SP2509

Catalog No.S7680 Synonyms: HCI-2509

For research use only.

SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.

SP2509 Chemical Structure

CAS No. 1423715-09-6

Selleck's SP2509 has been cited by 21 publications

Purity & Quality Control

Choose Selective Histone Demethylase Inhibitors

Biological Activity

Description SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.
Targets
LSD1 [1]
(Cell-free assay)
13 nM
In vitro

In AML cells, SP2509 inhibits the association of LSD1 with CoREST, increases promoter-specific H3K4Me3 and induces p53, p21 and C/EBPα. SP2509 also significantly inhibits the colony growth and induces apoptosis of OCI-AML3. In addition, SP2509 induces differentiation of cultured and primary AML cells, and exerts synergistic lethal activity when used in combination with panobinostat. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87 MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYi5OkBp MljnS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gWVg4KGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDBWHBtcXSnIHz1cYlv\XOlZX7j[UBie3OjeTDJR|UxRTFwMU[g{txO M1HUcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkO3NVk2Lz5{NEKzO|E6PTxxYU6=
SK-N-MC M3vIb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXO5OkBp MWDHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDTT{1PNU2FIHPlcIx{KGGodHXyJFk3KGi{czDifUBCXFCuaYTlJIx2dWmwZYPj[Y5k\SCjc4PhfUBKSzVyPUCuN|I6KM7:TR?= Ml;6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{M{exPVUoRjJ2MkO3NVk2RC:jPh?=
T47D NYPIVJAyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTiPVYhcA>? NVfwZohiT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hXDR5RDDj[YxteyCjZoTldkA6PiCqcoOgZpkhSVSSbHn0[UBtfW2rbnXzZ4Vv[2ViYYPzZZkhUUN3ME2wMlY1QSEQvF2= NUDhdWNLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyN|cyQTVpPkK0NlM4OTl3PD;hQi=>
PC3 NFLrUnFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{jXNVk3KGh? NVnTfWVIT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFk3KGi{czDifUBCXFCuaYTlJIx2dWmwZYPj[Y5k\SCjc4PhfUBKSzVyPUKuNVYh|ryP Mn\FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{M{exPVUoRjJ2MkO3NVk2RC:jPh?=
PANC1 MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3nPflk3KGh? NXzpXY9UT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hWEGQQ{GgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KEGWUHzpeIUhdHWvaX7ld4NmdmOnIHHzd4F6KEmFNUC9NU4yODRizszN MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ|N{G5OUc,OjR{M{exPVU9N2F-
MIAPaCa2 MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4XhOlk3KGh? MVLHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNTWFR[UOjMjDj[YxteyCjZoTldkA6PiCqcoOgZpkhSVSSbHn0[UBtfW2rbnXzZ4Vv[2ViYYPzZZkhUUN3ME2wMlQ3QCEQvF2= M{\2d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkO3NVk2Lz5{NEKzO|E6PTxxYU6=
MDA-MB-468 MoHUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXPjOol3QTZiaB?= NWTtW|RkT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{Bi\nSncjC5OkBpenNiYomgRXRRdGm2ZTDseY1qdmW|Y3XuZ4Uh[XO|YYmgTWM2OD1{LkezJO69VQ>? NH7V[oY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKzO|E6PSd-MkSyN|cyQTV:L3G+
MDA-MB-435 M3HEdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYfj[ok3QTZiaB?= M4\vWWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20N|Uh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFHUVIxqfGVibIXtbY5me2OnbnPlJIF{e2G7IFnDOVA:OS52NDFOwG0> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ|N{G5OUc,OjR{M{exPVU9N2F-
MDA-MB-231 M1TnbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn;FPVYhcA>? MlP1S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB7NjDodpMh[nliQWTQcIl1\SCudX3pcoV{[2WwY3WgZZN{[XliSVO1NF0yNjB2IN88US=> NVrEUW97RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyN|cyQTVpPkK0NlM4OTl3PD;hQi=>
MCF7 NEHJSWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGrPUYY6PiCq MoTsS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC5OkBpenNiYomgRXRRdGm2ZTDseY1qdmW|Y3XuZ4Uh[XO|YYmgTWM2OD1yLk[zO{DPxE1? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ|N{G5OUc,OjR{M{exPVU9N2F-
HT-29 NVPmbXdZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWHPNYlUQTZiaB?= NITYdo5Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA6PiCqcoOgZpkhSVSSbHn0[UBtfW2rbnXzZ4Vv[2ViYYPzZZkhUUN3ME2wMlQzQSEQvF2= M4nQ[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkO3NVk2Lz5{NEKzO|E6PTxxYU6=
Hs MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnLWPVYhcA>? NF;iPZVIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJeyB3N{jUJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCDVGDsbZRmKGy3bXnu[ZNk\W6lZTDhd5NigSCLQ{WwQVEvPyEQvF2= M4HtVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkO3NVk2Lz5{NEKzO|E6PTxxYU6=
HER218 NVfyU2JvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1HIb|k3KGh? NUO3d|RHT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEWUMkG4JINmdGy|IHHmeIVzKDl4IHjyd{BjgSCDVGDsbZRmKGy3bXnu[ZNk\W6lZTDhd5NigSCLQ{WwQVAvPjF{IN88US=> NFn5Xmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKzO|E6PSd-MkSyN|cyQTV:L3G+
HCT116 NVfIPHVGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGrqbXk6PiCq MWDHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JGFVWGyrdHWgcJVucW6nc3PlcoNmKGG|c3H5JGlEPTB;MD62NVQh|ryP NHfmWFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKzO|E6PSd-MkSyN|cyQTV:L3G+
BT20 NUHaVmxyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1vKUVk3KGh? Ml\5S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gRnQzOCClZXzsd{Bi\nSncjC5OkBpenNiYomgRXRRdGm2ZTDseY1qdmW|Y3XuZ4Uh[XO|YYmgTWM2OD1yLkS4PUDPxE1? NHHSU2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKzO|E6PSd-MkSyN|cyQTV:L3G+
BT549 MmPIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M13jOVk3KGh? MoriS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gRnQ2PDliY3XscJMh[W[2ZYKgPVYhcHK|IHL5JGFVWGyrdHWgcJVucW6nc3PlcoNmKGG|c3H5JGlEPTB;MT6wNUDPxE1? NX3JelFVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyN|cyQTVpPkK0NlM4OTl3PD;hQi=>
AN3CA M2LaV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXTJ[po5QTZiaB?= NXHyToFDT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSU5|Q1GgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KEGWUHzpeIUhdHWvaX7ld4NmdmOnIHHzd4F6KEmFNUC9NE4{PTZizszN NHjV[289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKzO|E6PSd-MkSyN|cyQTV:L3G+
