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Chemical Structure : BC-DXI-32982
Catalog No.: PC-38706Not For Human Use, Lab Use Only.
BC-DXI-32982 is a specific small molecule DX2-KRAS inhibitor that specifically binds to the KRAS-binding region of AIMP2-DX2, inhibits interaction between DX2 and KRAS4B with IC50 of 0.18 uM.
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BC-DXI-32982 is a specific small molecule DX2-KRAS inhibitor that specifically binds to the KRAS-binding region of AIMP2-DX2, inhibits interaction between DX2 and KRAS4B with IC50 of 0.18 uM.
BC-DXI-32982 shows little effect on the PRKACA-PRKAR2A interaction, exhibits inhibitory efficacy on the binding of endogenous DX2 to KRAS with no effect on p14ARF in co-immunoprecipitation.
BC-DXI-32982 (0-10 uM) dose-dependently reduces endogenous KRAS levels and the activities of downstream effectors, p-ERK and p-Akt, in compound treated H460 cells.
BC-DXI-32982 suppresses cell viability in cancer cell lines with high levels of DX2, with no effect on the viability of untransformed MEF cells.
BC-DXI-32982 treatment suppressed phosphorylation of ERK, a KRAS downstream effector, in cancer cell lines regardless of KRAS mutation status, exerts cytotoxic activity by suppressing ERK via KRAS.
BC-DXI-32982 competitively interferes with the interaction between DX2 and KRAS through its binding to the DX2 GST domain, leading to the suppression of KRAS-driven cancer cell growth.
AIMP2-DX2, a variant of the tumor suppressor AIMP2 (aminoacyl-tRNA synthetase-interacting multi-functional protein 2), acts as a cancer-specific regulator of KRAS stability, augmenting KRAS-driven tumorigenesis.
| M.Wt | 483.561 | |
| Formula | C28H22FN3O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Dae Gyu Kim, et al. AIMP2-DX2 provides therapeutic interface to control KRAS-driven tumorigenesis
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