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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $48 | In Stock | |
5 mg | $122 | In Stock | |
10 mg | $197 | In Stock | |
25 mg | $332 | In Stock | |
50 mg | $498 | In Stock | |
1 mL x 10 mM (in DMSO) | $157 | In Stock |
Description | ONX-0914 (PR-957) is an effective and specific immunoproteasome inhibitor, which has minimal cross-reactivity for the constitutive proteasome. |
In vitro | Selective inhibition of LMP7 by PR-957 blocked production of interleukin-23 (IL-23) by activated monocytes and interferon-gamma and IL-2 by T cells. |
In vivo | In mouse models of rheumatoid arthritis and lupus, the maximum tolerated dose (MTD) of ONX-0914 in mice to be 30 mg/kg body weight. |
Kinase Assay | 20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 μCi (γ)-32P ATP and 1.5 μM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. 32P-labeled bands are quantified using ImageJ and the IC50 values are calculated using GraphPad. |
Alias | ONX0914, PR-957, ONX 0914 |
Molecular Weight | 580.67 |
Formula | C31H40N4O7 |
Cas No. | 960374-59-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (86.11 mM) ![]() | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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