Wortmannin (KY 12420)

For research use only.

Catalog No.S2758 Synonyms: SL-2052, BRN 0067676, NSC 627609

234 publications

Wortmannin (KY 12420) Chemical Structure

CAS No. 19545-26-7

Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) 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 (KY 12420) has been cited by 234 publications

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Biological Activity

Description Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) 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 M3X2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfDWYQyOi53IN88US=> NYHHcmZXOS12IHS= NIPDXYZFVVOR MVHlcohidmOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKHS{ZXH0cYVvfCC5aYToJJRidW:6aX\lci=> NF3LdVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS5NFM5Oyd-MkW0PVA{QDN:L3G+
H1703 MlTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfDbVdCOi53IN88US=> NV;kbIxEOS12IHS= MkLhSG1UVw>? NHriVmFmdmijbnPld{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIITy[YF1dWWwdDD3bZRpKHSjbX;4bYZmdg>? NVTmfFBoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0PVA{QDNpPkK1OFkxOzh|PD;hQi=>
HUVECs NYXqfGZyS3m2b4TvfIlkcXS7IFHzd4F6 NVrHU|JEOTByIH7N NVzmdIM{OjRiaB?= MoXaZZR1\W63YYTld{B1cGViYXLyc4difGm4ZTDl[oZm[3S|IH;mJINidHmlb4PpckBwdiCYUlmtbY5lfWOnZDDjfZRwfG:6aXPpeJk> NWT0[VNqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0OVAyQDZpPkK1OFUxOTh4PD;hQi=>
APRE-19 NGjlU5NCeG:ydH;zbZMhSXO|YYm= NVznTIo1PSEQvF2= MXiyOEBp Mny2ZYJwdGm|aHXzJGZNYi2vZXTpZZRm\CCycn:td5Vzfmm4YXyvZY51cS2jcH;weI9{cXNiYXP0bZZqfHl? M2jXVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{K5OlE4Lz5{NUOyPVYyPzxxYU6=
MDA-MB-231 M1;3fGFxd3C2b4Ppd{BCe3OjeR?= NGr6SJkyyqEQvF5CpC=> MVS0PEBp MmjnSG1UVw>? NWPvWYUy\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKHS{ZXH0[YQhf2m2aDCyOUDPxE1ib3[gSlEhd3JiRkKgxsA> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMEmzNkc,OjV|MEC5N|I9N2F-
MCF7 NHu4S|dHfW6ldHnvckBCe3OjeR?= NVHUcYwzOTByIH7N MXGyOEBp MWPlcIlucW6jdHXzJGUzNWmwZIXj[YQhSVKHLVz1Z{Bi[3Srdnn0fS=> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF5MkW1O{c,OjVzN{K1OVc9N2F-
HT-29  NVTMeolpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjq[HlGOS53wrFCuW0> M3X2XVk3KGh? NYrLb3Fo\GWlcnXhd4V{KGOnbHyg[5Jwf3SqIIfobYNpKGOjbjDi[UBqdmirYnn0[YQh[nliS2nORS=> MoPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUKxNlMoRjJ3MEGyNVI{RC:jPh?=
MO59K  NWK3e5hYS3m2b4TvfIlkcXS7IFHzd4F6 M{DIRlXDqM7:TR?= NIPMWnI4KGR? MYrEUXNQ MoLm[Y5p[W6lZYOgeIhmKGO7dH;0c5hq[2m2eTDv[kBmfG:yb4Pp[IUhd3JiY3nzdIxifGmw Mly4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NUO1OlEoRjJ2OUWzOVYyRC:jPh?=
MO59J NWjUSW1vS3m2b4TvfIlkcXS7IFHzd4F6 NX6wXHRWPcLizszN NWqyWHVlPyCm MUHEUXNQ Mkfr[Y5p[W6lZYOgeIhmKGO7dH;0c5hq[2m2eTDv[kBmfG:yb4Pp[IUhd3JiY3nzdIxifGmw NVflUmlURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVM2PjFpPkK0PVU{PTZzPD;hQi=>
MO59K  NYn5[plESXCxcITvd4l{KEG|c3H5 MWCxNEDPxE1? NYfRR3JrOjRiaB?= M364UWROW09? M1\2[Ilv[3KnYYPld{B1cGViRGPCJIxmfmWuIHnu[JVk\WRiYomg[ZRweG:|aXTlJI9zKGOrc4DsZZRqdg>? M4i0NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUWzOVYyLz5{NEm1N|U3OTxxYU6=
MO59J M4PlW2Fxd3C2b4Ppd{BCe3OjeR?= NVj3dYl2OTBizszN NVPqXGZwOjRiaB?= MnHGSG1UVw>? NYHmPJEzcW6lcnXhd4V{KHSqZTDEV2IhdGW4ZXygbY5lfWOnZDDifUBmfG:yb4Pp[IUhd3JiY3nzdIxifGmw M3LkSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUWzOVYyLz5{NEm1N|U3OTxxYU6=
HepG2 M4TRSGZ2dmO2aX;uJGF{e2G7 M2n2b|ExOCCwTR?= M3vlTVAvPSCq NH3ORnlFVVOR NGD3fJVjdG:la4OgUWEucW6mdXPl[EBCc3RicHjvd5Bpd3K7bHH0bY9v MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh4M{O1NEc,OjR6NkOzOVA9N2F-
A549  M2XtR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXsXlQ{KML3TdMg NFzOcW4zKGh? M1faR5N2eHC{ZYPz[ZMheGWvZYTy[Zhm\C2rbnT1Z4VlKEGtdDDhcoQhT1ONM98yJIFkfGm4YYTpc44tKFNvcHjhd4Uh[XK{ZYP0MEBk\WyuIHHwc5B1d3OrczDhcoQh[2G|cHHz[U0{KGGldHn2ZZRqd25? MnXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6NEe4OlMoRjJ2OES3PFY{RC:jPh?=
A549  M1i1fWZ2dmO2aX;uJGF{e2G7 M1vJNFExyqEQvH5CpC=> M3rDbFE3KGh? MlfGSG1UVw>? M3frdI1w\HWuYYTld{B1cGViSVHWJJJmeGyrY3H0bY9vKGGwZDDjZZV{\XNicnX0[Y51cW:wIH;mJG5RKGmwIITo[UBvfWOuZYXzMi=> NIT3SlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEiwNlEyOSd-MkS4NFIyOTF:L3G+
SK-N-LO M{\Ke2Z2dmO2aX;uJGF{e2G7 NFy2SnEyODBibl2= MmTjNE42KGh? Mlyx[IVkemWjc3XzJJRp\SC|dHnteYxidnRiZX\m[YN1eyCxZjDtc5JxcGmwZTDvckBCc3RicHjvd5Bpd3K7bHH0bY9v MnTWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUS2NFYoRjJ2NkW0OlA3RC:jPh?=
HL-60 M1;vRmZ2dmO2aX;uJGF{e2G7 MoHENE4yyqEQvF2= NXPGRmJCPzJiaB?= NUDlenZs[myxY3vzJIRie2G2aX7pZk1qdmS3Y3XkJINmdGxiZHnm[oVz\W62aXH0bY9v M1v5c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkC3Nlc{Lz5{NE[wO|I4OzxxYU6=
HepG2  NV:0WYFbTnWwY4Tpc44hSXO|YYm= MXKyNFAhdk1? Mm\KNE42KGh? M{fl[IF1fGWwdXH0[ZMhTm:6TzDwbI9{eGixconsZZRqd25? NXvQN3ZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1N|UyQTJpPkK0OVM2OTl{PD;hQi=>
H520 M{D3cWZ2dmO2aX;uJGF{e2G7 MmDlNVDDqM7:TR?= MkfzNUBp MkHRSG1UVw>? MY\k[YNz\WG|ZYOgZ4VtdHWuYYKgdIhwe3Cqbz3BT3QheHKxdHXpckBt\X[nbIO= Ml7MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NEe5N|UoRjJ2NES3PVM2RC:jPh?=
H1975 M1vmOWZ2dmO2aX;uJGF{e2G7 M1flNFExyqEQvF2= MUGxJIg> M36zZmROW09? NUXPfWNG\GWlcnXhd4V{KGOnbHz1cIFzKHCqb4PwbI8uSUuWIIDyc5RmcW5ibHX2[Yx{ M{fBdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NES3PVM2Lz5{NES0O|k{PTxxYU6=
MG-63 MVPBdI9xfG:|aYOgRZN{[Xl? Mof2NVAhyrWP NIjuUncyOiCq NUjyOZc2\W6qYX7j[ZMhTFBvaX7keYNm\CCjcH;weI9{cXN? M3noUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W4N|AyLz5{NEO1PFMxOTxxYU6=
5637 MoTURZBweHSxc3nzJGF{e2G7 M2f1[VExyqEQvF2= MoPQOFAhdWmw M{LJUZJmfmW{c3XzJJAzOVeDRkGg[ZhxemW|c3nvckwhS0SNIHX4dJJme3Orb36sJIFv\CClZXzsJIlvcGmkaYTpc44hcW6mdXPl[EBjgSCodXPvbYRidg>? NYrUeIlHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|M5PjhpPkK0N|M{QDZ6PD;hQi=>
HEK-293 NWm2XW9yTnWwY4Tpc44hSXO|YYm= NInTfmEyPTCwTR?= MmrlNVYhcA>? MkL2SG1UVw>? MWDk[YNz\WG|ZYOgR3JVKGGldHn2bZR6 NF\ZVGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOyOFM3Pid-MkSzNlQ{PjZ:L3G+
