Zileuton (A-64077)

For research use only.

Catalog No.S1443 Synonyms: Abbott 64077, ZYFLO

4 publications

Zileuton (A-64077) Chemical Structure

CAS No. 111406-87-2

Zileuton (A-64077, Abbott 64077, ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.

Selleck's Zileuton (A-64077) has been cited by 4 publications

1 Customer Review

  • CD19+ B cells (A) or PBMCs (B) from a healthy donor were treated with zileuton (10 μM) prior to 17-HDHA or RvD1 treatment, followed by stimulation with the IgE-inducing cocktail. Cell culture supernatants were collected at day 7, and IgE levels were measured. The experiment was done in one representative donor (mean ± SEM). Data were analyzed by 1-way ANOVA with Tukey’s post test, **P ≤ 0.01, ***P ≤ 0.001. PBMC, peripheral blood mononuclear cell.

    JCI Insight, 2017, 2(3):e88588. Zileuton (A-64077) purchased from Selleck.

Purity & Quality Control

Choose Selective Lipoxygenase Inhibitors

Biological Activity

Description Zileuton (A-64077, Abbott 64077, ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.
Targets
Ferroptosis [6]
()
5-lipoxygenase [1]
()
In vitro

Zileuton suppresses PG biosynthesis by interference with arachidonic acid (AA) release in macrophages. Zileuton significantly reduces PGE2 and 6-keto prostaglandin F1α (PGF1α) levels in activated mouse peritoneal macrophages and in J774 macrophages. Zileuton inhibits PGE2 production in LPS-stimulated human whole blood and suppresses PGE2 and 6-keto PGF1α pleural levels in rat carrageenan-induced pleurisy. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RBI-1 M4nNe2Z2dmO2aX;uJIF{e2G7 MXHJckB3cXS{bzDpcohq[mm2aX;uJI9nKDVvbHnwc5h6\2WwYYPlJEg2NWyxKTDmdo9uKHSqZTCyNFAxOCCpIIP1dIVzdmG2YX70JI9nKFKEST2xJINmdGy|LDDJR|UxRTBwNt88US=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ4OUi5K|4zODZ4OUi5QE9iRg>?
RBL-1 M1;QdWZ2dmO2aX;uJIF{e2G7 MmKwTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiNT3sbZBwgHmpZX7hd4UhcW5icnH0JHJDVC1zIHPlcIx{NCCLQ{WwQVMvOs7:TR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek85QDNzN{W5K|45QDNzN{W5QE9iRg>?
basophilic leukemia cells MmO0SpVv[3Srb36gZZN{[Xl? NHXnTHdKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhPS2uaYDvfJlo\W6jc3Wgc4J1[WmwZXSg[pJwdSC{YYSgZoF{d3CqaXzpZ{Bt\XWtZX3pZUBk\WyuczygTWM2OD1yLkZOwG0> M3zQd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzl2OES0PVMoRjl2OES0PVM9N2F-
RBL-2H3 MkPUSpVv[3Srb36gZZN{[Xl? Mk\NTY5pcWKrdHnvckBw\iB3LXzpdI95gWenbnHz[UBu\WSrYYTl[EBkd264ZYLzbY9vKG:oIGuxOGNe[XKjY3jp[I9vcWNiYXPp[EB1dyCuZYXrc5RzcWWwZYOgbY4hWkKOLULIN{Bk\WyuczygTWM2OD1yLkiwOO69VQ>? NGH0XmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi97NUm5NlQ3Lz57NUm5NlQ3RC:jPh?=
granulocytes-type cells MorOSpVv[3Srb36gZZN{[Xl? NWPnWZZJXGinIHPvcZBwfW6mIIfhd{BmfmGudXH0[YQh\m:{IHn0d{BqdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhPS2uaYDvfJlo\W6jc3WgeZNqdmdiZ4LhcpVtd2O7dHXzMZR6eGViY3XscJMtKEmFNUC9Nk46|ryP NGD0eIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUi1PVAxOSd-MUG4OVkxODF:L3G+
