NSC 23766

Catalog No.S8031

For research use only.

NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.

NSC 23766 Chemical Structure

CAS No. 1177865-17-6

Selleck's NSC 23766 has been cited by 78 publications

Purity & Quality Control

Choose Selective Rho Inhibitors

Biological Activity

Description NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.
Targets
Rac GTPase [1]
(Cell-free assay)
50 μM
In vitro

NSC23766 is identified to fit into a surface groove of Rac1 known to be critical for GEF specification. NSC23766 effectively inhibits Rac1 binding and activation by the Rac-specific GEF Trio or Tiam1 in a dose-dependent manner without interfering with the closely related Cdc42 or RhoA binding or activation by their respective GEFs or with Rac1 interaction with BcrGAP or effector PAK1. [1] NSC 23766 is active in regulating Rac GTPase functions on cytoskeleton and many cell functions including cell cycle, cell growth, adhesion, migration and gene transcription. NSC 23766 (50 μM) potently blocks serum or platelet-derived growth factor-induced Rac1 activation and lamellipodia formation without affecting the activity of endogenous Cdc42 or RhoA in NIH 3T3 cells. NSC 23766 reduces Trio or Tiam1 but not Vav, Lbc, Intersectin, or a constitutively active Rac1 mutant-stimulated NIH 3T3 cells growth and suppresses Trio, Tiam1, or Ras-induced cell transformation. NSC23766 dose-dependently inhibits PC-3 cells proliferation and anchorage-independent growth. 25 μM NSC23766 inhibits the PC-3 cell invasion through Matrigel by 85%. [1] 50 μM NSC 23766 inhibits thrombin-induced activation of Rac1 an d Rac2 in human platelets, as well as platelet aggregation. [2] NSC23766 prevents Aβ40 and Aβ42 production in swAPP-HEK293cells without affecting Notch and sAPPα. NSC23766 prevents γ-secretase activity in cell, but not act as a direct γ-secretase inhibitor. NSC23766 dose-dependently reduces levels of secreted and intracellular Aβ40 with IC50 of 48.94 μM. 50 μM NSC 23766 inhibits release of Aβ42 by 57.97%. [3] NSC23766 regulates endothelial nitric oxide synthase expression and endothelial function. 100 μM NSC23766 represses the eNOS promoter activity by 60% in bovine aortic ECs and by 30% to 35% in bEND.3 cells. Inhibition of Rac1 with NSC23766 destabilizes eNOS mRNA and shortens its half-life to 17 hours. NSC23766 dose-dependently attenuates ACh-induced relaxation of wild-type mice aortic rings. [4] NSC23766 inhibits cell growth and induces apoptosis. NSC23766 decreases MDA-MB-468 and MDA-MB-231 cells viability in a dose-dependent manner with IC50 of ~10 μM, which is not correlated with the status of estrogen receptor (ER), progesterone receptor (PR), Her2, and p53 mutation. NSC23766 has little effect on the survival of the MCF12A normal mammary epithelial cells. After 24 hours expose to NSC 23766, MDA-MB-231 cells showes an increase from 41% to 65% in G1 phase and a concomitant decrease in S and G2-M phases. 100 μM NSC23766 induces a six-fold increase of apoptotic MDA-MB-468. The inhibition of NSC23766 on cell cycle arrest or apoptosis in breast cancer cells is mediated by downregulation of cyclin D1, survivin, and X-linked inhibitor of protein apoptosis. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RA4 NF3nc2dHfW6ldHnvckBCe3OjeR?= NWi2[3loPTBizszN NVXNeJZsOjRiaB?= MnrnbY5pcWKrdIOgUYF1emmpZXygbY53[XOrb36= NELKWIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[yNlMxQCd-MUe2NlI{ODh:L3G+
RA3 NGfXToxHfW6ldHnvckBCe3OjeR?= M4TDZlUxKM7:TR?= M4LldFI1KGh? MWnpcohq[mm2czDNZZRzcWenbDDpcpZie2mxbh?= M3TmVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NkKyN|A5Lz5zN{[yNlMxQDxxYU6=
RA2 MlvUSpVv[3Srb36gRZN{[Xl? M2DYZ|UxKM7:TR?= MljKNlQhcA>? MYTpcohq[mm2czDNZZRzcWenbDDpcpZie2mxbh?= M{G5[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NkKyN|A5Lz5zN{[yNlMxQDxxYU6=
RA1 MnX5SpVv[3Srb36gRZN{[Xl? MXK1NEDPxE1? MUSyOEBp M4q1e4lvcGmkaYTzJG1ifHKrZ3XsJIlvfmG|aX;u MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ{MkOwPEc,OTd4MkKzNFg9N2F-
RA-FLS (RA2)  NWGwW4N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HQVVI2NzVyIN88US=> NUjrUplQOS17IHS= NEC5d|FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70JI1idm6nch?= M2XUPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NkKyN|A5Lz5zN{[yNlMxQDxxYU6=
IEC-6  M{DOU2Z2dmO2aX;uJGF{e2G7 NEDwOmUyOjBiwsXN MUW0M|YwQCCq MmDEdJJmfmWwdIOgeIhmKGmwY4LlZZNm\CCjY4TpeoF1cW:wIH;mJGZCUyCjdDC2JIFv\CB6IHi= NGLjbFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MES0PFQ3OSd-MkC0OFg1PjF:L3G+
MDA-MB-231  MULGeY5kfGmxbjDBd5NigQ>? NF7Ld2o2OC9zMECg{txO MWq0PEBp NYL1W|N4cW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHnvckBw\iCyNkWgd5VjfW6rdB?= NHrLeZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1OCd-MkC1NVU6PDB:L3G+
MDA-MB-468 NVXD[WIzTnWwY4Tpc44hSXO|YYm= M3fHPFUxNzFyMDFOwG0> M{nxOlQ5KGh? MUfpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiZHXjdoVie2ViaX6gdIhwe3Cqb4L5cIF1cW:wIH;mJJA3PSC|dXL1col1 NG\HcmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1OCd-MkC1NVU6PDB:L3G+
MDA-MB-231  M1LIbWZ2dmO2aX;uJGF{e2G7 MnjXOVAwOTByIN88US=> NFvwNIYzPCCq MUfpcoNz\WG|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGpPUyCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M2nZfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQxLz5{MEWxOVk1ODxxYU6=
MDA-MB-468 M1jZSGZ2dmO2aX;uJGF{e2G7 NVzQUGg{PTBxMUCwJO69VQ>? MVuyOEBp NXf6W5o3cW6lcnXhd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCMTlugbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0NEc,OjB3MUW5OFA9N2F-
MDA-MB-468 Mn3MSpVv[3Srb36gRZN{[Xl? M2DL[|ExOCEQvF2= MlHvNlQhcA>? M2DDSIlvcGmkaYTzxsBk[XOyYYPlMVMh[WO2aY\heIlwdsLi M{frRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQxLz5{MEWxOVk1ODxxYU6=
MDA-MB-468 MkfHRZBweHSxc3nzJGF{e2G7 M1nHZlUxNzFyMDFOwG0> M1zPO|I1KGh? MX3pcoR2[2W|IHHwc5B1d3Orcx?= NWDzfVBjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDBpPkKwOVE2QTRyPD;hQi=>
T47D M3K5TWZ2dmO2aX;uJGF{e2G7 NH64U4QyODBizszN NFXJdJc1QCCq NEO5c|lqdmO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJIlvKEdzwrDwbIF{\SCjbnSg[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDpckBUKGGwZDDHNk1OKHCqYYPld:Kh NUDtSpJbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDBpPkKwOVE2QTRyPD;hQi=>
MCF7 MXPGeY5kfGmxbjDBd5NigQ>? MXGxNFAh|ryP MVm0PEBp NXvp[5Z7cW6lcnXhd4V{KHSqZTDj[YxtKG63bXLldkBqdiCJMdMgdIhie2ViYX7kJIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgbY4hWyCjbnSgS|IuVSCyaHHz[ZPDqA>? NIXsWWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1OCd-MkC1NVU6PDB:L3G+
MDA-MB-231  Ml74SpVv[3Srb36gRZN{[Xl? NHfzdpUyODBizszN MonjOFghcA>? MlLCbY5kemWjc3XzJJRp\SClZXzsJI52dWKncjDpckBIOcLicHjhd4Uh[W6mIHTlZ5Jm[XOnczD0bIUh[2WubDDueY1j\XJiaX6gV{BidmRiR{KtUUBxcGG|ZYRCpC=> NHvNdoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1OCd-MkC1NVU6PDB:L3G+
MDA-MB-231 MlzKSpVv[3Srb36gRZN{[Xl? NInPR4wxNTFyMDFOwG0> NXi1V2RmOjRiaB?= MUHz[Yxm[3SrdnXsfUBqdmirYnn0d{BT[WNzIHHjeIl3[XSrb36ge4l1cG:3dDDpcpRmem[ncnnu[{B4cXSqIITo[UBi[3Srdnn0fUBw\iC2aHWgZ4xwe2WueTDy[YxifGWmIIPtZYxtKEeWUHHz[UBE\GN2Mh?= NV;FcpZyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDBpPkKwOVE2QTRyPD;hQi=>
MDA-MB-231 MWTDfZRwfG:6aXPpeJkhSXO|YYm= M{DrfFAuOTByIN88US=> NEXrO|I1QCCq NHX5ZZhl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M1Pqb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQxLz5{MEWxOVk1ODxxYU6=
MDA-MB-468 NX;JR4pQS3m2b4TvfIlkcXS7IFHzd4F6 NHvxfWMxNTFyMDFOwG0> NHO1PYw1QCCq Mo\p[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M4fkTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQxLz5{MEWxOVk1ODxxYU6=
