Go6976

Catalog No.S7119 Batch:S711903

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Technical Data

Formula

C24H18N4O
Molecular Weight 377.42 CAS No. 136194-77-9
Solubility (25°C)* In vitro DMSO 25 mg/mL (66.23 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]
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 Assay:

[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 Study:

[4]
  • Animal Models

    LPS/D-GalN-challenged mice

  • Dosages

    2.5 mg/kg

  • Administration

    i.p.

Customer Product Validation

, , Cell Signal, 2016, 28(9):1422-31.

Data from [Data independently produced by , , Acta Physiol, 2018, 223(3):e13055]

Data from [Data independently produced by , , J Biol Chem, 2018, doi:10.1074/jbc.RA118.002191]

Data from [Data independently produced by , , Infect Immun, 2017, e00087-17]

Selleck's Go6976 has been cited by 37 publications

Lamin A/C phosphorylation at serine 22 is a conserved heat shock response to regulate nuclear adaptation during stress [ J Cell Sci, 2023, 136(4)jcs259788] PubMed: 36695453
Spatially differential regulation of ATF2 phosphorylation contributes to warning coloration of gregarious locusts [ Sci Adv, 2023, 9(34):eadi5168] PubMed: 37611100
Spatially differential regulation of ATF2 phosphorylation contributes to warning coloration of gregarious locusts [ Sci Adv, 2023, 9(34):eadi5168] PubMed: 37611100
Trafficking of the glutamate transporter is impaired in LRRK2-related Parkinson's disease [ Acta Neuropathol, 2022, 144-1:81-106] PubMed: 35596783
p52 signaling promotes cellular senescence [ Cell Biosci, 2022, 12(1):43] PubMed: 35379326
(+)-Borneol inhibits the generation of reactive oxygen species and neutrophil extracellular traps induced by phorbol-12-myristate-13-acetate [ Front Pharmacol, 2022, 13:1023450] PubMed: 36419617
Combination of IL-17A/F and TNF-α uniquely alters the bronchial epithelial cell proteome to enhance proteins that augment neutrophil migration [ J Inflamm (Lond, 2022, 19(1:26)] PubMed: 36517803
Exploiting polypharmacology to dissect host kinases and kinase inhibitors that modulate endothelial barrier integrity [ Cell Chem Biol, 2021, S2451-9456(21)00303-2] PubMed: 34216546
Ubash3b promotes TPA-mediated suppression of leukemogenesis through accelerated downregulation of PKCδ protein [ Biochimie, 2021, 184:8-17] PubMed: 33556471
Five Constituents in Psoralea corylifolia L. Attenuate Palmitic Acid-Induced Hepatocyte Injury via Inhibiting the Protein Kinase C-α/Nicotinamide-Adenine Dinucleotide Phosphate Oxidase Pathway. [ Front Pharmacol, 2020, 10:1589] PubMed: 32116659

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.