Wortmannin

For research use only.

Catalog No.S2758 Synonyms: KY 12420, SL-2052

225 publications

Wortmannin Chemical Structure

CAS No. 19545-26-7

Wortmannin (KY 12420, SL-2052) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.

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Selleck's Wortmannin has been cited by 225 publications

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Biological Activity

Description Wortmannin (KY 12420, SL-2052) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Targets
PI3K [3]
(Cell-free assay)
DNA-PK [12]
(Cell-free assay)
ATM [12]
(Cell-free assay)
MLCK [1]
(Cell-free assay)
3 nM 16 nM 150 nM 170 nM
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A459 NFvJVmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH22NVgzNjVizszN NV:5O5B4OS12IHS= MXPEUXNQ M3m3bYVvcGGwY3XzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25idILlZZRu\W62IIfpeIghfGGvb4jp[oVv M3PSNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEmwN|g{Lz5{NUS5NFM5OzxxYU6=
H1703 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v4SFIvPSEQvF2= NGnzOlQyNTRiZB?= NXLITHhmTE2VTx?= NEjrVmNmdmijbnPld{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIITy[YF1dWWwdDD3bZRpKHSjbX;4bYZmdg>? Mle2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2OUCzPFMoRjJ3NEmwN|g{RC:jPh?=
HUVECs M2HpOWN6fG:2b4jpZ4l1gSCDc4PhfS=> MmTaNVAxKG6P M176R|I1KGh? MVvheJRmdnWjdHXzJJRp\SCjYoLv[4F1cX[nIHXm[oVkfHNib3[gZ4FtgWOxc3nuJI9vKF[UST3pcoR2[2WmIHP5eI91d3irY3n0fS=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3MEG4Okc,OjV2NUCxPFY9N2F-
APRE-19 NXnYZlZXSXCxcITvd4l{KEG|c3H5 MkTLOUDPxE1? Mo\kNlQhcA>? MXzhZo9tcXOqZYOgSmxbNW2nZHnheIVlKHC{bz3zeZJ3cX[jbD;hcpRqNWGyb4D0c5NqeyCjY4Tpeol1gQ>? NXHDXYFYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNlk3OTdpPkK1N|I6PjF5PD;hQi=>
MDA-MB-231 MmjzRZBweHSxc3nzJGF{e2G7 NWHoZWlpOcLizszNxsA> NUDoZYNmPDhiaB?= NWjtUWVVTE2VTx?= NFHwVHBl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhfHKnYYTl[EB4cXSqIEK1JO69VSCxZjDGNUBweiCIMjFCpC=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMEmzNkc,OjV|MEC5N|I9N2F-
MCF7 Mmq5SpVv[3Srb36gRZN{[Xl? M3TyNlExOCCwTR?= NYnt[nN{OjRiaB?= MkDo[YxqdWmwYYTld{BGOi2rbnT1Z4VlKEGURT3MeYMh[WO2aY\peJk> MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF5MkW1O{c,OjVzN{K1OVc9N2F-
HT-29  M4nWWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLLNU42yqEEtV2= MVW5OkBp NF3zVXBl\WO{ZXHz[ZMh[2WubDDndo94fGhid3jpZ4gh[2GwIHLlJIlvcGmkaYTl[EBjgSCNWV7B MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzMkGyN{c,OjVyMUKxNlM9N2F-
MO59K  NIe5b4dEgXSxdH;4bYNqfHliQYPzZZk> MXW1xsDPxE1? M1TCb|ch\A>? NWjZNJNRTE2VTx?= M2\0TYVvcGGwY3XzJJRp\SCleYTveI95cWOrdImgc4Yh\XSxcH;zbYRmKG:{IHPpd5Bt[XSrbh?= NH;BVm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1N|U3OSd-MkS5OVM2PjF:L3G+
MO59J NGnHV3ZEgXSxdH;4bYNqfHliQYPzZZk> NXfvN2ZpPcLizszN NHLUTlY4KGR? M3HLSmROW09? MX3lcohidmOnczD0bIUh[3m2b4TvfIlkcXS7IH;mJIV1d3Cxc3nk[UBweiClaYPwcIF1cW5? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3M{W2NUc,OjR7NUO1OlE9N2F-
MO59K  M1nkb2Fxd3C2b4Ppd{BCe3OjeR?= NUPUOGxEOTBizszN MWGyOEBp Mlz6SG1UVw>? NWP0fmxJcW6lcnXhd4V{KHSqZTDEV2IhdGW4ZXygbY5lfWOnZDDifUBmfG:yb4Pp[IUhd3JiY3nzdIxifGmw NWjEelFiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVM2PjFpPkK0PVU{PTZzPD;hQi=>
MO59J NYTqT|dPSXCxcITvd4l{KEG|c3H5 MlKzNVAh|ryP MUCyOEBp MWjEUXNQ NIHLV|VqdmO{ZXHz[ZMhfGinIFTTRkBt\X[nbDDpcoR2[2WmIHL5JIV1d3Cxc3nk[UBweiClaYPwcIF1cW5? NWeyc3d2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVM2PjFpPkK0PVU{PTZzPD;hQi=>
HepG2 M3i5NmZ2dmO2aX;uJGF{e2G7 MVixNFAhdk1? MonNNE42KGh? Mo\TSG1UVw>? MmfJZoxw[2u|IF3BMYlv\HWlZXSgRYt1KHCqb4PwbI9zgWyjdHnvci=> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh4M{O1NEc,OjR6NkOzOVA9N2F-