HCT116 MX7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M2TGXlk3KGi{cx?= MmLIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgc5Zmei2neIDy[ZN{cW6pIFzTSFEh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IH3lZZN2emWmIHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkOzJO69VS5? NFrzTIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WyOFMxQSd-Mke1NlQ{ODl:L3G+
MCF7 MnfCRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NIO2ZpM4OiCqcoO= MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEyVREGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjR2IN88UU4> NVjSXWVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NlQ{ODlpPkK3OVI1OzB7PD;hQi=>
DU145 NWrMNmN{SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NVPaWGF{QTZiaILz M1fNWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRGWxOFUh[2WubIOgc5Zmei2neIDy[ZN{cW6pIFzTSFEh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IH3lZZN2emWmIHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLk[yJO69VS5? M1OydFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUK0N|A6Lz5{N{WyOFMxQTxxYU6=
HCT116 MnSxRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MoK4O|IhcHK| MmDvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgc5Zmei2neIDy[ZN{cW6pIFzTSFEh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IH3lZZN2emWmIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLk[1JO69VS5? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV{NEOwPUc,Ojd3MkSzNFk9N2F-
MDA-MB-231 NEG0bY5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4XtWVk3KGi{cx?= MorTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KG:4ZYKt[ZhxemW|c3nu[{BNW0RzIHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBu\WG|dYLl[EBi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE44PSEQvF2u MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV{NEOwPUc,Ojd3MkSzNFk9N2F-
A2780 NFqwRnBCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVS5OkBpenN? MnzhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczDveoVzNWW6cILld5NqdmdiTGPENUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHlibXXhd5Vz\WRiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwN{eg{txONg>? NUXxS4Q1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NlQ{ODlpPkK3OVI1OzB7PD;hQi=>
A549 M4DYfWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MYS5OkBpenN? MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEyVREGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KG2nYYP1doVlKGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjh|IN88UU4> M{jOUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUK0N|A6Lz5{N{WyOFMxQTxxYU6=
MDA-MB-231 NHSzem5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFT5R2M4OiCqcoO= NV\ub5Y5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IH;2[ZIu\XiycnXzd4lv\yCOU1SxJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCvZXHzeZJm\CCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOS52IN88UU4> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV{NEOwPUc,Ojd3MkSzNFk9N2F-
NCI-H1299 MkjQRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M{TEb|k3KGi{cx?= MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INVI6QSClZXzsd{BwfmW{LXX4dJJme3OrbnegUHNFOSCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgcYVie3W{ZXSgZYZ1\XJiOU[gbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGuO|Mh|ryPLh?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV{NEOwPUc,Ojd3MkSzNFk9N2F-
A2780 M3TWdmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NEfMUIk4OiCqcoO= NFmyVGZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJI93\XJvZYjwdoV{e2mwZzDMV2QyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDt[YF{fXKnZDDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMj6xOEDPxE1w M3jBPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUK0N|A6Lz5{N{WyOFMxQTxxYU6=
A549 NFzWSW5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Ml3EO|IhcHK| MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEyVREGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAzNjZ7IN88UU4> NF3xV4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WyOFMxQSd-Mke1NlQ{ODl:L3G+
NCI-H1299 MWDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MoOzO|IhcHK| M1rP[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyOjl7IHPlcIx{KG:4ZYKt[ZhxemW|c3nu[{BNW0RzIHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBu\WG|dYLl[EBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gN{4xOSEQvF2u NEjnd4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WyOFMxQSd-Mke1NlQ{ODl:L3G+
PC3 Ml7ORY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? Mk\uPVYhcHK| MljKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEyVREGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KG2nYYP1doVlKGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUA1NjR3IN88UU4> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV{NEOwPUc,Ojd3MkSzNFk9N2F-
SMMC7721 MkGwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MW[5OkBpenN? NInpV5FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPNUWM4PzJzIHPlcIx{KG:4ZYKt[ZhxemW|c3nu[{BNW0RzIHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBu\WG|dYLl[EBi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gOU4{PiEQvF2u M3zPWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUK0N|A6Lz5{N{WyOFMxQTxxYU6=
DU145 MnLYRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXPFWY9pPzJiaILz MlXHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCGVUG0OUBk\WyuczDveoVzNWW6cILld5NqdmdiTGPENUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHlibXXhd5Vz\WRiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDF|LkC4JO69VS5? NHnRO3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WyOFMxQSd-Mke1NlQ{ODl:L3G+
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H460 NYTVUXhKSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M{HPfVQ5KHSxIEeyJIhzew>? M4Dye2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSES2NEBk\WyuczDh[pRmeiB2ODD0c{A4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC52NzFOwG0v NXznc484RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVQxPzZpPkK5O|U1ODd4PD;hQi=>
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In vivo In mice bearing OCI-AML3 xenografts, SP2509 (25 mg/kg i.p.) significantly improved the survival of the mice, while co-treatment with SP2509 and panobinostat exerts superior in vivo activity.

Protocol (from reference)

Kinase Assay:[1]
  • SP2509 activity assays:

    Test compounds are diluted to 20 × the desired test concentration in 100% DMSO and 2.5 μL of the diluted drug sampleis added to a black 384-well plate. The LSD1 enzyme stock is diluted 17-fold with assay buffer and 40 μL of the diluted LSD1 enzyme is added to the appropriate wells. Substrate, consisting of horseradish peroxidase, dimethyl K4 peptide corresponding to the first 21 amino acids of the N-terminal tail of histone H3, and 10-acetyl-3,7-dihydroxyphenoxazine is then added to wells. Resorufin is analyzed on an Envision plate reader with an excitation wavelength of 530 nm and an emission wavelength of 595 nm. The activity of SP2509 on the other oxidases is determined by using commercially available kits. The glucose oxidase activity (which also noncovalently binds FAD in an elongate conformation), is determined using the glucose oxidase kit. The MAO assays are performed using the MAO-glo kit with MAO-A and MAO-B.

Cell Research:[1]
  • Cell lines: OCI-AML3, MV4-11 and MOLM13 cells
  • Concentrations: ~10 μM
  • Incubation Time: 96 hours
  • Method: Cultured AML cells are treated with SP2509 and/or PS for 96 h. At the end of treatment, cells are washed free of the drugs and 500 cells per condition are plated in methylcellulose and incubated at 37 °C. Colony formation is measured 7–10 days after plating.
Animal Research:[1]
  • Animal Models: NOD/SCID mice bearing OCI-AML3 xenografts
  • Dosages: 20% Cremaphor, 20% DMSO, 60% sterile water
  • Administration: i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
10% DMSO+corn oil
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 437.90
Formula

C19H20ClN3O5S

CAS No. 1423715-09-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=NNC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCOCC2)C3=C(C=CC(=C3)Cl)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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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