polymorphonuclear cells M1;LRmFvfGmuZYXrc5RzcWWwaXOgZZN{[Xl? MXvBcpRqdGW3a3;0dolmdmmlIHHjeIl3cXS7IHnuJJJifCCyb3z5cY9zeGixboXjcIVieiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxVSjRiYnnvd5lvfGinc3nzMEBKSzVyPUCuNFHPxE1? Moi4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2NEi1O|UoRjF5NES4OVc2RC:jPh?=
MC9 NU\ZVYpwTnWwY4Tpc44h[XO|YYm= NX\ncW1OUW6qaXLpeIlwdiCxZjDMWGI1KHC{b3T1Z5Rqd25iaX6gcY92e2ViTVO5JINmdGy|LDDJR|UxRTBwNUZOwG0> M{HNbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEm4NVUxLz5zOES5PFE2ODxxYU6=
MC9 NEW4cJhHfW6ldHnvckBie3OjeR?= MVvJcohq[mm2aX;uJI9nKGyndXvveJJq\W6nczDwdo9lfWO2aX;uJIlvKG2xdYPlJG1EQSClZXzsdy=> NF22Tmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES5PFE2OCd-MUi0PVgyPTB:L3G+
PMNL Ml;wSpVv[3Srb36gZZN{[Xl? MmXSNVUhdWmwcx?= NGPwRpJKdmirYnn0bY9vKG:oIEWtcIlxd3i7Z3XuZZNmKGmwIHPlcIwh\nKnZTDTNVAxKG[{ZYPocJkhcXOxbHH0[YQhcHWvYX6gVG1PVCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGEzOzF6Nz3zeIlufWyjdHXkJFUuVE9icILv[JVkfCCob4LtZZRqd25icILlbY5kfWKjdHXkJIZweiBzNTDtbY5{KG2nYYP1doVlKGGodHXyJFExKG2rboOgZpkhUFCOQzDhcoFtgXOrczygTWM2OD1yLkZOwG0> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV3MU[yPUc,OjJ3NUG2Nlk9N2F-
BMM NEPHN5RHfW6ldHnvckBie3OjeR?= MX[zNEBucW6| NYi4VJBqUW6qaXLpeIlwdiCxZjC1MWxQKGmwIH3veZNmKEKPTTDj[YxteyCjc4Pld5Nm\CCjczDmc5Ju[XSrb36gc4YhVFSFNDDh[pRmeiB|MDDtbY5{KGK7IHXufplu\SCrbX31co9ie3OjeTygTWM2OD1yLkG5{txO NY\2UlVQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0N|I3ODVpPkK2OFMzPjB3PD;hQi=>
A549 M4fGN2Z2dmO2aX;uJIF{e2G7 NV\4e5BTOTVibXnudy=> MYHJcohq[mm2aX;uJI9nKG2SR1XTMVEhcXOxbHH0[YQh\nKxbTDtbYNzd3OxbXXzJI9nKGmwdHXycIV2c2mwLUGgZoV1[S2|dHnteYxifGWmIHj1cYFvKEF3NEmgZ4VtdHNidYPpcochWEeKMjDhd{B{fWK|dILheIUheHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAyKG2rbjDifUBTWC2KUFzDJIFv[Wy7c3nzMEBKSzVyPUCuOu69VQ>? NWXndIZ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwOVM4OjBpPkOwNFU{PzJyPD;hQi=>
RAW264.7 MVzGeY5kfGmxbjDhd5NigQ>? NWjidmZXPSC3TR?= M{nnR|I1KGi{cx?= M1nsXmlvcGmkaYTpc44hd2ZiTGDTM2lHVmejbX3hMZN1cW23bHH0[YQhdGmyaXSgdIVzd3irZHH0bY9vKGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIF1KDVidV2gZYZ1\XJiMkSgbJJ{KGK7IFLPSGlRYSB3OEGvOVkyKENzMT3zeIFqdmmwZzDiZZNm\CCIQVPTJIF{e2G7 NVOxdlZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OlQzQTVpPkOwPVY1Ojl3PD;hQi=>
RAW264.7 NGHxVlFHfW6ldHnvckBie3OjeR?= MVG1JJVO NVGy[np5PDhiaILz MYnQdo91\WO2aX;uJIFo[Wmwc4SgUHBUNWmwZIXj[YQh[2WubDDk[YF1cCCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDj[YxtKH[rYXLpcIl1gSCjdDC1JJVOKG2nYYP1doVlKGGodHXyJFQ5KGi{czDifUBOXFNiYYPzZZkhemWuYYTpeoUhfG9iY3;ueJJwdA>? NVPpfZAyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OlQzQTVpPkOwPVY1Ojl3PD;hQi=>
PMNL Ml;XSpVv[3Srb36gZZN{[Xl? NGHXdpM2KG2rboO= NHHRbYVKdmirYnn0bY9vKG:oIEWtUG8hcW5iaIXtZY4hWE2QTDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hdGW3a3;0dolmdmViZn;ycYF1cW:wIIDy[Ylv[3WkYYTl[EBnd3JiNTDtbY5{KG[xbHzve4VlKGK7IIToZZB{cWejcnfpckB{fGmvdXzheIlwdiCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KFKSLVjQUGMh[W6jbInzbZMtKEmFNUC9Nk4{Oc7:TR?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTJ4MEi4PUc,OzF{NkC4PFk9N2F-
