Chemical Properties | Back Directory | [Boiling point ]
548.1±50.0 °C(Predicted) | [density ]
1.16±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:50.0(Max Conc. mg/mL);131.07(Max Conc. mM) | [form ]
Solid | [color ]
White to off-white |
Hazard Information | Back Directory | [Biological Activity]
BJE6-106 (B106) is a potent and selective PKCδ inhibitor with IC50 value of 0.05 μM, BJE6-106 (B106) targets PKCδ 1000-fold more selective than the PKC isoenzyme PKCα (IC50=50 μM) . BJE6-106 (B106) induces apoptosis in caspase-dependent cells. BJE6-106 (B106) has tumor-specific effects. | [in vitro]
BJE6-106 (B106) (0.2 μM, 0.5 μM; 24-72 hours) suppresses cell survival in melanoma cell lines with NRAS mutations. BJE6-106 (B106) (0.2 μM, 0.5 μM; 6- 24 hours) triggers caspase-dependent apoptosis, increases the activity of caspase 3/7, the effect of B106 is greater than rottlerin (10-fold) in SBcl2 cells. BJE6-106 (B106) (0.5 μM; 2-10 hours) activates the MKK4-JNK-H2AX Pathway by inducing MKK4, JNK and H2AX activation at different times in SBcl2 cells. Cell Viability Assay Cell Line: | Melanoma cell lines with NRAS mutations: SBcl2, FM6, SKMEL2, WM1366, WM1361A, and WM852 cells | Concentration: | 0.2 μM, 0.5 μM | Incubation Time: | 24 hours, 48 hours, or 72 hours | Result: | Inhibited cell survival in melanoma cell lines. | Apoptosis Analysis Cell Line: | < td class="col2"> SBcl2 cells Concentration: | 0.2 μM, 0.5 μM | Incubation Time: | 6 hours, 12 hours, or 24 hours | Result: | Induced caspase 3/7 activation. | Western Blot Analysis Cell Line : | SBcl2 cells | Concentration: | 0.2 μM , 0.5 μM | Incubation Time: | 2 hours, 5 hours, 10 hours | < /tr> Result: Increased phosphorylation of MKK4, JNK and H2AX. | | [target]
PKCδ 0.05 μM (IC 50 ) | PKCα 50 μM (IC 50 ) | |
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