[Chemdea] Wortmannin Analogs


Wortmannin Analogs

 

 

Product Name: 17-b-Hydroxywortmannin (HWT)

 

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A cell-permeable Wortmannin 17β-Hydroxy analog (HWT) that acts as an irreversible PI 3-Kinhibitor with an 8.4-

fold higher potency than that of Wortmannin (IC50= 0.5 and 4.2 nM, respectively) and inhibits mTOR only at much

higher concentrations (IC50 = 0.193 µM). Both Wortmannin and HWTcovalently modify a conserved lysine residue

(Lys833 in porcine PI 3-Kγ) in the PI 3-K ATP binding pocket via their electrophilic furan ring at C-20position. HWT

is shown to effectively arrest the growth of LNCaP cells (IC50 = 1.464 µM) in vitro, however, its high in vivotoxicity

renders it unsuitable for tumor killing studies in mice. Also reported to inhibit latephase PLD-mediated PA

production upon fMLP stimulation of human neutrophils. See also our product PX-866-17OH (Cat # CD0323) and

PX-13-17OH (Cat # CD0305) with similar activity.

 

Details

Chemical Formula:

 

C23H26O8

CAS No.:

 

58053-83-1

Molecular weight:

 

430.5

Purity:

99% by HPLC

Appearance:

 

Off white solid

Chemical name:

 

17-b-Hydroxywortmannin (LY 301497)

Solubility:

 

DMSO (100 mg/mL).

Storage:

Protect from light. Packaged under inert gas

 

References

 

Product Name: PX-13-17OH – PI3K Inhibitor

 

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PX-13-17OH is an irreversible, isoform non-specific Wortmannin analog which potently inhibits PI3Ka/b/g/d (IC50=

6.4 nM, 13 nM, 8 nM and 11 nM respectively). PX-13-17OH does not appreciably inhibit mTOR (IC50 = 2.92 mM). In

a kinase panel PX-13-17OH did not show significan inhibition of other kinases (IC50 > 10 mM). In a cellular assay

PX-13-17OH inhibited the LNCap cell line (IC50 = 0.39 mM). In a nude mouse xenograft model (U87MG glioma)PX-

13-17OH showed potent inhibition of tumor growth aldeardyat 1.25 mg/Kg in iv dosing. See also our product PX-

866-17OH (Cat# CD0323) and 17-b-Hydroxywortmannin (Cat# CD0278) with similar activity.

 

Details

Chemical Formula:

 

C29H42N2O8

CAS No.:

 

884539-95-1

Molecular weight:

 

546.65

Purity:

98% by HPLC

Appearance:

 

Yellow solid

Chemical name:

 

(1E,4S,4aR,5R,6aS,7S,9aR)-5-(Acetyloxy)-1-[[[3-(dimethylamino)propyl]methylamino]methylene]-4a,5,6,6a,7,8,9,9a-octahydro-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethylcyclopenta[5,6]na-phtho[1,2-c]pyran-2,10(1H,4H)-dione

Solubility:

 

DMSO (80 mg/mL), water (10 mg/mL)

Storage:

Protect from light. Packaged under inert gas

 

Reference

 

 

Product Name: PX-866-17OH – PI3K Inhibitor

 

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PX-866-17OH is an irreversible, isoform non-specific Wortmannin analog which potently inhibits PI3Ka/b/g/d.PX-

866-17OH is an 17-OH active metabolite of compound PX-866 (Cat# CD0279), that is a more potent PI-3Kinhibitor

than the parent compound and retains the same irreversiblemechanism of action. See also our product PX-13-

17OH (Cat# CD0305) and 17-b-Hydroxywortmannin (Cat# CD0278) with similar activity.

 

Details

Chemical Formula:

 

C29H37NO8

CAS No.:

 

1012327-63-7

Molecular weight:

 

527.61

Purity:

> 99% by HPLC

Appearance:

 

Yellow solid

Chemical name:

 

(1E,4S,4aR,5R,6aS,7S,9aR)-5-(Acetyloxy)-1-[(di-2-propen-1-ylamino)methylene]-4a,5,6,6a,7,8,9,9a-octahydro-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethylcyclopenta[5,6]naphtho[1,2-c]pyran-2,10(1H,4H)-dione

Solubility:

 

DMSO (50 mg/mL)

Storage:

Protect from light. Packaged under inert gas

 

References

 

Product Name: Wortmannin (KY 12420)

 

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A cell-permeable, fungal metabolite that acts as a potent, selective, and irreversibleinhibitor 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 ofinsulin in

isolated rat adipocytes without affecting the insulin receptortyrosine kinase activity. Inhibits MAP kinase activation

induced by platelet activating factor in guinea pig neutrophils (200 - 300 nM). Also inhibitsother 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

 

 

Ordering informations

 

Catalog No.

Product Name

Size

CD0278

17-b-Hydroxywortmannin (HWT)

1mg, 5mg, 10mg

& 25mg

CD0305

PX-13-17OH – PI3K Inhibitor

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

50mg & 100mg

CD0323

PX-866-17OH – PI3K Inhibitor

1mg, 5mg, 10mg, 25mg

& 50mg

CD0277

Wortmannin (KY 12420)

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

50mg, 100mg & 300mg

 

 

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