HEK293 MX7GeY5kfGmxbjDhd5NigQ>? NHvTTnUyKHWP MXS1JI1qdnN? M2HrZWlvcGmkaYTpc44hd2ZiaIXtZY4hPS2OTzD0doFve2[nY4Tl[EBqdiCKRVuyPVMh[2WubIOgZ49mgHC{ZYPzbY5oKE[OQWCgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHzleYtwfHKrZX7lJIZwem2jdHnvckBifCBzIIXNJJV{cW6pIHHyZYNpcWSxbnnjJIFkcWRiYYOgd5Vje3S{YYTlJJBz\WmwY4XiZZRm\CCob4KgOUBucW6|IH\vcIxwf2WmIHL5JINidGOrdX2gbY9vd3Cqb4LlJGEzOzF6Nz;hdoFkcGmmb37pZ{Bi[2mmIHHk[Il1cW:wIHHu[EBu\Q>? NUL0e|k5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GyOlA5QDlpPkOxNlYxQDh7PD;hQi=>
PMNL M2T5cWZ2dmO2aX;uJIF{e2G7 NGOzZVgyKHWP NFP3PYc2KG2rboO= NH64cJRKdmirYnn0bY9vKG:oIEWtUG8hcW5iaIXtZY4hWE2QTDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hdGW3a3;0dolmdmViZn;ycYF1cW:wIHH0JFEhfU1icILlbY5kfWKjdHXkJIZweiB3IH3pcpMh\m:ubH;3[YQh[nlidHjhdJNq\2G{Z3nuJJN1cW23bHH0bY9vKG2nYYP1doVlKGGodHXyJFE2KG2rboOgZpkhWlBvSGDMR{BidmGueYPpd{Bz\WyjdHn2[UB1dyClb370do9t NF:4Z4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUK2NFg5QSd-M{GyOlA5QDl:L3G+
BL21 (DE3) NWXj[FNYTnWwY4Tpc44h[XO|YYm= M1rOfFExKG2rboO= Mnq5TY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiB3LXzpdI95gWenbnHz[UBmgHC{ZYPz[YQhcW5iRYPjbIVzcWOqaXGgZ49tcSCETEKxJEhFTTNrIHPlcIx{KHW|aX7nJIFz[WOqaXTvcolkKGGlaXSgZZMhe3Wkc4TyZZRmKHC{ZXnuZ5Vj[XSnZDDmc5IhOTBibXnud{Bnd2yub4fl[EBjgSC|dYPieJJifGViYXTkbZRqd25iYX7kJI1m[XO3cnXkJIFnfGW{IEGwJI1qdnNiYomgdoV3\XK|ZTDwbIF{\SCKUFzDJI1mfGixZDygTWM2OD1yLkZOwG0> NUHuVYFRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G0OlUzOjVpPkOxOFY2OjJ3PD;hQi=>
insect cells NX\IT5B3TnWwY4Tpc44h[XO|YYm= M1HlWVUhdWmwcx?= NXi4R4l4UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDC1MWxQYCCneIDy[ZN{\WRiaX6gbY5{\WO2IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJJBzd2S3Y4Tpc44hd2ZiNT3IVGVVTSCjbnSgOU1JTVSHIIXzbY5oKGG{YXPobYRwdmmlIHHjbYQh[XNic4Xid5Rz[XSnIIDy[Ylv[3WkYYTl[EBnd3JiNTDtbY5{KG[xbHzve4VlKGK7IIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB{MDDtbY5{KGmwIHThdosh[nliZnXydolkKGmxLDDJR|UxRTJ|LkpOwG0> NH\ZSow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUe3OFY4Pid-M{G3O|Q3PzZ:L3G+
RBL-2H3 NXjIclZCTnWwY4Tpc44h[XO|YYm= NGHaSmhKdmirYnn0bY9vKG:oIEWtUIlxd3i7Z3XuZZNmKG:oIILheEBj[XOxcHjpcIlkKGyndXvlcYliKGOnbHzzMEBKSzVyPUCuNVTPxE1? M4f3cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{Nyd-Q3jFUWJNRC:jPh?=
Sf21 MVjGeY5kfGmxbjDhd5NigQ>? MWi0JI1qdnN? MnLqTY5pcWKrdHnvckBw\iC{YYSgOU1NV1hiZYjwdoV{e2WmIHnuJHNnOjFiaX7z[YN1KGOnbHzzJJBz\WmwY4XiZZRm\CCob4KgOEBucW6|IH\vcIxwf2WmIHL5JGFCKHO3YoP0doF1\SCjZHTpeIlwdiCjbnSgcYVie3W{ZXSgZYZ1\XJiNDDtbY5{KGK7IF\PXEBie3OjeTygTWM2OD1yLkG4{txO NVrYXopJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTNxJ{7DbGVOSkx:L3G+
RBL-2H3 NHLCXVRHfW6ldHnvckBie3OjeR?= NHnBPIRKdiC4aYTyc{BqdmirYnn0bY9vKG:oIEWtcIlxd3i7Z3XuZZNmKGmwIGLCUE0zUDNiKGLheEBj[XOxcHjpcIlkKGyndXvlcYliMSClZXzsd{whUUN3ME2xMlI2|ryP NXf6coJuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTNxJ{7DbGVOSkx:L3G+

