NSC 23766

For research use only.

Catalog No.S8031

70 publications

NSC 23766 Chemical Structure

CAS No. 1177865-17-6

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.

Selleck's NSC 23766 has been cited by 70 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 M4XJR2Z2dmO2aX;uJGF{e2G7 NUC1dFJsPTBizszN MV[yOEBp NFOxWlVqdmirYnn0d{BO[XS{aXflcEBqdn[jc3nvci=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ{MkOwPEc,OTd4MkKzNFg9N2F-
RA3 NWPuN3M{TnWwY4Tpc44hSXO|YYm= NYHW[5NQPTBizszN NGHUXoczPCCq MVPpcohq[mm2czDNZZRzcWenbDDpcpZie2mxbh?= M4DaflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NkKyN|A5Lz5zN{[yNlMxQDxxYU6=
RA2 M1zjVmZ2dmO2aX;uJGF{e2G7 NWm4WXR5PTBizszN M1T2NVI1KGh? NGXRZY5qdmirYnn0d{BO[XS{aXflcEBqdn[jc3nvci=> NGPlOWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[yNlMxQCd-MUe2NlI{ODh:L3G+
RA1 MkS2SpVv[3Srb36gRZN{[Xl? MlTwOVAh|ryP NU\OWXluOjRiaB?= NWL0cIZkcW6qaXLpeJMhVWG2cnnn[YwhcW64YYPpc44> NGrJS5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[yNlMxQCd-MUe2NlI{ODh:L3G+
RA-FLS (RA2)  NW\jR2NJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDVV2FmOjVxNUCg{txO MlHiNU06KGR? M1H5eolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboSgcYFvdmW{ M3PNOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NkKyN|A5Lz5zN{[yNlMxQDxxYU6=
IEC-6  MUHGeY5kfGmxbjDBd5NigQ>? NWLmdHhsOTJyINM1US=> M33BZlQwPi96IHi= MW\wdoV3\W62czD0bIUhcW6lcnXhd4VlKGGldHn2ZZRqd25ib3[gSmFMKGG2IE[gZY5lKDhiaB?= NVfQOVVVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0OFg1PjFpPkKwOFQ5PDZzPD;hQi=>
MDA-MB-231  NWj2Vnd3TnWwY4Tpc44hSXO|YYm= M1fmPFUxNzFyMDFOwG0> NW\HN5VCPDhiaB?= MVjpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiZHXjdoVie2ViaX6gdIhwe3Cqb4L5cIF1cW:wIH;mJJA3PSC|dXL1col1 MlPtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3MUW5OFAoRjJyNUG1PVQxRC:jPh?=
MDA-MB-468 NGfpPWVHfW6ldHnvckBCe3OjeR?= MV21NE8yODBizszN NHTBS4U1QCCq MYnpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiZHXjdoVie2ViaX6gdIhwe3Cqb4L5cIF1cW:wIH;mJJA3PSC|dXL1col1 NV7OUlkyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDBpPkKwOVE2QTRyPD;hQi=>
MDA-MB-231  NGW1dpdHfW6ldHnvckBCe3OjeR?= NIL0b3A2OC9zMECg{txO MXGyOEBp NGfiWJVqdmO{ZXHz[ZMheGixc4Doc5J6dGG2aX;uJI9nKEqQSzDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M1TpR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQxLz5{MEWxOVk1ODxxYU6=
MDA-MB-468 NHrV[HBHfW6ldHnvckBCe3OjeR?= MX61NE8yODBizszN NWDBSYQ6OjRiaB?= NY[5bIROcW6lcnXhd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCMTlugbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NHfER|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1OCd-MkC1NVU6PDB:L3G+
MDA-MB-468 M2nQ[GZ2dmO2aX;uJGF{e2G7 NEnGZ5EyODBizszN NGXM[GYzPCCq M2DzUIlvcGmkaYTzxsBk[XOyYYPlMVMh[WO2aY\heIlwdsLi MmO4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3MUW5OFAoRjJyNUG1PVQxRC:jPh?=
MDA-MB-468 MkDCRZBweHSxc3nzJGF{e2G7 M2\lfFUxNzFyMDFOwG0> MkTPNlQhcA>? MmC1bY5lfWOnczDhdI9xfG:|aYO= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0NEc,OjB3MUW5OFA9N2F-
T47D NUPPSZFHTnWwY4Tpc44hSXO|YYm= NUG0OmlSOTByIN88US=> MVq0PEBp MULpcoNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IHnuJGcyyqCyaHHz[UBidmRiZHXjdoVie2W|IITo[UBk\WyuIH71cYJmeiCrbjDTJIFv\CCJMj3NJJBp[XOnc9Mg MmjLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3MUW5OFAoRjJyNUG1PVQxRC:jPh?=
MCF7 MYPGeY5kfGmxbjDBd5NigQ>? Mm\mNVAxKM7:TR?= MXS0PEBp NXO1[GNncW6lcnXhd4V{KHSqZTDj[YxtKG63bXLldkBqdiCJMdMgdIhie2ViYX7kJIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgbY4hWyCjbnSgS|IuVSCyaHHz[ZPDqA>? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0NEc,OjB3MUW5OFA9N2F-
MDA-MB-231  M4PzfGZ2dmO2aX;uJGF{e2G7 NUPESIs{OTByIN88US=> NHnheHM1QCCq NHTFWIpqdmO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJIlvKEdzwrDwbIF{\SCjbnSg[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDpckBUKGGwZDDHNk1OKHCqYYPld:Kh NGDyOYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1OCd-MkC1NVU6PDB:L3G+