A549  M1e1S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[zJOK2VcLi M2rCTVIhcA>? M3f4RpN2eHC{ZYPz[ZMheGWvZYTy[Zhm\C2rbnT1Z4VlKEGtdDDhcoQhT1ONM98yJIFkfGm4YYTpc44tKFNvcHjhd4Uh[XK{ZYP0MEBk\WyuIHHwc5B1d3OrczDhcoQh[2G|cHHz[U0{KGGldHn2ZZRqd25? NHvseW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi0O|g3Oyd-MkS4OFc5PjN:L3G+
A549  MUHGeY5kfGmxbjDBd5NigQ>? NHzBUnAyOMLizsztxsA> NGKyUmUyPiCq NH7hR3BFVVOR NFTCS5pud2S3bHH0[ZMhfGinIFnBWkBz\XCuaXPheIlwdiCjbnSgZ4F2e2W|IILleIVvfGmxbjDv[kBPWCCrbjD0bIUhdnWlbHX1d{4> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhyMkGxNUc,OjR6MEKxNVE9N2F-
SK-N-LO NYDqRXlCTnWwY4Tpc44hSXO|YYm= M1\TWFExOCCwTR?= M3i3[FAvPSCq M4DQO4Rm[3KnYYPld{B1cGVic4TpcZVt[W62IHXm[oVkfHNib3[gcY9zeGirbnWgc44hSWu2IIDoc5NxcG:{eXzheIlwdg>? NUDmN5I2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVQ3ODZpPkK0OlU1PjB4PD;hQi=>
HL-60 NWTCT3VuTnWwY4Tpc44hSXO|YYm= NGTzPGoxNjIEoN88US=> M3PuXlczKGh? M2juO4Jtd2OtczDkZZNifGmwaXKtbY5lfWOnZDDj[YxtKGSrZn\ldoVvfGmjdHnvci=> NI\wTY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[wO|I4Oyd-MkS2NFczPzN:L3G+
HepG2  NFPwOYNHfW6ldHnvckBCe3OjeR?= NXPiW|BlOjByIH7N M{\ZcFAvPSCq MlTBZZR1\W63YYTld{BHd3iRIIDoc5NxcG:{eXzheIlwdg>? NVzkc406RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1N|UyQTJpPkK0OVM2OTl{PD;hQi=>
H520 MXHGeY5kfGmxbjDBd5NigQ>? MYGxNOKh|ryP M{CyOFEhcA>? NYHRcXhETE2VTx?= NFHO[Wpl\WO{ZXHz[ZMh[2WubIXsZZIheGixc4Doc{1CU1RicILveIVqdiCuZY\lcJM> NVTuN204RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OFc6OzVpPkK0OFQ4QTN3PD;hQi=>
H1975 NEn2RWVHfW6ldHnvckBCe3OjeR?= MlrHNVDDqM7:TR?= M{TNdFEhcA>? MkOwSG1UVw>? MnjP[IVkemWjc3XzJINmdGy3bHHyJJBpd3OyaH:tRWtVKHC{b4TlbY4hdGW4ZXzz MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR2N{mzOUc,OjR2NEe5N|U9N2F-
MG-63 MV7BdI9xfG:|aYOgRZN{[Xl? NVzUT3A3OTBiwsXN MWexNkBp MYjlcohidmOnczDEVE1qdmS3Y3XkJIFxd3C2b4Ppdy=> M1LCeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W4N|AyLz5{NEO1PFMxOTxxYU6=
5637 M{LEWmFxd3C2b4Ppd{BCe3OjeR?= MYOxNOKh|ryP MV60NEBucW5? MlzYdoV3\XK|ZYOgdFIyX0GIMTDlfJBz\XO|aX;uMEBETEtiZYjwdoV{e2mxbjygZY5lKGOnbHygbY5pcWKrdHnvckBqdmS3Y3XkJIJ6KG[3Y3;p[IFv NYHOc2pnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|M5PjhpPkK0N|M{QDZ6PD;hQi=>
HEK-293 MVzGeY5kfGmxbjDBd5NigQ>? MV6xOVBvVQ>? MlXDNVYhcA>? Mn3ISG1UVw>? M4TyVoRm[3KnYYPld{BEWlRiYXP0bZZqfHl? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN{NEO2Okc,OjR|MkSzOlY9N2F-
SW480  NGX1bJBHfW6ldHnvckBCe3OjeR?= NH7RRZUyPTCwTR?= NHXVWVQzOCCq M1LWZmROW09? MlL0doVlfWOnczDj[YxtfWyjcjDhZ4N2dXWuYYTpc44hd2ZizsKtZ4F1\W6rbh?= NVu1[4pkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzNlQ{PjZpPkK0N|I1OzZ4PD;hQi=>
HepG2 MlLjSpVv[3Srb36gRZN{[Xl? NH[4TGwyODBibl2= MWKyOEBp NVnFWoh2[XS2ZX71ZZRmeyC2aHWgZ49td26rZYOgc4YhfGinIIT1cY9zKGOnbHzzJJdqfGhidYDy[Yd2dGG2aX;uJI9nKEGtdEG= NWHl[VJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPVc2OTBpPkK0Nlk4PTFyPD;hQi=>
HCT 116  NIXPbIxHfW6ldHnvckBCe3OjeR?= NV;xfnhVOTByIH7N NXSyRZBSOjRiaB?= M1X4NIF1fGWwdXH0[ZMhfGinIHPvcI9vcWW|IH;mJJRp\SC2dX3vdkBk\WyuczD3bZRpKHWycnXneYxifGmxbjDv[kBCc3Rz NUGwfYtIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPVc2OTBpPkK0Nlk4PTFyPD;hQi=>
BEL/FU NVvDPINoTnWwY4Tpc44hSXO|YYm= MmXENUBuVQ>? NH7CUHUzPCCq MYfk[YNz\WG|ZYOgdJJwfGWrbjDs[ZZmdHNib3[geIhmKFCLM1uvRYt1KHCjdHj3ZZk> NW\iO4RiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyN|IxQTlpPkK0NlMzODl7PD;hQi=>
Huh7  MlPBSpVv[3Srb36gRZN{[Xl? NEnMfGc{yqEQvF2= NYHzUIJKOSCq MnXxdoVlfWOnczD0bIUhfmm{dYOg[Y51enliaX70c{B1cGViY3XscJM> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF6NEG5Okc,OjRzOESxPVY9N2F-
