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AZ960 is a novel and specific inhibitor of the JAK2 kinase with a Ki of 0.45nM in vitro. AZ 960 effectively induced growth arrest and apoptosis of human T-cell lymphotropic virus type 1, HTLV-1-infected T cells (MT-1 and MT-2) in parallel with downregulation of the phosphorylated forms of Jak2 and Bcl-2 family proteins including Bcl-2 and Mcl-1. Importantly, genetic inhibition of Bcl-xL by a small interfering RNA potentiated antiproliferative effects of AZ960 in MT-1 cells. Taken together, Jak2 is an attractive molecular target for treatment of ATL.
Bioorg Med Chem. 2016 Oct 1;24(19):4647-51.
Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor
AZ 960 purchased from AbMole
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Source | Bioorganic & Medicinal Chemistry (2016) . Figure 6. AZ960 was purchased from Abmole (Catalog No. M1660; Houston, TX) |
| Method | Kinase assays | |
| Cell Lines | T. brucei, primary mouse left ventricle smooth muscle cells (vSMC), and rat pancreatic b cells (ins-1) | |
| Concentrations | 0.5 and 1 µM | |
| Incubation Time | 30 min | |
| Results | As shown in Figure 6, treatment of these cells with inhibitor concentrations ranging from 100 nM to 2 mM resulted in dosedependent inhibition of cell growth. The IC50 of AZ960 for mouse ventricular smooth muscle cells was determined to be 25 lM ± 3 and 10 lM ± 1 for rat pancreatic b cells. |
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Source | Bioorganic & Medicinal Chemistry (2016) . Figure 5. AZ960 was purchased from Abmole (Catalog No. M1660; Houston, TX) |
| Method | Kinase assays | |
| Cell Lines | ||
| Concentrations | 0.5 and 1 µM | |
| Incubation Time | 30 min | |
| Results | We calculated the Michaelis–Menten constant (Km) for TbERK8 to be 3.4 lM ± 0.12 (Fig. 5A). The inhibition constant (Ki) of AZ960 for TbERK8 was calculated to be 1.25 lM ± 0.35 (Fig. 5B). |
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Source | Bioorganic & Medicinal Chemistry (2016) . Figure 4. AZ960 was purchased from Abmole (Catalog No. M1660; Houston, TX) |
| Method | Kinase assays | |
| Cell Lines | ||
| Concentrations | 1 µM | |
| Incubation Time | 30 min | |
| Results | As shown in Figure 4, compounds that inhibited TbERK8 kinase activity to 20% or less included AZD5438, PF-03814735, Milciclib, and AZ960. Our studies suggest that SNS-032, NVP-BGT226, GSK2126458, Dinaciclib, and Torin 2 have anti-T. brucei activities with mechanisms that likely do not involve inhibition of TbERK8. |
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Source | Bioorganic & Medicinal Chemistry (2016) . Figure 3. AZ960 was purchased from Abmole (Catalog No. M1660; Houston, TX) |
| Method | Cell Titer-Glo Promega assay | |
| Cell Lines | T. brucei strain WT-221 | |
| Concentrations | 80 nM to 1 µM | |
| Incubation Time | 48 h | |
| Results | The inhibitor activities ranged from 80 nM to 1 µM. Dinaciclib was the most potent inhibitor with an IC50 of 80 nM, but SNS-032, GSK2126458, and AZ960 were almost equally as potent with IC50 values of 120 nM, 111 nM, 120 nM, respectively. A representative dose–response curve for AZ960 is shown in Figure 3. |
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Source | Bioorganic & Medicinal Chemistry (2016) . Figure 2. AZ960 was purchased from Abmole (Catalog No. M1660; Houston, TX) |
| Method | luciferase-based phenotypic screen | |
| Cell Lines | T. brucei strain WT-221 | |
| Concentrations | 1 µM | |
| Incubation Time | 48 h | |
| Results | A rescreen that tested the select hits demonstrated a dramatic decrease in the mean RLU values by about 2 log10 orders, confirming the antiparasitic activity of the compounds (Fig. 2). |
| Cell Experiment | |
|---|---|
| Cell lines | SET-2 and TEL-JAK2 Ba/F3 cells |
| Preparation method | Proliferation Assay Cellular proliferation was evaluated using the fluorometric/colorimetric BIOSOURCE AlamarBlue Assay (Invitrogen) and read in the Spectra Max Gemini EM microplate reader (Molecular Devices, Sunnyvale, CA). SET-2 cells were plated at 20,000 cells/well, TEL-JAK2 Ba/F3 cells at 2000 cells/well, and all other TEL-JAKs at 5000 cells/well in 96-well plates. Cells were treated with compound 24 h after plating and grown for 72 h for SET-2 and 48 h for TEL-JAK Ba/F3 cells. Following the indicated growth period Alamar Blue (10 μl/well) was added, cells were incubated at 37 °C in 5% CO2 for 2 h, and fluorescence was measured at 545 (excitation) and 600 nm (emission). Data are normalized to percent of the control, and GI50 values (the concentration that causes 50% growth inhibition) were calculated using Xlfit4 version 4.2.2 for Microsoft Excel. |
| Concentrations | 0~100 μM |
| Incubation time | 72 h for SET-2 and 48 h for TEL-JAK Ba/F3 cells |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 354.36 |
| Formula | C18H16F2N6 |
| CAS Number | 905586-69-8 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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AG490 (Tyrphostin AG490) is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). |
| Momelotinib (CYT387)
Momelotinib (CYT387) is a small-molecule, ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 and 18 nM respectively. |
| TG101348
TG101348 is a selective small-molecule Janus kinase 2 (JAK2) inhibitor with IC50 of 3 nM. |
| WP1130
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| INCB18424
Ruxolitinib (INCB018424) is a first-in-class, potent, selective JAK1/2 inhibitor with an IC50 of 3.3 nM/2.8 nM. It is more than 130-fold more selective for JAK1, JAK2, and JAK3 than JAK3. It can be used in studies related to pemphigus, myelofibrosis and vitiligo. |
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