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Go6976 selectively inhibits PKCα and PKCβ1 (IC50 values are 2.3 and 6.2 nM respectively). Go6976 also inhibits TrkA, TrkB, JAK2 and JAK3 tyrosine kinases (IC50 values are 5, 30, 130 and 370 nM respectively), PKCμ (PKD1) and the mitotic spindle checkpoint. Go 6976 blocks neurotrophin-induced signaling and autophosphorylation of neurotrophin-specific tyrosine kinase (Trk) receptors.
Patent. CN117942336A 2024 Apr 30.
Patent. CN117942336A
Go6976 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | Primary AML cells |
| Preparation method | Suspending cells at 2 × 105 per point in 200 μl RPMI/10% FCS. Adding the inhibitor under investigation at the appropriate concentration and incubating the cells for 48 h at 37°C, 5% CO2. Measuring MTS activity by CellTiter kit according to the manufacturers instructions. Expressing results as a percentage of control (cells without inhibitor). |
| Concentrations | 1 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | LPS/D-GalN-challenged mice |
| Formulation | DMSO |
| Dosages | 2.5 mg/kg |
| Administration | i.p. |
| Molecular Weight | 378.43 |
| Formula | C24H18N4O |
| CAS Number | 136194-77-9 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PKC Products |
|---|
| Enzastaurin
Enzastaurin inhibits PKCβ, PKCα, PKCγ and PKCε with IC50's of 0.006, 0.039, 0.083 and 0.110 µM, respectively. |
| Go 6983
Go 6983 is a fast acting, lipid soluble, broad spectrum protein kinase C inhibitor. |
| Staurosporine
Staurosporine (AM-2282) is a potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively. |
| Zoledronic acid
Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects. |
| Dequalinium Chloride
Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM. |
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