T47D NXLzeFl7S3m2b4TvfIlkcXS7IFHzd4F6 MVewMVExOCEQvF2= M2XNXFQ5KGh? MV;k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NXnQXJhmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDBpPkKwOVE2QTRyPD;hQi=>
MCF7 MYXDfZRwfG:6aXPpeJkhSXO|YYm= MXKwMVExOCEQvF2= NEfk[4U1QCCq Mlq2[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M2jzPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQxLz5{MEWxOVk1ODxxYU6=
SKBR3-pMKO.1 Mmq1SpVv[3Srb36gRZN{[Xl? NYDGfmNQPTBizszN Ml;RNlQhcA>? NHflR4ZqdmirYnn0d{BT[WNzIHHjeIl3[XSrb36= Ml7pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NEO4NlUoRjJzOUSzPFI2RC:jPh?=
SKBR3 M3L1SmZ2dmO2aX;uJGF{e2G7 NI\EelE2OCEQvF2= NVTqVZBHOjRiaB?= MUHpcohq[mm2czDSZYMyKGGldHn2ZZRqd25? NGT4OWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm0N|gzPSd-MkG5OFM5OjV:L3G+
NCI-H1703 MWrGeY5kfGmxbjDBd5NigQ>? MlzQNE02ODBizszN MU[yOEBp MVjkbY1qdmm|aHXzJIJie2GuIF7GMe67SiCjY4Tpeol1gSCmb4PlJIRmeGWwZHXueIx6yqB? M2rUOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUS5NVYxLz5{MkW0PVE3ODxxYU6=
NCI-H1703 NWDOZ2VpTnWwY4Tpc44hSXO|YYm= MlHhNVAxKM7:Zz;tcC=> NGHNZY4zPCCq MX7zcI94eyCycn;ndoV{e2mxbjD0bJJwfWeqIITo[UBIOcLicHjhd4Uhd2ZidHjlJINmdGxiY4njcIU> NFPtd4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW0PVE3OCd-MkK1OFkyPjB:L3G+
NCI-H1703 NYHQb41ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXewMVUxOCEQvF2= MlzKNlQhcA>? NFeySWpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NEfDVnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW0PVE3OCd-MkK1OFkyPjB:L3G+
T98MG M1:wWGZ2dmO2aX;uJGF{e2G7 MX:1NEBuVQ>? NVHNRllwOjRiaB?= MmjaSG1UVw>? NH\5UYZmdmijbnPld{B1cGViYX70bY1q\3KjdH;yfUBm\m[nY4Sgc4Yh\XKub4Tpcolj M1jCTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEOyNVIxLz5{M{izNlEzODxxYU6=
A172MG NF23ZXFHfW6ldHnvckBCe3OjeR?= M3WxWVUxKG2P NVrGclBEOjRiaB?= MYTEUXNQ Ml3C[Y5p[W6lZYOgeIhmKGGwdHntbYdz[XSxcomg[YZn\WO2IH;mJIVzdG:2aX7pZi=> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh|MkGyNEc,OjN6M{KxNlA9N2F-
U87MG NVrON2NnTnWwY4Tpc44hSXO|YYm= M2DSPFUxKG2P M4fVUlI1KGh? NGrjS3dFVVOR NHjVcWFmdmijbnPld{B1cGViYX70bY1q\3KjdH;yfUBm\m[nY4Sgc4Yh\XKub4Tpcolj NGfMOYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{izNlEzOCd-MkO4N|IyOjB:L3G+
PC40 M1T4WWNmdGxiVnnhZoltcXS7IFHzd4F6 MVW1NEBuVQ>? NY\XVFE1OTR2IHi= M1vFUWROW09? NX[yfHVQ\XiqaXLpeJMhe3mwZYLnbZN1cWNiYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyClb33ibY5m\CC2cnXheI1mdnRid3n0bEBmemyxdHnubYLDqA>? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh|MkGyNEc,OjN6M{KxNlA9N2F-
PC38 M4rzPWNmdGxiVnnhZoltcXS7IFHzd4F6 M1n3WVUxKG2P M3zNPVE1PCCq NIDINpRFVVOR M3rySYV5cGmkaYTzJJN6dmW{Z3nzeIlkKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMh[2:vYnnu[YQhfHKnYYTt[Y51KHerdHig[ZJtd3SrbnnixsA> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh|MkGyNEc,OjN6M{KxNlA9N2F-
T98MG NEjsbHZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIryU|U2OCCvTR?= MmfLNVQ1KGh? M1zHXmROW09? MnLh[ZhpcWKrdIOgd5lv\XKpaYP0bYMh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{Bkd22kaX7l[EB1emWjdH3lcpQhf2m2aDDldoxwfGmwaXNCpC=> M2TIfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEOyNVIxLz5{M{izNlEzODxxYU6=
A172MG NGfZU|dE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFf5S3A2OCCvTR?= MYKxOFQhcA>? M2LtW2ROW09? MUDlfIhq[mm2czDzfY5memerc4TpZ{BidnSrcILvcIln\XKjdHn2[UBm\m[nY4TzJINwdWKrbnXkJJRz\WG2bXXueEB4cXSqIHXycI91cW6rYtMg M3LkeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEOyNVIxLz5{M{izNlEzODxxYU6=
U87MG MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYq1NEBuVQ>? MXKxOFQhcA>? NFHUNXhFVVOR NYOy[5kx\XiqaXLpeJMhe3mwZYLnbZN1cWNiYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyClb33ibY5m\CC2cnXheI1mdnRid3n0bEBmemyxdHnubYLDqA>? Mn7rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6M{KxNlAoRjJ|OEOyNVIxRC:jPh?=
Ki-67+ CLL Mmj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjNS4I2OCEEtV2= NYnv[5RiPSCm MVHk[YNz\WG|ZYOgeIhmKG63bXLldkBw\iCNaT22O{vDqEOOTDDj[Yxtew>? NVjpVYg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NFEzOTdpPkK0OVAyOjF5PD;hQi=>
NIH3T3  NIG5VGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYixNFAh|ryP M{Ll[VI1yqCq NWfueHFZcGG|IH7vJJNq\26rZnnjZY51KGmvcHHjeEBwdiClZXzsJJZq[WKrbHn0fS=> MlTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyM{ewOlAoRjJ3MEO3NFYxRC:jPh?=
U2-OS NHX2SY5HfW6ldHnvckBCe3OjeR?= MnP1NVAxKM7:TR?= NGnQVFAzPCCq NU\GVVI1TE2VTx?= NFrpOJBqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKHSqZTDHNUBxcGG|ZdMg NXzkRndsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNFk{OjdpPkK1NVA6OzJ5PD;hQi=>
SW480  NUG0[pFNTnWwY4Tpc44hSXO|YYm= NYm3NGJtOTByIN88US=> NFz1N2IzPCCq NEPTUYJFVVOR M1jmSolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hfGinIFexJJBp[XOnwrC= Ml;vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMEmzNlcoRjJ3MUC5N|I4RC:jPh?=
A431 NHL1bmZHfW6ldHnvckBCe3OjeR?= MYKxNFAh|ryP NXzXeop2OjRiaB?= NX7Db5p5TE2VTx?= MUfpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJJRp\SCJMTDwbIF{\cLi NIHF[mY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGwPVMzPyd-MkWxNFk{Ojd:L3G+
U2-OS M{DSbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:xNFAh|ryP NIPrUXYzPC92OD:3NkBp NIT6PWdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJJRqdWViZHXw[Y5l\W62IH3hco5meg>? MnXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMEmzNlcoRjJ3MUC5N|I4RC:jPh?=
SW480  MoLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofsNVAxKM7:TR?= M4LOdVI1NzR6L{eyJIg> NEXj[G5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJJRqdWViZHXw[Y5l\W62IH3hco5meg>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTFyOUOyO{c,OjVzMEmzNlc9N2F-
A431 NWjFNXFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHZNVAxKM7:TR?= MkPlNlQwPDhxN{KgbC=> NUHjVJBNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUB1cW2nIHTldIVv\GWwdDDtZY5v\XJ? NV:xRnBsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNFk{OjdpPkK1NVA6OzJ5PD;hQi=>
RBMECs MoD1SpVv[3Srb36gRZN{[Xl? NX7PXmV{OTByIN88UeKh MU[zNOKhdWmw NF\xUW1jdG:la3XzJFZDdnpvY1HNVE1u\WSrYYTl[EBi[3SrdnH0bY9vKG:oIGLhZ|EhcW5iRV3BVE1KUS22cnXheIVlKFKETVXDdy=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3OECzPUc,OjZ|NUiwN|k9N2F-
human aortic smooth muscle cells MUTGeY5kfGmxbjDBd5NigQ>? MmjEOVAhfU1? MVnJcohq[mm2aX;uJI9nKFKjY{GgZolv\GmwZzD0c{BR[WtzIHnuJIh2dWGwIHHvdpRq[yC|bX;veIghdXW|Y3zlJINmdGy|IHH0JFUxKHWPIHL5JHNFWy2SQVfFJIJie2WmIHPo[Y1qdHWvaX7ld4NmdmOn M3Tnc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUK3NFMzLz5zOUWyO|A{OjxxYU6=
human aortic smooth muscle cells NGfzfo5HfW6ldHnvckBCe3OjeR?= M{nTbFExOCEQvF2= M3LLZ2lvcGmkaYTpc44hd2ZiUnHjNUBjcW6maX7nJJRwKFCja{GgbY4hcHWvYX6gZY9zfGmlIIPtc491cCCvdYPjcIUh[2WubIOgZZQhOTByIIXNJIJ6KFOGUz3QRWdGKGKjc3XkJINp\W2rbIXtbY5me2OnbnPl NEL4Xnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUWyO|A{Oid-MUm1NlcxOzJ:L3G+
Assay
Methods Test Index PMID
Western blot pCREB / CREB ; OCT4 / SOX2 / Nanog ; active Rac1 / Rac1 25319697 31338333
Immunofluorescence IP3K-A / F-actin ; BART / Rac1 19890013 22745590
In vivo NSC23766 induces mobilization of hematopoietic stem cells/progenitors. Intraperitoneal administration of NSC23766 (2.5 mg/kg) into the ‘‘poorly mobilizing ’’ C57Bl/6 mouse strain leads to a two-fold increase in circulating hematopoietic stem cells/progenitors 6 hr after injection. [2] NSC23766 alleviates lipopolysaccharide-induced acute pulmonary injury in mice. Treatment with NSC23766 at 1 or 3mg/kg not only reduces the inflammatory cells infiltration and MPO activities, but also inhibits pro-inflammatory mediators, tumor necrosis factor-α and interleukin-1β, mRNA expression. NSC23766 also reduces Evans Blue and albumin accumulation in LPS-challenged lungs. [6]