SW480  MYjGeY5kfGmxbjDBd5NigQ>? MX[xOVBvVQ>? Mn3VNlAhcA>? M1L3SmROW09? NFvLeJZz\WS3Y3XzJINmdGy3bHHyJIFk[3WvdXzheIlwdiCxZjFOtk1k[XSnbnnu MkGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|MkSzOlYoRjJ2M{K0N|Y3RC:jPh?=
HepG2 MmWzSpVv[3Srb36gRZN{[Xl? NWm4V2ZpOTByIH7N MkH0NlQhcA>? MXHheJRmdnWjdHXzJJRp\SClb3zvcolmeyCxZjD0bIUhfHWvb4KgZ4VtdHNid3n0bEB2eHKnZ4XsZZRqd25ib3[gRYt1OQ>? M2exPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mkm3OVExLz5{NEK5O|UyODxxYU6=
HCT 116  MonqSpVv[3Srb36gRZN{[Xl? NELOVFYyODBibl2= NEHPZpkzPCCq MV;heJRmdnWjdHXzJJRp\SClb3zvcolmeyCxZjD0bIUhfHWvb4KgZ4VtdHNid3n0bEB2eHKnZ4XsZZRqd25ib3[gRYt1OQ>? M3XMbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mkm3OVExLz5{NEK5O|UyODxxYU6=
BEL/FU MYDGeY5kfGmxbjDBd5NigQ>? M1TlSlEhdU1? MW[yOEBp Mk[1[IVkemWjc3XzJJBzd3SnaX6gcIV3\Wy|IH;mJJRp\SCSSUPLM2FsfCCyYYToe4F6 M4G4UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkOyNFk6Lz5{NEKzNlA6QTxxYU6=
Huh7  NVW0cFdyTnWwY4Tpc44hSXO|YYm= NVfxcXp{O8LizszN NEXkVI8yKGh? MoDqdoVlfWOnczD0bIUhfmm{dYOg[Y51enliaX70c{B1cGViY3XscJM> M{TiXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUi0NVk3Lz5{NEG4OFE6PjxxYU6=
A-375 M3zHfGFxd3C2b4Ppd{BCe3OjeR?= NVvBV5A6PC96IN88US=> MmLuNlQhcA>? Moiw[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXQEoB?= NHfndpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGxN|E4Oyd-MkSxNVMyPzN:L3G+
A-375-TS  M37xN2Fxd3C2b4Ppd{BCe3OjeR?= Mlq3OE85KM7:TR?= MWSyOEBp NFjiWlhmdmijbnPld{BVWkGLTD3pcoR2[2WmIHHwc5B1d3Orc9Mg MlLBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMUOxO|MoRjJ2MUGzNVc{RC:jPh?=
Mel-HO NH\RfoVCeG:ydH;zbZMhSXO|YYm= MXS0M|gh|ryP M1vINFI1KGh? NEfvc45mdmijbnPld{BVWkGLTD3pcoR2[2WmIHHwc5B1d3Orc9Mg M1yz[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUGzNVc{Lz5{NEGxN|E4OzxxYU6=
Mel-HO-TS MmW5RZBweHSxc3nzJGF{e2G7 MlO0OE85KM7:TR?= MkPJNlQhcA>? NXLDUIp2\W6qYX7j[ZMhXFKDSVytbY5lfWOnZDDhdI9xfG:|aYRCpC=> NGPrS|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGxN|E4Oyd-MkSxNVMyPzN:L3G+
MeWo M1r3UWFxd3C2b4Ppd{BCe3OjeR?= NXjBNYNUPC96IN88US=> NIHxNHEzPCCq NFK0VJdmdmijbnPld{BVWkGLTD3pcoR2[2WmIHHwc5B1d3Orc9Mg MnfiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMUOxO|MoRjJ2MUGzNVc{RC:jPh?=
Mel-2a NV;uT2F5SXCxcITvd4l{KEG|c3H5 MWi0M|gh|ryP NXe0XJY1OjRiaB?= MX3lcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqe8Li M37kbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUGzNVc{Lz5{NEGxN|E4OzxxYU6=
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MDA-MB-231 MUXGeY5kfGmxbjDBd5NigQ>? M1HVZlQxOCCwTR?= NVPmWZY5PCCq MVnk[YNz\WG|ZYOgUW1RNTliYX7kJGlNNThicILveIVqdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mmf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7ME[yOVkoRjJ{OUC2NlU6RC:jPh?=
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Jurkat  NFzYS4tMcW6jc3WgRZN{[Xl? M{XmdmlEPTBib3[gNlQhdk1? NVLiWJZHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW2OlQ2OTlpPkG1OlY1PTF7PD;hQi=>
Sf9 NV7jcnRoTnWwY4Tpc44h[XO|YYm= NV7kXWVuUW6qaXLpeIlwdiCxZjDoeY1idiCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BjgSCobIXvdoV{[2WwdDDwc4xiemm8YYTpc44h[XO|YYmsJGlEPTBiPTCwMlAyOiEQvF2u MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTF{MU[zNUc,OjFzMkG2N|E9N2F-
HeLa MUTGeY5kfGmxbjDhd5NigQ>? MYnJcohq[mm2aX;uJI9nKEG[LUe1NFMh[mmwZHnu[{B1dyC{ZXPvcYJqdmGwdDDQcIs{KGW6cILld5Nm\CCrbjDI[WxiKGOnbHzzJIJ6KFenc4Tldo4h[myxdDygTWM2OCB;IECuNFQ6KM7:TT6= NXHCSFJZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUexN|UzPDhpPkG3NVM2OjR6PD;hQi=>
HeLa NVvleZk2TnWwY4Tpc44h[XO|YYm= MmjLRolv\GmwZzDh[oZqdmm2eTDmc5IhTE6DIHTldIVv\GWwdDDwdo91\WmwIHvpcoF{\SCrc3;sZZRm\CCocn;tJGhmVGFiY3XscJM8KFKjbnflJIl{KDJyLUGyNEwhU2liPTCwMlEzKM7:TT6= M1zmRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3NkW4PFcxLz5zNU[1PFg4ODxxYU6=
HeLa NWf3N5k{TnWwY4Tpc44h[XO|YYm= NV7mTZhQSmmwZHnu[{Bi\m[rbnn0fUBnd3JiUHjvd5Bp[XSrZInsbY5we2m2b3ygN{1scW6jc3WgbZNwdGG2ZXSg[pJwdSCKZVzhJINmdGy|OzDSZY5o\SCrczCyNE0yOjBuIFvpJF0hOC5zMjFOwG0v M3vUTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3NkW4PFcxLz5zNU[1PFg4ODxxYU6=
A549 NF3vTGRHfW6ldHnvckBie3OjeR?= NUDRVpNJUW6qaXLpeIlwdiCxZjDQcIs{KGmwIHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4F{\WmwIIP1ZpN1emG2ZTDwbI9{eGixconsZZRqd25iYomgW4V{fGW{bjDicI91NCCLQ{WwJF0hOC5{MjFOwG0v NV\O[|VpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUexN|UzPDhpPkG3NVM2OjR6PD;hQi=>
A549 NFfWe2ZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NI\L[oQ1QCCqcoO= MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDt[ZRpd2RuIFnDOVAhRSBzMT60JO69VS5? M4T4WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkOwPFk1Lz5zOE[zNFg6PDxxYU6=
GM00637 Mon0SpVv[3Srb36gZZN{[Xl? M{HESVEhfU1? NWnxU4dYUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBRdGt|IHX4dJJme3OnZDDpckBpfW2jbjDHUVAxPjN5IHPlcIx{KGG2IEGgeW0h[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gdFU{KHOncnnu[U0zOCCyaH;zdIhwenmuYYTpc44> MnLRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTdzM{WyOFgoRjF5MUO1NlQ5RC:jPh?=
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HeLa MVzGeY5kfGmxbjDhd5NigQ>? MmW2NVAxKG6P MlPlNVAhdWmwcx?= M4nWRmlvcGmkaYTpc44hd2ZiUFmzT{BqdiCqdX3hckBJ\UyjIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBGT0Zvc4TpcZVt[XSnZDDBT3QheGixc4Doc5J6dGG2aX;uJIF1KFN2N{OgZZQhOTByIH7NJJBz\WmwY4XiZZRm\CCob4KgNVAhdWmwczDmc4xtd3enZDDifUBGT0Zic4TpcZVt[XSrb36gcYVie3W{ZXSgZYZ1\XJiNTDtbY5{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NHnvVGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO4NFg3PSd-M{CzPFA5PjV:L3G+
HeLa MmTpSpVv[3Srb36gZZN{[Xl? MY[xNFAhdk1? NFzVfY4yOCCvaX7z MlfJTY5pcWKrdHnvckBw\iCSSUPLJIlvKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGVITi2|dHnteYxifGWmIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhXDNyODDheEAyODBibl2gdJJmcW6ldXLheIVlKG[xcjCxNEBucW6|IH\vcIxwf2WmIHL5JGVITiC|dHnteYxifGmxbjDt[YF{fXKnZDDh[pRmeiB3IH3pcpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NHjyRmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO4NFg3PSd-M{CzPFA5PjV:L3G+

... 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 SL-2052, BRN 0067676, NSC 627609
Smiles CC(=O)OC1CC2(C(CCC2=O)C3=C1C4(C(OC(=O)C5=COC(=C54)C3=O)COC)C)C

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID