Wortmannin (KY 12420)

For research use only.

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

242 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.

Selleck's Wortmannin (KY 12420) has been cited by 242 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 NV\CVlFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1P2blIvPSEQvF2= NYOwd2QzOS12IHS= NXrHdGZHTE2VTx?= M1H0TIVvcGGwY3XzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25idILlZZRu\W62IIfpeIghfGGvb4jp[oVv MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR7MEO4N{c,OjV2OUCzPFM9N2F-
H1703 MoW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuyMlUh|ryP MYKxMVQh\A>? MWjEUXNQ M2TsbYVvcGGwY3XzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25idILlZZRu\W62IIfpeIghfGGvb4jp[oVv M2TXbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEmwN|g{Lz5{NUS5NFM5OzxxYU6=
HUVECs M3vlPWN6fG:2b4jpZ4l1gSCDc4PhfS=> MWKxNFAhdk1? NIK1[4kzPCCq MXjheJRmdnWjdHXzJJRp\SCjYoLv[4F1cX[nIHXm[oVkfHNib3[gZ4FtgWOxc3nuJI9vKF[UST3pcoR2[2WmIHP5eI91d3irY3n0fS=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3MEG4Okc,OjV2NUCxPFY9N2F-
APRE-19 NUHrTpFuSXCxcITvd4l{KEG|c3H5 M3O4XVUh|ryP M1jsZlI1KGh? NWC2WJlQ[WKxbHnzbIV{KE[OWj3t[YRq[XSnZDDwdo8ue3W{dnn2ZYww[W62aT3hdI9xfG:|aYOgZYN1cX[rdIm= M2PufVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{K5OlE4Lz5{NUOyPVYyPzxxYU6=
MDA-MB-231 NHPwOXpCeG:ydH;zbZMhSXO|YYm= NWWxXlExOcLizszNxsA> MlzGOFghcA>? MX\EUXNQ NGf4OoJl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhfHKnYYTl[EB4cXSqIEK1JO69VSCxZjDGNUBweiCIMjFCpC=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMEmzNkc,OjV|MEC5N|I9N2F-
MCF7 NGjheopHfW6ldHnvckBCe3OjeR?= MojlNVAxKG6P MUKyOEBp NVLhTnNu\WyrbXnuZZRmeyCHMj3pcoR2[2WmIFHSSU1NfWNiYXP0bZZqfHl? M4nHe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUeyOVU4Lz5{NUG3NlU2PzxxYU6=
HT-29  NWDVO3hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHHNI1tOS53wrFCuW0> Mkj0PVYhcA>? M1KyZ4Rm[3KnYYPld{Bk\WyuIHfyc5d1cCC5aHnjbEBk[W5iYnWgbY5pcWKrdHXkJIJ6KEu\TlG= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzMkGyN{c,OjVyMUKxNlM9N2F-
MO59K  NFHYNY9EgXSxdH;4bYNqfHliQYPzZZk> NHfibJA2yqEQvF2= NXf4NmR7PyCm NXLadYxJTE2VTx?= NVryblZl\W6qYX7j[ZMhfGinIHP5eI91d3irY3n0fUBw\iCndH;wc5Nq\GVib4KgZ4l{eGyjdHnu MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3M{W2NUc,OjR7NUO1OlE9N2F-
MO59J M2i4b2N6fG:2b4jpZ4l1gSCDc4PhfS=> MojPOeKh|ryP NFK4eWE4KGR? Ml23SG1UVw>? NYTX[ZNV\W6qYX7j[ZMhfGinIHP5eI91d3irY3n0fUBw\iCndH;wc5Nq\GVib4KgZ4l{eGyjdHnu Mm\sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NUO1OlEoRjJ2OUWzOVYyRC:jPh?=
MO59K  M1jtRWFxd3C2b4Ppd{BCe3OjeR?= M3\relExKM7:TR?= M1\uelI1KGh? M4fqNmROW09? NIHmUnNqdmO{ZXHz[ZMhfGinIFTTRkBt\X[nbDDpcoR2[2WmIHL5JIV1d3Cxc3nk[UBweiClaYPwcIF1cW5? NXi5[ZZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVM2PjFpPkK0PVU{PTZzPD;hQi=>
MO59J NWPUZ5FMSXCxcITvd4l{KEG|c3H5 NVLUOIU3OTBizszN NYj0SWNGOjRiaB?= MYrEUXNQ M3u3U4lv[3KnYYPld{B1cGViRGPCJIxmfmWuIHnu[JVk\WRiYomg[ZRweG:|aXTlJI9zKGOrc4DsZZRqdg>? M2H5ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUWzOVYyLz5{NEm1N|U3OTxxYU6=
HepG2 Mm\uSpVv[3Srb36gRZN{[Xl? MlPkNVAxKG6P NFfBT5AxNjViaB?= MnTVSG1UVw>? Mnr4Zoxw[2u|IF3BMYlv\HWlZXSgRYt1KHCqb4PwbI9zgWyjdHnvci=> M3\qOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OE[zN|UxLz5{NEi2N|M2ODxxYU6=
A549  NWLoOnJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37tcVMhyrWPwrC= M321dlIhcA>? MnXFd5VxeHKnc4Pld{Bx\W2ndILlfIVlNWmwZIXj[YQhSWu2IHHu[EBIW0t|zsKgZYN1cX[jdHnvckwhWy2yaHHz[UBienKnc4SsJINmdGxiYYDvdJRwe2m|IHHu[EBk[XOyYYPlMVMh[WO2aY\heIlwdg>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh2N{i2N{c,OjR6NEe4OlM9N2F-
A549  NUDCeVhUTnWwY4Tpc44hSXO|YYm= MknBNVDDqM7:bdMg Ml;MNVYhcA>? NIHEdI9FVVOR MVPtc4R2dGG2ZYOgeIhmKEmDVjDy[ZBtcWOjdHnvckBidmRiY3H1d4V{KHKndHXueIlwdiCxZjDOVEBqdiC2aHWgcpVkdGW3cz6= MmToQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MEKxNVEoRjJ2OECyNVEyRC:jPh?=
SK-N-LO MoDRSpVv[3Srb36gRZN{[Xl? MWqxNFAhdk1? MYCwMlUhcA>? MYjk[YNz\WG|ZYOgeIhmKHO2aX31cIFvfCCnZn\lZ5R{KG:oIH3vdpBpcW6nIH;uJGFsfCCyaH;zdIhwenmuYYTpc44> NInuPYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1OFYxPid-MkS2OVQ3ODZ:L3G+
HL-60 NWKxdGNTTnWwY4Tpc44hSXO|YYm= MXSwMlHDqM7:TR?= NInaO2U4OiCq MVXicI9kc3NiZHHzZZRqdmmkLXnu[JVk\WRiY3XscEBlcW[oZYLlcpRq[XSrb36= NHnQRm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[wO|I4Oyd-MkS2NFczPzN:L3G+
HepG2  Mlm4SpVv[3Srb36gRZN{[Xl? MnS0NlAxKG6P NUj2d3Z[OC53IHi= MoXaZZR1\W63YYTld{BHd3iRIIDoc5NxcG:{eXzheIlwdg>? NF36Opc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWzOVE6Oid-MkS1N|UyQTJ:L3G+
H520 MYXGeY5kfGmxbjDBd5NigQ>? MWOxNOKh|ryP NYnud4ZOOSCq NGjmb4dFVVOR MYLk[YNz\WG|ZYOgZ4VtdHWuYYKgdIhwe3Cqbz3BT3QheHKxdHXpckBt\X[nbIO= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR2N{mzOUc,OjR2NEe5N|U9N2F-
H1975 Mo\nSpVv[3Srb36gRZN{[Xl? NGXifGcyOMLizszN MYOxJIg> NVz5c3FQTE2VTx?= MXPk[YNz\WG|ZYOgZ4VtdHWuYYKgdIhwe3Cqbz3BT3QheHKxdHXpckBt\X[nbIO= NGDBR5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES0O|k{PSd-MkS0OFc6OzV:L3G+
MG-63 M4S5[WFxd3C2b4Ppd{BCe3OjeR?= M3nJblExKML3TR?= MkT3NVIhcA>? MnXB[Y5p[W6lZYOgSHAucW6mdXPl[EBieG:ydH;zbZM> MoCyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NUizNFEoRjJ2M{W4N|AyRC:jPh?=
5637 NUnnRmhNSXCxcITvd4l{KEG|c3H5 NVG1XoQ{OTEEoN88US=> Mn7wOFAhdWmw M4TLV5JmfmW{c3XzJJAzOVeDRkGg[ZhxemW|c3nvckwhS0SNIHX4dJJme3Orb36sJIFv\CClZXzsJIlvcGmkaYTpc44hcW6mdXPl[EBjgSCodXPvbYRidg>? NID5XlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzN|g3QCd-MkSzN|M5Pjh:L3G+
HEK-293 MmLmSpVv[3Srb36gRZN{[Xl? NE\RfmEyPTCwTR?= NFjOSIsyPiCq MV\EUXNQ MnnH[IVkemWjc3XzJGNTXCCjY4Tpeol1gQ>? NIHDVXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOyOFM3Pid-MkSzNlQ{PjZ:L3G+
SW480  M4[zZWZ2dmO2aX;uJGF{e2G7 MXmxOVBvVQ>? NETST2UzOCCq MWfEUXNQ M{npXJJm\HWlZYOgZ4VtdHWuYYKgZYNkfW23bHH0bY9vKG:oIN8yMYNifGWwaX6= NHW1O4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOyOFM3Pid-MkSzNlQ{PjZ:L3G+
HepG2 MWjGeY5kfGmxbjDBd5NigQ>? MluzNVAxKG6P M2j0cVI1KGh? M176T4F1fGWwdXH0[ZMhfGinIHPvcI9vcWW|IH;mJJRp\SC2dX3vdkBk\WyuczD3bZRpKHWycnXneYxifGmxbjDv[kBCc3Rz NE\vXlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK5O|UyOCd-MkSyPVc2OTB:L3G+
HCT 116  NULOcIJ[TnWwY4Tpc44hSXO|YYm= M1XQR|ExOCCwTR?= NH:3TpMzPCCq M2DXN4F1fGWwdXH0[ZMhfGinIHPvcI9vcWW|IH;mJJRp\SC2dX3vdkBk\WyuczD3bZRpKHWycnXneYxifGmxbjDv[kBCc3Rz MkfwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OUe1NVAoRjJ2Mkm3OVExRC:jPh?=
BEL/FU MWDGeY5kfGmxbjDBd5NigQ>? M2rafFEhdU1? M{HHeFI1KGh? MWDk[YNz\WG|ZYOgdJJwfGWrbjDs[ZZmdHNib3[geIhmKFCLM1uvRYt1KHCjdHj3ZZk> NWLyOnlVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyN|IxQTlpPkK0NlMzODl7PD;hQi=>
Huh7  NHrPZnpHfW6ldHnvckBCe3OjeR?= NU[5fYE2O8LizszN M2fFOFEhcA>? MlzBdoVlfWOnczD0bIUhfmm{dYOg[Y51enliaX70c{B1cGViY3XscJM> M2P4VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUi0NVk3Lz5{NEG4OFE6PjxxYU6=
A-375 NES2fZdCeG:ydH;zbZMhSXO|YYm= Mn32OE85KM7:TR?= NGHrN3EzPCCq MkTY[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXQEoB?= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFzM{G3N{c,OjRzMUOxO|M9N2F-
A-375-TS  NWXDT4pTSXCxcITvd4l{KEG|c3H5 MVm0M|gh|ryP NV\MSZVDOjRiaB?= NGrKfpBmdmijbnPld{BVWkGLTD3pcoR2[2WmIHHwc5B1d3Orc9Mg NH3JTFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGxN|E4Oyd-MkSxNVMyPzN:L3G+
Mel-HO NF7XOo1CeG:ydH;zbZMhSXO|YYm= M4rJTVQwQCEQvF2= M2fmc|I1KGh? NFvSSWRmdmijbnPld{BVWkGLTD3pcoR2[2WmIHHwc5B1d3Orc9Mg MkG1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMUOxO|MoRjJ2MUGzNVc{RC:jPh?=
Mel-HO-TS M4PyUGFxd3C2b4Ppd{BCe3OjeR?= M2f2XVQwQCEQvF2= NF\qO4ozPCCq M1H2eoVvcGGwY3XzJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m|wrC= NYi4NlR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNVMyPzNpPkK0NVE{OTd|PD;hQi=>
MeWo NXLhSYhZSXCxcITvd4l{KEG|c3H5 MX:0M|gh|ryP M32yXVI1KGh? M16xVoVvcGGwY3XzJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m|wrC= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFzM{G3N{c,OjRzMUOxO|M9N2F-
Mel-2a NYq1eWZGSXCxcITvd4l{KEG|c3H5 NVm1RYFJPC96IN88US=> MlXhNlQhcA>? MXflcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqe8Li MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFzM{G3N{c,OjRzMUOxO|M9N2F-
MDA-MB-231 NHLRPFBHfW6ldHnvckBCe3OjeR?= MVWw5qCUPDByIH7N MX20JIg> NXTtbGw{e3WycILld5NmeyCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M3LNRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUC2NlU6Lz5{MkmwOlI2QTxxYU6=
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... 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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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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