A-375 MWXBdI9xfG:|aYOgRZN{[Xl? MmnxOE85KM7:TR?= MWCyOEBp NVfrU4V3\W6qYX7j[ZMhXFKDSVytbY5lfWOnZDDhdI9xfG:|aYRCpC=> NETt[pM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGxN|E4Oyd-MkSxNVMyPzN:L3G+
A-375-TS  MUXBdI9xfG:|aYOgRZN{[Xl? MkHROE85KM7:TR?= NWfSelhDOjRiaB?= NXfI[mZk\W6qYX7j[ZMhXFKDSVytbY5lfWOnZDDhdI9xfG:|aYRCpC=> M2fmNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUGzNVc{Lz5{NEGxN|E4OzxxYU6=
Mel-HO NHL2Zo5CeG:ydH;zbZMhSXO|YYm= NFfsUWc1NzhizszN NYD0b4Z6OjRiaB?= MVLlcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqe8Li NYDYZ5BIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNVMyPzNpPkK0NVE{OTd|PD;hQi=>
Mel-HO-TS NVfmbIo6SXCxcITvd4l{KEG|c3H5 MX60M|gh|ryP M3THZlI1KGh? NVn0SVNQ\W6qYX7j[ZMhXFKDSVytbY5lfWOnZDDhdI9xfG:|aYRCpC=> MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFzM{G3N{c,OjRzMUOxO|M9N2F-
MeWo MWjBdI9xfG:|aYOgRZN{[Xl? M3rTOVQwQCEQvF2= NUPSPZZrOjRiaB?= MkjB[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXQEoB?= M2XydlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUGzNVc{Lz5{NEGxN|E4OzxxYU6=
Mel-2a Mln2RZBweHSxc3nzJGF{e2G7 NG\FN3g1NzhizszN NVfS[2tROjRiaB?= MWTlcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqe8Li MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFzM{G3N{c,OjRzMUOxO|M9N2F-
MDA-MB-231 M3HaPWZ2dmO2aX;uJGF{e2G7 Mn;LNQKBmzRyMDDuUS=> NHvnVmg1KGh? NVvuSolUe3WycILld5NmeyCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M2nIWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUC2NlU6Lz5{MkmwOlI2QTxxYU6=
MDA-MB-231 NF[wfZdHfW6ldHnvckBCe3OjeR?= M{PFd|QxOCCwTR?= NIfrXYs1KGh? Ml62[IVkemWjc3XzJG1OWC17IHHu[EBKVC16IIDyc5RmcW5iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NEnHRpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmwOlI2QSd-MkK5NFYzPTl:L3G+
Jurkat M2TpeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKwMlI2NTFwMkWg{txO MXWyOE81QCCq NFfQRYFFVVOR NIfHNIdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYn;0bEB1cW2nLTDhcoQh\G:|ZT2g[IVx\W6mZX70JI1idm6nch?= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd3N{G4OUc,OTl5NUexPFU9N2F-
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A549 MkmySpVv[3Srb36gZZN{[Xl? NGfVdJJKdmirYnn0bY9vKG:oIGDsb|MhcW5iaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDjZZNmcW5ic4Xid5Rz[XSnIIDoc5NxcG:{eXzheIlwdiCkeTDX[ZN1\XKwIHLsc5QtKEmFNUCgQUAxNjJ{IN88UU4> M33ZeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MUO1NlQ5Lz5zN{GzOVI1QDxxYU6=
A549 MXfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NGTYclM1QCCqcoO= NUPiSWR5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIhdWW2aH;kMEBKSzVyIE2gNVEvPCEQvF2u NYHFNIF6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi2N|A5QTRpPkG4OlMxQDl2PD;hQi=>
GM00637 NV3O[FRDTnWwY4Tpc44h[XO|YYm= M{Xse|EhfU1? M3;U[2lvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgVIxsOyCneIDy[ZN{\WRiaX6gbJVu[W5iR12wNFY{PyClZXzsd{BifCBzIIXNJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIIC1N{B{\XKrbnWtNlAheGixc4Doc5J6dGG2aX;u MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzF|NUK0PEc,OTdzM{WyOFg9N2F-
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HeLa MW\GeY5kfGmxbjDhd5NigQ>? NFLYWmwyODBibl2= M134S|ExKG2rboO= Ml7KTY5pcWKrdHnvckBw\iCSSUPLJIlvKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGVITi2|dHnteYxifGWmIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhXDNyODDheEAyODBibl2gdJJmcW6ldXLheIVlKG[xcjCxNEBucW6|IH\vcIxwf2WmIHL5JGVITiC|dHnteYxifGmxbjDt[YF{fXKnZDDh[pRmeiB3IH3pcpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz M1LIT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{iwPFY2Lz5|MEO4NFg3PTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-GSK3β / GSK3β / Bcl-xl / Bax / Caspase-3 / Cleaved caspase-3; 