Protocol (from reference)

Kinase Assay:[1]
  • Rho GTPase activity assay:

    Cells are grown in log phase in a 10-cm dish, and are starved in 0.5% serum medium or indicated otherwise for 24 h before lysis in a buffer containing 20 mM Tris HCl (pH 7.6), 100 mM NaCl, 10 mM MgCl2, 1% Nonidet P-40, 10% glycerol, and 1× protease inhibitor mixture. Lysates are clarified, the protein concentrations are normalized, and the GTP-bound Rac1 in the lysates is measured by an effector domain pull-down assay. For the His6-PAK1 PBD pull-down assay, cell lysates are incubated with Ni2+-agarose-immobilized His6-PAK1 PBD domain (∼1 μg each) purified from E. coli for 30 min. The Ni2+-agarose co-precipitates are washed twice in the wash buffer and analyzed by immunoblotting with anti-Rac1 monoclonal antibody.

Cell Research:[5]
  • Cell lines: Human breast cancer cells MDA-MB-468
  • Concentrations: 0-100 μM
  • Incubation Time: 2 days
  • Method: Cells (1.5 × 104/mL) are seeded in each well of 96-well tissue culture plates with 200 μL of medium. After 24 hours of plating, the medium is replaced with 200 μL of fresh medium containing NSC23766 at the indicated concentrations. At the end of the treatment period 20 μL of MTS solution are added to each well and incubated at 37 ℃ for 2 hours. Absorbance at 490 nm is read on a 96-well plate reader.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 530.96
Formula

C24H35N7.3HCl

CAS No. 1177865-17-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN(CC)CCCC(C)NC1=NC(=CC(=N1)NC2=CC3=C(C=C(N=C3C=C2)C)N)C.Cl.Cl.Cl

In vivo Formulation Calculator (Clear solution)

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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
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Molarity Calculator

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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.

Handling Instructions

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