... Click to View More Cell Line Experimental Data

In vivo

Zileuton significantly reduces macroscopic damage score after four weeks of treatment in rats. Zileuton administration significantly increases the intracolonic release of both thromboxane B2 at week 1 and prostaglandin E2 at weeks 2 and 4 in rats. [2] Zileuton reduces the spinal cord inflammation and tissue injury, neutrophil infiltration, TNF-alpha, COX-2 and pERK1/2 expression, PGE(2) and LTB(4) production, and apoptosis in mice. Zileuton significantly improves the recovery of limb function over 10 days in mice.[3]

 

Zileuton administrated before I/R significantly reduces the degree of renal dysfunction (urea, creatinine) and injury (AST, histology) in 5-lipoxygenase knockout mice. Zileuton reduces the expression of ICAM-1 and the associated PMN infiltration caused by I/R of the mouse kidney in 5-lipoxygenase knockout mice. [4]

 

Zileuton inhibits LTB(4) production in the peritonitis model more effectively than the LTA(4)H inhibitor, but the influx of neutrophils into the peritoneum after 1 and 2 hours is significantly higher in Zileuton- versus JNJ-26993135-treated mice. [5]

Protocol

Solubility (25°C)

In vitro DMSO 47 mg/mL (198.9 mM)
Water Insoluble
Ethanol '''47 mg/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 236.29
Formula

C11H12N2O2S

CAS No. 111406-87-2
Storage powder
in solvent
Synonyms Abbott 64077, ZYFLO
Smiles CC(C1=CC2=CC=CC=C2S1)N(C(=O)N)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01136941 Completed Drug: Zileuton Sickle Cell Disease Children''s Hospital Medical Center Cincinnati September 2010 Phase 1
NCT01130688 Terminated Drug: Zileuton Chronic Myelogenous Leukemia University of Massachusetts Worcester January 2010 Phase 1

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID