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Chemical Structure : IDH2 R140Q inhibitor CP-17
Catalog No.: PC-20532Not For Human Use, Lab Use Only.
IDH2 R140Q inhibitor CP-17 is a potent, selective inhibitor of IDH2 R140Q mutation with IC50 of 40.75 nM, 50-fold selectivity over wild-type IDH1/2.
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IDH2 R140Q inhibitor CP-17 is a potent, selective inhibitor of IDH2 R140Q mutation with IC50 of 40.75 nM, 50-fold selectivity over wild-type IDH1/2.
CP-17 binds to an allosteric site located within the interface of IDH2/R140Q homodimer, stabilizing an open conformation of the active site.
CP-17 (3 uM) significantly inhibited the GM-CSF-independent growth of TF-1(IDH2/R140Q) cells but had no obvious effect on the proliferation of TF-1(WT) cells.
CP-17 showed a dose-dependent inhibition against intracellular D-2-HG production by TF-1(IDH2/R140Q) cells with IC50 of 141.4 nM.
CP-17 (1 and 3 uM) induced a dose-dependent decrease in histone methylation, thus restored the differentiation of TF-1(IDH2/R140Q) cells.
| M.Wt | 448.95 | |
| Formula | C25H25ClN4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jiao Chen, et al. Cell Commun Signal. 2020 Apr 3;18(1):55.
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