MDA-MB-231 NWPJXoFLTnWwY4Tpc44hSXO|YYm= M1PGXFAuOTByIN88US=> NFfuR5MzPCCq M4HDOpNmdGWldHn2[Yx6KGmwaHnibZR{KFKjY{GgZYN1cX[jdHnvckB4cXSqb4X0JIlvfGW{ZnXybY5oKHerdHigeIhmKGGldHn2bZR6KG:oIITo[UBkdG:|ZXz5JJJmdGG2ZXSgd41idGxiR2TQZZNmKEOmY{Sy M3riSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQxLz5{MEWxOVk1ODxxYU6=
MDA-MB-231 NESwdnFEgXSxdH;4bYNqfHliQYPzZZk> NFTYNG0xNTFyMDFOwG0> NFjjRpc1QCCq NFPaW2Jl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M1HHU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQxLz5{MEWxOVk1ODxxYU6=
MDA-MB-468 NWnpT3dMS3m2b4TvfIlkcXS7IFHzd4F6 NHPLdGgxNTFyMDFOwG0> MmTSOFghcA>? MnnX[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0NEc,OjB3MUW5OFA9N2F-
T47D M1vON2N6fG:2b4jpZ4l1gSCDc4PhfS=> MV:wMVExOCEQvF2= NEG0Z3k1QCCq NXjNc|Vb\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NUjPfFd3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDBpPkKwOVE2QTRyPD;hQi=>
MCF7 MnvuR5l1d3SxeHnjbZR6KEG|c3H5 M4nZSlAuOTByIN88US=> NWrRN5lSPDhiaB?= MkX4[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NVTRRo1{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDBpPkKwOVE2QTRyPD;hQi=>
SKBR3-pMKO.1 NF3rZnlHfW6ldHnvckBCe3OjeR?= M1\nXVUxKM7:TR?= MWGyOEBp M33DV4lvcGmkaYTzJHJi[zFiYXP0bZZifGmxbh?= M1robVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUSzPFI2Lz5{MUm0N|gzPTxxYU6=
SKBR3 M3v3NWZ2dmO2aX;uJGF{e2G7 MUC1NEDPxE1? MoT0NlQhcA>? NH;2[HRqdmirYnn0d{BT[WNzIHHjeIl3[XSrb36= NIXEZmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm0N|gzPSd-MkG5OFM5OjV:L3G+
NCI-H1703 NVLzcVVrTnWwY4Tpc44hSXO|YYm= NGjxNmUxNTVyMDFOwG0> NWDwfmZOOjRiaB?= MmTR[IlucW6rc3jld{Bj[XOjbDDOSk3PwkJiYXP0bZZqfHliZH;z[UBl\XCnbnTlcpRtgcLi NXrXTYhDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFkyPjBpPkKyOVQ6OTZyPD;hQi=>
NCI-H1703 NVjH[2llTnWwY4Tpc44hSXO|YYm= MoHyNVAxKM7:Zz;tcC=> NU\qWVV7OjRiaB?= MXLzcI94eyCycn;ndoV{e2mxbjD0bJJwfWeqIITo[UBIOcLicHjhd4Uhd2ZidHjlJINmdGxiY4njcIU> NYD2Om9bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFkyPjBpPkKyOVQ6OTZyPD;hQi=>
NCI-H1703 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnHTYIxNTVyMDFOwG0> M1nLelI1KGh? NIrubJdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M3\rXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUS5NVYxLz5{MkW0PVE3ODxxYU6=
T98MG M{XKXGZ2dmO2aX;uJGF{e2G7 MYK1NEBuVQ>? Mlq3NlQhcA>? NXrleJFPTE2VTx?= M1TCWYVvcGGwY3XzJJRp\SCjboTpcYloemG2b4L5JIVn\mWldDDv[kBmemyxdHnubYI> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh|MkGyNEc,OjN6M{KxNlA9N2F-
A172MG Mnf4SpVv[3Srb36gRZN{[Xl? NGrkbng2OCCvTR?= Mny0NlQhcA>? MoXhSG1UVw>? MlLy[Y5p[W6lZYOgeIhmKGGwdHntbYdz[XSxcomg[YZn\WO2IH;mJIVzdG:2aX7pZi=> MkjpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6M{KxNlAoRjJ|OEOyNVIxRC:jPh?=
U87MG NETWSHVHfW6ldHnvckBCe3OjeR?= NIjD[XQ2OCCvTR?= MljENlQhcA>? MkTlSG1UVw>? MlL5[Y5p[W6lZYOgeIhmKGGwdHntbYdz[XSxcomg[YZn\WO2IH;mJIVzdG:2aX7pZi=> NWGyPYJiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4N|IyOjBpPkKzPFMzOTJyPD;hQi=>
PC40 M{LzeGNmdGxiVnnhZoltcXS7IFHzd4F6 M4TPWlUxKG2P NELqeIIyPDRiaB?= MWfEUXNQ NFuwfoNmgGirYnn0d{B{gW6ncnfpd5Rq[yCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5R{KGOxbXLpcoVlKHS{ZXH0cYVvfCC5aYToJIVzdG:2aX7pZuKh MlO0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6M{KxNlAoRjJ|OEOyNVIxRC:jPh?=
PC38 NGnkbFVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MofoOVAhdU1? MlSyNVQ1KGh? MoT0SG1UVw>? M{nPcoV5cGmkaYTzJJN6dmW{Z3nzeIlkKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMh[2:vYnnu[YQhfHKnYYTt[Y51KHerdHig[ZJtd3SrbnnixsA> M4Lk[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEOyNVIxLz5{M{izNlEzODxxYU6=
T98MG NXXaVItLS2WubDDWbYFjcWyrdImgRZN{[Xl? MVy1NEBuVQ>? MlXVNVQ1KGh? NIrqUmVFVVOR Mm[0[ZhpcWKrdIOgd5lv\XKpaYP0bYMh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{Bkd22kaX7l[EB1emWjdH3lcpQhf2m2aDDldoxwfGmwaXNCpC=> NUfWWppPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4N|IyOjBpPkKzPFMzOTJyPD;hQi=>
A172MG MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmPBOVAhdU1? M3zYSFE1PCCq NEftNm5FVVOR NIDBTXBmgGirYnn0d{B{gW6ncnfpd5Rq[yCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5R{KGOxbXLpcoVlKHS{ZXH0cYVvfCC5aYToJIVzdG:2aX7pZuKh MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh|MkGyNEc,OjN6M{KxNlA9N2F-
U87MG NYXoelhbS2WubDDWbYFjcWyrdImgRZN{[Xl? Mlz6OVAhdU1? NY[ydo5zOTR2IHi= MWXEUXNQ NXHPN2pk\XiqaXLpeJMhe3mwZYLnbZN1cWNiYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyClb33ibY5m\CC2cnXheI1mdnRid3n0bEBmemyxdHnubYLDqA>? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh|MkGyNEc,OjN6M{KxNlA9N2F-
Ki-67+ CLL MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;NSVdbPTBiwsXN M3jBcVUh\A>? NUjKfVNv\GWlcnXhd4V{KHSqZTDueY1j\XJib3[gT4kuPjdtwrDDUGwh[2WubIO= MkXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3MEGyNVcoRjJ2NUCxNlE4RC:jPh?=
NIH3T3  MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjNXm1WOTByIN88US=> MmnnNlTDqGh? M{DaU4hieyCwbzDzbYdvcW[rY3HueEBqdXCjY4Sgc44h[2WubDD2bYFjcWyrdIm= NHvOSZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCzO|A3OCd-MkWwN|cxPjB:L3G+
U2-OS Mo\BSpVv[3Srb36gRZN{[Xl? NWXq[Zd2OTByIN88US=> NXPxRmZDOjRiaB?= NX;uXYVOTE2VTx?= M{Xv[olv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hfGinIFexJJBp[XOnwrC= M{PMWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUC5N|I4Lz5{NUGwPVMzPzxxYU6=
SW480  MoXBSpVv[3Srb36gRZN{[Xl? M4W0TVExOCEQvF2= MYmyOEBp MlnNSG1UVw>? M2rGWYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hfGinIFexJJBp[XOnwrC= NUC3SmJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNFk{OjdpPkK1NVA6OzJ5PD;hQi=>
A431 MV7GeY5kfGmxbjDBd5NigQ>? M2rIbFExOCEQvF2= NUnSVWRwOjRiaB?= MkfOSG1UVw>? MWrpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJJRp\SCJMTDwbIF{\cLi NXrGe|JkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNFk{OjdpPkK1NVA6OzJ5PD;hQi=>
U2-OS M2jmRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrtXIMyODBizszN NULhTm1yOjRxNEivO|IhcA>? MlrCbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> NGrucZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGwPVMzPyd-MkWxNFk{Ojd:L3G+
SW480  NYq1foIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvFfpI3OTByIN88US=> NVfYRoF3OjRxNEivO|IhcA>? Mli1bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> M17PNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUC5N|I4Lz5{NUGwPVMzPzxxYU6=
A431 M4Lh[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzER5FkOTByIN88US=> NXLJU4ttOjRxNEivO|IhcA>? NWjob|M3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUB1cW2nIHTldIVv\GWwdDDtZY5v\XJ? M2DHS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUC5N|I4Lz5{NUGwPVMzPzxxYU6=
RBMECs NXzNbZp2TnWwY4Tpc44hSXO|YYm= NFTmNpAyODBizszNxsA> MlP0N|DDqG2rbh?= M37yOIJtd2OtZYOgOmJvgi2lQV3QMY1m\GmjdHXkJIFkfGm4YYTpc44hd2ZiUnHjNUBqdiCHTVHQMWlKNXS{ZXH0[YQhWkKPRVPz M{HsXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{W4NFM6Lz5{NkO1PFA{QTxxYU6=
human aortic smooth muscle cells MV7GeY5kfGmxbjDBd5NigQ>? NX;wVWo4PTBidV2= Mly4TY5pcWKrdHnvckBw\iCUYXOxJIJqdmSrbnegeI8hWGGtMTDpckBpfW2jbjDhc5J1cWNic33vc5RpKG23c3Ps[UBk\WyuczDheEA2OCC3TTDifUBUTFNvUFHHSUBj[XOnZDDjbIVucWy3bXnu[ZNk\W6lZR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV{N{CzNkc,OTl3MkewN|I9N2F-
human aortic smooth muscle cells MkfWSpVv[3Srb36gRZN{[Xl? NUTZV2JOOTByIN88US=> MljYTY5pcWKrdHnvckBw\iCUYXOxJIJqdmSrbnegeI8hWGGtMTDpckBpfW2jbjDhc5J1cWNic33vc5RpKG23c3Ps[UBk\WyuczDheEAyODBidV2gZpkhW0SVLWDBS2Uh[mG|ZXSgZ4hmdWmudX3pcoV{[2WwY3W= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV{N{CzNkc,OTl3MkewN|I9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pCREB / CREB; 

PubMed: 25319697     


Rac1 inhibitor NSC23766 decreases CREB phosphorylation at serine 133 (pCREB) in cortical neurons. Left, Temporal profiles of NSC23766 (100 μm) on basal pCREB levels. Right, Dose–response effects of NSC23766 (30 min) application on pCREB. 

OCT4 / SOX2 / Nanog ; 

PubMed: 31338333     


Down-regulation of Rac1-GTP treated with NSC23766 decreased expression of Nanog, Sox2, and Oct4 levels in TUFT1—MDA-MB-231 and TUFT1—HCC1937 cells (n = 3). 

active Rac1 / Rac1 ; 

PubMed: 31338333     


Western blot showed effect of Rac1 inhibitor NSC23766 on Rac1-GTP in MDA-MB-231 cells (n = 3). 

25319697 31338333
Immunofluorescence
IP3K-A / F-actin; 

PubMed: 19890013     


Rac1-specific inhibitor NSC23766 gradually blocked the IP3K-A expression-induced formation of filopodia in HeLa cells. Following transfection of GFP-IP3K-A, HeLa cells were incubated for 24 hrs in medium containing the Rac1 inhibitor. Treatment with 40 µM䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙

BART / Rac1; 

PubMed: 22745590     


S2-013 cells were pretreated with or without the Rac1 inhibitor (NSC23766) and were immunocytochemically stained using anti-BART (green) and anti-Rac1 (red) antibodies. Arrows indicate colocalized BART and Rac1 in lamellipodial-like protrusions; blue, DAP䲧疝Ỵ疞㧀疜膉痘 

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

Kinase Assay:[1]
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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]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (188.33 mM)
Water 100 mg/mL warmed (188.33 mM)
Ethanol Insoluble

* 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 530.96
Formula

C24H35N7.3HCl

CAS No. 1177865-17-6
Storage powder
in solvent
Synonyms N/A
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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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID