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Evo312 is an inhibitor of protein kinase C beta I (PKCβI) with an IC50 of 117.34 nM and exhibits dose-dependent characteristics. It acts by inhibiting the expression of the PKCβI protein, which leads to cell cycle arrest and apoptosis in PANC-GR (gemcitabine-resistant pancreatic cancer cells). Evo312 also demonstrates antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR, with IC50 values of 0.08 μM and 0.07 μM respectively, while presenting an IC50 of 2.95 μM in normal human pancreatic ductal epithelial cells HPDE6-c7. Additionally, Evo312 has shown antitumor activity in a mouse xenograft model using PANC-GR cells.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | 10-14 weeks | |
50 mg | Inquiry | 10-14 weeks |
Description | Evo312 is an inhibitor of protein kinase C beta I (PKCβI) with an IC50 of 117.34 nM and exhibits dose-dependent characteristics. It acts by inhibiting the expression of the PKCβI protein, which leads to cell cycle arrest and apoptosis in PANC-GR (gemcitabine-resistant pancreatic cancer cells). Evo312 also demonstrates antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR, with IC50 values of 0.08 μM and 0.07 μM respectively, while presenting an IC50 of 2.95 μM in normal human pancreatic ductal epithelial cells HPDE6-c7. Additionally, Evo312 has shown antitumor activity in a mouse xenograft model using PANC-GR cells. |
Targets&IC50 | PKCβ1:117.34 nM |
In vitro | Evo312, when applied at concentrations ranging from 0-160 nM for 24 hours, inhibits the expression of PKCβ1 protein and the phosphorylation of downstream target proteins in PANC-GR cells. Additionally, Evo312 at the same concentration and duration induces G2/M cell cycle arrest and inhibits mitosis in PANC-GR cells. Furthermore, when administered at the same concentration for 48 hours, Evo312 induces apoptosis in PANC-GR cells. |
In vivo | Evo312 (5 mg/kg, i.p., three times a week, 20 days) inhibits tumor growth in a xenograft mouse model of PANC-GR (gemcitabine-resistant cells) by downregulating PKCβI. The effect of gemcitabine treatment on tumor growth was negligible. |
Molecular Weight | 361.39 |
Formula | C21H19N3O3 |
Cas No. | 2820245-53-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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