BC-DXI-32982 | DX2-KRAS inhibitor | Probechem Biochemicals

Chemical Structure : BC-DXI-32982

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BC-DXI-32982 (DX2-KRAS inhibitor)

货号: 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.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	483.561
分子式	C28H22FN3O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(2-fluorophenyl)-N-((5-(4-methoxy-3-methylphenyl)thiophen-2-yl)methyl)quinoxaline-2-carboxamide

参考文献

1. Dae Gyu Kim, et al. AIMP2-DX2 provides therapeutic interface to control KRAS-driven tumorigenesis.