Go6976

Catalog No.S7119 Synonyms: PD406976

For research use only.

Go6976 (PD406976) is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.

Go6976 Chemical Structure

CAS No. 136194-77-9

Selleck's Go6976 has been cited by 27 publications

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Biological Activity

Description Go6976 (PD406976) is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
Targets
JAK2 [2]
(Cell-free assay)
FLT3 [2]
(Cell-free assay)
PKCα [1]
(Cell-free assay)
PKCβ1 [1]
(Cell-free assay)
PKC [1]
(Rat brain)
2.3 nM 6.2 nM 7.9 nM
In vitro

Go6976 have no effect on the kinase activity of the Ca(2+)-independent PKC subtypes delta, epsilon, and zeta. [1] Beside WT JAK2, Go6976 also inhibits the mutant forms (JAK2 V617F and TEL-JAK2) found in haematological malignancies, and has activity against mutant forms of FLT3. In AML cells, Go6976 reduces the survival to 55% of control in FLT3-ITD cases and to 69% in FLT3-WT samples.[2] Go 6976 potently inhibits HIV-1 induction by Bryostatin 1, tumor necrosis factor alpha, and interleukin 6. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Vero NGfOZoxEgXSxdH;4bYNqfHliYYPzZZk> MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBC\nKrY3HuJIdz\WWwIH3vcotmgSCYZYLvJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBu\WG|dYLl[EBwdiCmYYmgOUBxd3O2IHTvd4Uh[nliTWTTM3BOWyCkYYPl[EBucWO{b4Pjc5Bq[yCjbnHsfZNqeyxiQ1O1NF03|ryPLh?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ6OUm3OUc,Ojh4OEm5O|U9N2F-
primary microglial cells M13qVmZ2dmO2aX;uJIF{e2G7 Ml;ETY5pcWKrdHnvckBw\iCLRl6t[4FudWFvaX7keYNm\CCLRl6t[4FudWFicnXneYxifG:{eTDmZYN1d3JibHX2[Yx{KGmwIGPwdoFofWVvRHH3cIV6KHKjdDDwdolu[XK7IH3pZ5Jw\2yrYXygZ4VtdHNiYomgW4V{fGW{bjDicI91fGmwZx?= NVzzWVkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVU2QTBpPkG3N|k2PTlyPD;hQi=>
primary microglial cells NWHYVIJ{TnWwY4Tpc44h[XO|YYm= NEnpOFcyNjNidV2= NVHtV5QyW3WycILld5Nqd25ib3[gTWZPNWejbX3hMYlv\HWlZXSgVGtE[WyyaHGvZoV1[TJiboXjcIVieiC2cnHud4xw[2G2aX;uJIlvKFOycnHneYUuTGG5bHX5JJJifCCycnntZZJ6KG2rY4Lv[4xq[WxiY3XscJMh[XRiMT6zJJVOKGK7IGfld5Rmem5iYnzveJRqdmd? M4[0NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m1OVkxLz5zN{O5OVU6ODxxYU6=
primary microglial cells MVjGeY5kfGmxbjDhd5NigQ>? MlvmNU4{KHWP MWPTeZBxemW|c3nvckBw\iCLRl6t[4FudWFvaX7keYNm\CCLRl6t[4FudWFicnXneYxifG:{eTDmZYN1d3JiMTDueYNt\WG{IITyZY5{dG:lYYTpc44hcW5iU4DyZYd2\S2GYYfs[ZkhemG2IIDybY1ienlibXnjdo9odGmjbDDj[YxteyCjdDCxMlMhfU1iYomgW4V{fGW{bjDicI91fGmwZx?= MlPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|OUW1PVAoRjF5M{m1OVkxRC:jPh?=
DAOY MmDTdWhVWyCjc4PhfS=> MUjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>? NGnzbHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MmnRdWhVWyCjc4PhfS=> Mnm5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NXXCRmJWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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NB-EBc1 NUTQRlBZeUiWUzDhd5NigQ>? M{\CNpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NWiydlhYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NYTKVJRleUiWUzDhd5NigQ>? Mm\adWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH NHPjd41yUFSVIHHzd4F6 M{XjTpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz M1;QdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 NX7SWlVweUiWUzDhd5NigQ>? M{fQOpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= MlHkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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MG 63 (6-TG R) MlLCdWhVWyCjc4PhfS=> NXz6colVeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz MlPQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 NGT5UpByUFSVIHHzd4F6 M{LkSZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG5DOTZ2MzDj[Yxtew>? Mn\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 NXzZfoJueUiWUzDhd5NigQ>? MkPTdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRVY4OyClZXzsd{k> M33v[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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NB-EBc1 MXvxTHRUKGG|c3H5 NGDXVYxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBPSi2HQnOxJINmdGy| MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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TC32 NHfiO4FyUFSVIHHzd4F6 M1qzcJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> NX;5VGFKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Assay
Methods Test Index PMID
Western blot p-EGFR / EGFR / p-AKT / AKT / p-ERK / ERK / p-S6 / S6 23229345
Immunofluorescence p62 / LAMP2 29794026
In vivo Go6976 (2.5 mg/kg i.p.), as a PKD inhibitor, effectively prevents LPS/D: -GalN-induced acute liver injury by inhibition of MAPKs activation to reduce TNF-α production, and significantly improves the survival of LPS/D-GalN-challenged mice. [4]

Protocol (from reference)

Kinase Assay:

[1]

  • PKC Activity Assay:

    In brief, for measuring PKCα, and PKCβ1 and PKC from rat brain, the assay mixture of 200 μl contains 50 mM HEPES (pH7.5), 5 mM MgCl2, 1 mM EDTA, 1.25 mM EGTA, 1.32 mM CaC12, 1 mM dithiothreitol, 1 μg of phosphatidylserine, 0.2 μg of diolein, 40 μg of histone Hi, 10 μM [γ-32P]ATP (1 μCi/ml), and 5-10 units (pmol of Pi/min) of PKC. Assays are started by the addition of [γ-32P]ATP, incubated for 5 min at 30 °C, stopped by the addition of 2 ml of 8.5% H3PO4, filtered through 0.45-μm nitrocellulose filters, and evaluated by scintillation counting.

Cell Research:

[2]

  • Cell lines: Primary AML cells
  • Concentrations: 1 μM
  • Incubation Time: 48 hours
  • Method:

    Cells are suspended at 2 × 105 per point in 200 μl RPMI/10% FCS. The inhibitor under investigation is added at the appropriate concentration and the cells incubated for 48 h at 37°C, 5% CO2. MTS activity is measured by CellTiter kit according to the manufacturers instructions. Results are expressed as a percentage of control (cells without inhibitor).

Animal Research:

[4]

  • Animal Models: LPS/D-GalN-challenged mice
  • Dosages: 2.5 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 18 mg/mL warmed
(47.69 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% CMC Na+1% Tween 80
For best results, use promptly after mixing.

30mg/mL

Chemical Information

Molecular Weight 377.42
Formula

C24H18N4O

CAS No. 136194-77-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2=CC=CC=C2C3=C4C(=C5C6=CC=CC=C6N(C5=C31)CCC#N)CNC4=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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