Wortmannin

Catalog No.S2758

Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.

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Wortmannin Chemical Structure

Wortmannin Chemical Structure
Molecular Weight: 428.43

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Related Compound Libraries

Wortmannin is available in the following compound libraries:

PI3K Inhibitors with Unique Features

Product Information

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  • Research Area
  • Inhibition Profile

Product Description

Biological Activity

Description Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.
Targets PI3K [3]
(Cell-free assay)
DNA-PK [12]
(Cell-free assay)
ATM [12]
(Cell-free assay)
MLCK [1]
(Cell-free assay)
ATR [12]
(Cell-free assay)
IC50 3 nM 16 nM 150 nM 170 nM 1.8 μM
In vitro The inhibition of MLCK by Wortmannin is not affected by calmodulin or peptide substrat, while reduced by high concentration of ATP. Wortmannin directly interacts with the catalytic domain of MLCK and leads to an irreversible loss of the enzyme activity. Wortmannin has no inhibitory to cAMP-dependent protein kinase, cGMP-dependent protein kinase, and calmodulin-dependent protein kinase II, and has little effect on protein kinase C activity. [1] Wortmannin inhibits N-formylmethionyl-leucylphenylalanine (fMLP)-stimulated PtdInsP3 (phosphatidylinositol 3,4,5-trisphosphate) formation with IC50 of 5 nM and this inhibition is completely abolished when pretreated with 100 nM Wortmannin in human neutrophils, with increased PtdInsP2 levels and no effects on cellular PtdInsP and PtdIns contents. Wortmannin could develop oscillatory changes in F-actin content and does not inhibit fMLP-stimulated actin polymerization in neutrophils. [2] Wortmannin irreversibly inhibits phosphatidylinositol 3-kinase (PI3-kinase) activity with binding to the 110-kDa protein (IC50 of 3 nM) and has no effect PI4-kinase in RBL-2H3 cells. Wortmannin also inhibits both Fc epsilon RI-mediated histamine secretion and leukotriene release, with no effect on the activation of the tyrosine kinase Lyn. [3] Wortmannin completely abolishes the insulin-induced hexose uptake in isolated rat adipocytes at 0.1 μM, without impairing isoproterenol-stimulated lipolytic activity. [4] Wortmannin suppresses insulin-induced production of nitric oxide by 50% at 500 nM in human umbilical vein endothelial cells, which is in response to IGF-1. [5] Wortmannin suppresses DNA double strand break (DSB) repair and has no effect on DSB levels or the kinetics of single strand break (SSB) repair in Chinese hamster ovary cells at 50 μM. Wortmannin could potentiate ionizing radiation (IR)-induced cytotoxicity with no toxicity by itself. [6] Wortmannin inhibits polo-like kinase (PLK1) activity IC50 of 24 nM in intact G2/M-arrested cells. [7] Wortmannin increases Toll-like receptor (TLR)-mediated accumulation of IL-6 in human macrophages with EC50 of 50 nM. Meanwhile Wortmannin significantly enhances TLR-mediated inducible nitric-oxide synthase (iNOS) expression and nitrite accumulation in mouse macrphages. Wortmannin activates the nuclear factor-κB and up-regulates the cytokine mRNA production. [8] Wortmannin also inhibits Polo-like kinase (PlK) 1 and PlK3, which play important roles in mitosis. Wortmannin treatment could lead to a reduction in phosphorylation of p53 on serine 20 induced by DNA damage. [9] Wortmannin suppresses hyaluronan-induced Akt phosphorylation and cell motility/migration in SW1990 cells. [10]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
A459MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1e4dFIvPSEQvF2=MWKxMVQh\A>?NX\pSm5UTE2VTx?=MmHl[Y5p[W6lZYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiC2cnXheI1mdnRid3n0bEB1[W2xeHnm[Y4>NYXBdGtDOjV2OUCzPFM>
H1703M4n4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2Xv[|IvPSEQvF2=MWWxMVQh\A>?NWfET5B2TE2VTx?=NUO1boE3\W6qYX7j[ZMh[2WubDDndo94fGhiaX7obYJqfGmxbjD0doVifG2nboSge4l1cCC2YX3vfIln\W5?M3vXR|I2PDlyM{iz
HUVECsMkfGR5l1d3SxeHnjbZR6KEG|c3H5M4fXflExOCCwTR?=MlPNNlQhcA>?MUXheJRmdnWjdHXzJJRp\SCjYoLv[4F1cX[nIHXm[oVkfHNib3[gZ4FtgWOxc3nuJI9vKF[UST3pcoR2[2WmIHP5eI91d3irY3n0fS=>NG\uOmkzPTR3MEG4Oi=>
APRE-19NVqyPWx4SXCxcITvd4l{KEG|c3H5MlfROUDPxE1?MV2yOEBpNYrTeGpt[WKxbHnzbIV{KE[OWj3t[YRq[XSnZDDwdo8ue3W{dnn2ZYww[W62aT3hdI9xfG:|aYOgZYN1cX[rdIm=NH\kO4QzPTN{OU[xOy=>
MDA-MB-231NILyNWRCeG:ydH;zbZMhSXO|YYm=MY[xxsDPxE4EoB?=NWfmcINKPDhiaB?=M2PneWROW09?M4O1TYRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEB1emWjdHXkJJdqfGhiMkWg{txOKG:oIF[xJI9zKEZ{INMgMmTrNlU{ODB7M{K=
MCF7MVTGeY5kfGmxbjDBd5NigQ>?MkS3NVAxKG6PM{XMS|I1KGh?NHfuV5BmdGmvaX7heIV{KEV{LXnu[JVk\WRiQWLFMWx2[yCjY4Tpeol1gQ>?M2nMe|I2OTd{NUW3
HT-29 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NEjuWZgyNjYEoNM1US=>M1HmVFk3KGh?NWL1TmJD\GWlcnXhd4V{KGOnbHyg[5Jwf3SqIIfobYNpKGOjbjDi[UBqdmirYnn0[YQh[nliS2nORS=>MX6yOVAyOjF{Mx?=
MO59K MXzDfZRwfG:6aXPpeJkhSXO|YYm=NEnZVI82yqEQvF2=MlnVO{BlM{TUZmROW09?NXroS4J1\W6qYX7j[ZMhfGinIHP5eI91d3irY3n0fUBw\iCndH;wc5Nq\GVib4KgZ4l{eGyjdHnuMW[yOFk2OzV4MR?=
MO59JMUHDfZRwfG:6aXPpeJkhSXO|YYm=NVXOUFJwPcLizszNNEfxTGc4KGR?MUDEUXNQNE\pfZNmdmijbnPld{B1cGViY4n0c5RwgGmlaYT5JI9nKGW2b4Dvd4ll\SCxcjDjbZNxdGG2aX6=Mk\INlQ6PTN3NkG=
MO59K NHv0S|NCeG:ydH;zbZMhSXO|YYm=MXuxNEDPxE1?M3;aWVI1KGh?M{TMZ2ROW09?NHvCXXJqdmO{ZXHz[ZMhfGinIFTTRkBt\X[nbDDpcoR2[2WmIHL5JIV1d3Cxc3nk[UBweiClaYPwcIF1cW5?MlrNNlQ6PTN3NkG=
MO59JNETnUYxCeG:ydH;zbZMhSXO|YYm=M1rGVlExKM7:TR?=NF3GbpQzPCCqMVPEUXNQNHPxW41qdmO{ZXHz[ZMhfGinIFTTRkBt\X[nbDDpcoR2[2WmIHL5JIV1d3Cxc3nk[UBweiClaYPwcIF1cW5?M2nIPFI1QTV|NU[x
HepG2M2j2XWZ2dmO2aX;uJGF{e2G7MUixNFAhdk1?M1q4SlAvPSCqM12wdmROW09?NV24XWUx[myxY3vzJG1CNWmwZIXj[YQhSWu2IIDoc5NxcG:{eXzheIlwdg>?M3zHWlI1QDZ|M{Ww
A549 MlXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M4mzOFMhyrWPwrC=NVq3S456OiCqM4jUZ5N2eHC{ZYPz[ZMheGWvZYTy[Zhm\C2rbnT1Z4VlKEGtdDDhcoQhT1ONM98yJIFkfGm4YYTpc44tKFNvcHjhd4Uh[XK{ZYP0MEBk\WyuIHHwc5B1d3OrczDhcoQh[2G|cHHz[U0{KGGldHn2ZZRqd25?MXmyOFg1Pzh4Mx?=
A549 NEPUWYlHfW6ldHnvckBCe3OjeR?=M3TseFExyqEQvH5CpC=>Mnq2NVYhcA>?MWjEUXNQNGTkcIJud2S3bHH0[ZMhfGinIFnBWkBz\XCuaXPheIlwdiCjbnSgZ4F2e2W|IILleIVvfGmxbjDv[kBPWCCrbjD0bIUhdnWlbHX1d{4>MUeyOFgxOjFzMR?=
SK-N-LONFzSZZFHfW6ldHnvckBCe3OjeR?=NWfB[lBXOTByIH7NM3\GdVAvPSCqNGfabIJl\WO{ZXHz[ZMhfGinIIP0bY12dGGwdDDl[oZm[3S|IH;mJI1wenCqaX7lJI9vKEGtdDDwbI9{eGixconsZZRqd25?MoXqNlQ3PTR4ME[=
HL-60M3Hyb2Z2dmO2aX;uJGF{e2G7MnzJNE4yyqEQvF2=M1fUe|czKGh?NIPkRXljdG:la4Og[IF{[XSrbnniMYlv\HWlZXSgZ4VtdCCmaX\m[ZJmdnSrYYTpc44>MmO2NlQ3ODd{N{O=
HepG2 Mk\iSpVv[3Srb36gRZN{[Xl?NFixOmkzODBibl2=NYTmOow5OC53IHi=NWfCcoc6[XS2ZX71ZZRmeyCIb4jPJJBpd3OyaH;yfYxifGmxbh?=NYrQb|MzOjR3M{WxPVI>
H520MkDLSpVv[3Srb36gRZN{[Xl?MV2xNOKh|ryPMl3rNUBpNWqyV4VmTE2VTx?=MVHk[YNz\WG|ZYOgZ4VtdHWuYYKgdIhwe3Cqbz3BT3QheHKxdHXpckBt\X[nbIO=MkD3NlQ1PDd7M{W=
H1975MlPqSpVv[3Srb36gRZN{[Xl?MUOxNOKh|ryPMXqxJIg>Mn3sSG1UVw>?NEfuflJl\WO{ZXHz[ZMh[2WubIXsZZIheGixc4Doc{1CU1RicILveIVqdiCuZY\lcJM>MYOyOFQ1Pzl|NR?=
MG-63NYDBfWxCSXCxcITvd4l{KEG|c3H5NIriXGgyOCEEtV2=Mo\LNVIhcA>?MWTlcohidmOnczDEVE1qdmS3Y3XkJIFxd3C2b4Ppdy=>Ml7uNlQ{PTh|MEG=
5637MWXBdI9xfG:|aYOgRZN{[Xl?M2K2NFExyqEQvF2=M4roRlQxKG2rbh?=MX\y[ZZmenOnczDwNlFYSUZzIHX4dJJme3Orb36sJGNFUyCneIDy[ZN{cW:wLDDhcoQh[2WubDDpcohq[mm2aX;uJIlv\HWlZXSgZpkh\nWlb3nkZY4>NVnvO2RYOjR|M{O4Olg>
HEK-293NYrQfFRpTnWwY4Tpc44hSXO|YYm=NHvjWGQyPTCwTR?=NF7EdXIyPiCqMlW3SG1UVw>?NGjSRVNl\WO{ZXHz[ZMhS1KWIHHjeIl3cXS7MkC3NlQ{OjR|Nk[=
SW480 M3;rSWZ2dmO2aX;uJGF{e2G7MX2xOVBvVQ>?M4jj[lIxKGh?Ml;VSG1UVw>?NXzlWIFTemWmdXPld{Bk\WyudXzhdkBi[2O3bYXsZZRqd25ib3[g{tIu[2G2ZX7pci=>MnTQNlQ{OjR|Nk[=
HepG2MnK1SpVv[3Srb36gRZN{[Xl?NWjBXol1OTByIH7NM2XicFI1KGh?MoWyZZR1\W63YYTld{B1cGViY3;sc45q\XNib3[geIhmKHS3bX;yJINmdGy|IIfpeIghfXC{ZXf1cIF1cW:wIH;mJGFsfDF?MlnVNlQzQTd3MUC=
HCT 116 MXzGeY5kfGmxbjDBd5NigQ>?MnnLNVAxKG6PM{fRbVI1KGh?MYHheJRmdnWjdHXzJJRp\SClb3zvcolmeyCxZjD0bIUhfHWvb4KgZ4VtdHNid3n0bEB2eHKnZ4XsZZRqd25ib3[gRYt1OQ>?M3TCb|I1Ojl5NUGw
BEL/FUNEP2T29HfW6ldHnvckBCe3OjeR?=M3fSUVEhdU1?MmfKNlQhcA>?Mny4[IVkemWjc3XzJJBzd3SnaX6gcIV3\Wy|IH;mJJRp\SCSSUPLM2FsfCCyYYToe4F6MmnJNlQzOzJyOUm=
Huh7 M1TDc2Z2dmO2aX;uJGF{e2G7M3nSPVPDqM7:TR?=NH7lPVUyKGh?NW\sOZVDemWmdXPld{B1cGVidnnyeZMh\W62comgbY51dyC2aHWgZ4VtdHN?M1f1U|I1OTh2MUm2
A-375MYXBdI9xfG:|aYOgRZN{[Xl?NUfvcGZoPC96IN88US=>NF\mU|UzPCCqMkfJ[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXQEoB?=MX[yOFEyOzF5Mx?=
A-375-TS MYPBdI9xfG:|aYOgRZN{[Xl?M3LiR|QwQCEQvF2=MnPaNlQhcA>?MofM[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXQEoB?=NH\2XFAzPDFzM{G3Ny=>
Mel-HONYnjNos{SXCxcITvd4l{KEG|c3H5MljNOE85KM7:TR?=NX;XXFQ6OjRiaB?=NYLtRVB[\W6qYX7j[ZMhXFKDSVytbY5lfWOnZDDhdI9xfG:|aYRCpC=>MXeyOFEyOzF5Mx?=
Mel-HO-TSMXHBdI9xfG:|aYOgRZN{[Xl?NHn3bXM1NzhizszNNFLmO|YzPCCqM2rqe4VvcGGwY3XzJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m|wrC=M3uydFI1OTF|MUez
MeWoNV\r[29rSXCxcITvd4l{KEG|c3H5NFLMb|k1NzhizszNNXnQSHRPOjRiaB?=MVnlcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqe8LiMk\INlQyOTNzN{O=
Mel-2aM1e4[mFxd3C2b4Ppd{BCe3OjeR?=MXq0M|gh|ryPMmPyNlQhcA>?Mn31[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXQEoB?=MX[yOFEyOzF5Mx?=
MDA-MB-231NEHufZpHfW6ldHnvckBCe3OjeR?=MWKw5qCUPDByIH7NMXy0JIg>M37KdJN2eHC{ZYPz[ZMhSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?NWnrU3JKOjJ7ME[yOVk>
MDA-MB-231M2LPZmZ2dmO2aX;uJGF{e2G7NYPCRZNtPDByIH7NNX;sWHY1PCCqNYPrXYpj\GWlcnXhd4V{KE2PUD25JIFv\CCLTD24JJBzd3SnaX6gbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=MX:yNlkxPjJ3OR?=
JurkatMVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXfRNGszOC5{NT2xMlI2KM7:TR?=NGfU[VczPC92ODDoMo\KSG1UVw>?MY\pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[m:2aDD0bY1mNSCjbnSg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>?NHz5d4IyQTd3N{G4OS=>
NamalwaM3fxO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{exclAvOjVvMT6yOUDPxE1?Ml\sNlQwPDhiaB?=MY\EUXNQMmm5bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGKxdHigeIlu\S1iYX7kJIRwe2VvIHTldIVv\GWwdDDtZY5v\XJ?NUjkfIFlOTl5NUexPFU>
JurkatNWfHWWdRSXCxcITvd4l{KEG|c3H5Mmq0NE4zPS1zLkK1JO69VQ>?NXHrc3hxOjRxNEigbC=>NVjNXZJCTE2VTx?=NUTGcXdocW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBjd3SqIITpcYUuKGGwZDDkc5NmNSCmZYDlcoRmdnRibXHucoVzMX[xPVc2PzF6NR?=
NamalwaM1O4WWFxd3C2b4Ppd{BCe3OjeR?=Mn3WNE4zPS1zLkK1JO69VQ>?M1P3cFI1NzR6IHi=NXm0cIEyTE2VTx?=NXyxN5lPcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBjd3SqIITpcYUuKGGwZDDkc5NmNSCmZYDlcoRmdnRibXHucoVzM4TEVVE6PzV5MUi1
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SW1990MXzGeY5kfGmxbjDBd5NigQ>?MlXBNE4xOS1zIN88US=>MXSxJIg>NXe1XYF1cW6qaXLpeJMhUEFvaX7keYNm\CCDa4SgdIhwe3Cqb4L5cIF1cW:wMWSxPVQ3QTB{MB?=
RT112 NIXnSYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mnu3NVDDqM7:TR?=Ml2yNlQhcA>?MYHEUXNQMXPk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gS|IwVSClZXzsdy=>NGTZNpYyQDd6N{izNi=>
MHG-U1NIDoTWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M{j2c|ExyqEQvF2=MnXUNlQhcA>?MULEUXNQMUDk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gS|IwVSClZXzsdy=>NX\nZVVoOTh5OEe4N|I>
SMMC-7721NHfuPZBCeG:ydH;zbZMhSXO|YYm=NWDjVHc2OjBywrDuUS=>Mnv3NlQhcA>?MX\pcoNz\WG|ZYOgR2hZNWmwZIXj[YQh[XCxcITvd4l{MXmxO|U2PzF7MR?=
SMMC-7721M3focWZ2dmO2aX;uJGF{e2G7MlrVNlAxyqCwTR?=MlX1NlQhcA>?MorJeZAuemWpdXzheIV{KM7{MTy0S3QyKGW6cILld5Nqd25?M1nxc|E4PTV5MUmx
HeLaMmDrSpVv[3Srb36gRZN{[Xl?NXfYW3RuOTBywrDuUeKhMV2xJIg>MUjhcJRmenNidHjlJI1wenCqb3zv[5khd2ZidHjlJJRz[W6|ZnXydolvKHKnY4njcIlv\yClb33wZZJ1dWWwdB?=MXmxOlg6ODlzNR?=
MRC5VIMUjGeY5kfGmxbjDBd5NigQ>?M3LlVVEzNjVibV2=M4ryfFAvPSCqM2izN2ROW09?MYnhZo9tcXOqZYOgeIhmKFOnckS3N{9VcHJ|MElCpJBpd3OyaH;yfYxifGmxbjDv[kBCc3SSS1NCpC=>MlPXNVYzOjd|OUS=
AT5BIVAM3XtW2Z2dmO2aX;uJGF{e2G7NH:5OmoyOi53IH3NNVPKfpltOC53IHi=M4PkVWROW09?M1zTbIFjd2yrc3jld{B1cGViU3XyOFc{N1SqckOwPOKheGixc4Doc5J6dGG2aX;uJI9nKEGtdGDLRuKhMXexOlIzPzN7NB?=
M059JMkDaSpVv[3Srb36gRZN{[Xl?MXyxNk42KG2PMXiwMlUhcA>?NYnRPYZRTE2VTx?=MnnFZYJwdGm|aHXzJJRp\SCVZYK0O|MwXGi{M{C4xsBxcG:|cHjvdplt[XSrb36gc4YhSWu2UFvCxsA>NXHYbYhnOTZ{MkezPVQ>
HeLaMoG2SpVv[3Srb36gRZN{[Xl?M3rwVFEzNjVibV2=NGXVZWgxNjViaB?=MUfEUXNQMYrhZo9tcXOqZYOgeIhmKFOnckS3N{9VcHJ|MElCpJBpd3OyaH;yfYxifGmxbjDv[kBCc3SSS1NCpC=>MljENVYzOjd|OUS=
N2aMWXBdI9xfG:|aYOgRZN{[Xl?M4\FSFAvOS1zMDFOwG0>M{C4VlIhcA>?NHnQOGFqdmS3Y3XzJIRm[3KnYYPl[EBk\WyuII\pZYJqdGm2eTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6nch?=NWfBbodpOTV6NEK3Olc>
Jurkat MnrXT4lv[XOnIFHzd4F6MmezTWM2OCCxZjCyOEBvVQ>?MYixOVY3PDVzOR?=

... Click to View More Cell Line Experimental Data

In vivo Wortmannin inhibits peritoneal metastasis of SW1990 in mice at 1 mg/kg, without any weight loss. [10] Wortmannin inhibits phosphatidylinositide 3-kinase-protein kinase B (PKB)/Akt phosphorylation in both normal tissues (lung, heart and brain homogenates) and tumor tissue in mice, without mortality or acute toxicity at 0.7 mg/kg. Combination with LY188011, Wortmannin significantly increases apoptosis and inhibit tumor growth in orthotopic tumor, while both monotherapy could not. [11]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

MLCK assay MLCK activity is assayed with peptide substrate (KKRPQRATSNVFS-NH2) or myosin light chain. The peptide substrate (24 μM) is phosphorylated in a reaction mixture containing 25 mM Tris-HC1 (pH 7.5), 0.5 mg/mL bovine serum albumin, 4 mM MgCl2, 0.5 mM CaCl2, 2.6 nM calmodulin, 1.5 nM MLCK, and 400 μM ATP in a final volume of 0.25 mL. After a 10-min preincubation at 28 ºC without ATP, the reaction is started by addition of ATP at 28 ºC and terminated by the addition of 0.1 mL of 10% (v/v) acetic acid after 30 min. The mixture is analyzed by high performance liquid chromatography: column, Unisil Pack 5C18 4.6 X 150 mm; solvent, 18% (v/v) acetonitrile, 0.1% (v/v) trifluoroacetic acid in water; flow rate, 1.0 mL/min; temperature, 40 ºC; detection, absorbance at 220 nm. Percent of reaction is calculated from the ratio of peak areas of phosphorylated form to those of unphosphorylated form. Specific activity measured under the conditions described above is 0.81 μmol/min/mg. Myosin light chain (108 μg/mL) is phosphorylated in a reaction mixture containing 25 mM Tris-HC1 (pH 7.5), 0.5 mg/mL bovine serum albumin, 4 mM MgCl2, 0.5 mM CaCl2, 4.2 nM calmodulin, 0.92 nM enzyme, and 10 μM[γ-32P]ATP (100-900 cpm/pmol) in a final volume of 0.25 mL. After a 3-min preincubation at 30 ºC without ATP, the reaction is started by the addition of [γ-32P]ATP at 30 ºC and stopped by the addition of 0.125 mL of trichloroacetic acid after 5 min. The acid-precipitable materials are collected on a nitrocellulose membrane filter and washed with four 1-mL aliquots of 5% (v/v) trichloroacetic acid. The radioactivity on the filter is measured in a toluene scintillation fluid, using a Packard Tri-Carb liquid scintillation spectrometer Model 4530. The specific activity measured under the conditions is 1.23 μmol/min/mg. [1]
PI3K assay In an ordinary solution assay, partially purified PI3-kinase from calf thymus is used at a final concentration of 20 ng/mL. In the case of immunocomplex assay, P13-kinase activity is measured in immunoprecipitates with anti-PI3-kinase p85 antiserum, anti-

Animal Study: [11]

Animal Models Human pancreatic adenocarcinoma cells PK1 are injected both s.c. and orthotopically into SCID mice.
Formulation Dissolved at 0.4 mg/mL in DMSO, and diluted with 0.9% NaCl before use
Dosages 0.175, 0.35, and 0.7 mg/kg
Administration Injected by i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Nakanishi S, et al. J Biol Chem, 1992, 267(4), 2157-2163.

[2] Arcaro A, et al. Biochem J, 1993, 296(Pt 2), 297-301.

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Chemical Information

Download Wortmannin SDF
Molecular Weight (MW) 428.43
Formula

C23H24O8

CAS No. 19545-26-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms KY 12420
Solubility (25°C) * In vitro DMSO 85 mg/mL (198.39 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 8 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 3H-Furo[4,3,2-de]indeno[4,5-h]-2-benzopyran-3,6,9-trione, 11-(acetyloxy)-1,6b,7,8,9a,10,11,11b-octahydro-1-(methoxymethyl)-9a,11b-dimethyl-, (1S,6bR,9aS,11R,11bR)-

Tech Support

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