PubMed: 25344912     


Four esophageal cancer cell lines were treated with different concentrations of wortmannin for 48 h, and cell lysates were collected for Western blot analysis of p-AKT, AKT, p-GSK3β, GSK3β, Bcl-xL, Bax, caspase-3, and cleaved caspase-3.

25344912
Immunofluorescence
DNMT1; 

PubMed: 24001151     


PC3 cells were treated with DMSO or wortmannin (1 μM) for 24 hours. DNMT1 and DNMT3B cellular localization was visualized by immunofluorescent staining. After 24h of treatment, cells were fixed in methanol, incubated with the indicated antibodies, stained with Alexa Fluor 594-tagged secondary antibodies and counterstained with DAPI. Slides were then mounted and examined under a fluorescence microscope. The bright field images of PC3 cells treated with DMSO or wortmannin (1 μM) for 24 hours are shown (right panel).

24001151
Growth inhibition assay
Cell viability; 

PubMed: 25344912     


MTT assay was used to determine the effects of different concentrations of wortmannin on viability of esophageal cancer cells lines KYSE150, HKESC-1, KYSE270, and T.Tn. Bars, SD; * P < 0.05; **, P < 0.01; ***, P < 0.001 compared with DMSO-treated cells.

25344912
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]

Protocol

Animal Research:[11]
- Collapse
  • Animal Models: Human pancreatic adenocarcinoma cells PK1 are injected both s.c. and orthotopically into SCID mice.
  • Dosages: 0.175, 0.35, and 0.7 mg/kg
  • Administration: Injected by i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 85 mg/mL (198.39 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* 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 Information

Molecular Weight 428.43
Formula

C23H24O8

CAS No. 19545-26-7
Storage powder
in solvent
Synonyms KY 12420, SL-2052
Smiles CC(=O)OC1CC2(C(CCC2=O)C3=C1C4(C(OC(=O)C5=COC(=C54)C3=O)COC)C)C

In vivo Formulation Calculator (Clear solution)

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID