KRAS inhibitor-9 |
Catalog No.GC60969 |
강력한 KRAS 억제제(Kd=92μM)인 KRAS 억제제-9는 GTP-KRAS의 형성과 KRAS의 다운스트림 활성화를 차단합니다. KRAS 억제제-9는 KRAS G12D, KRAS G12C 및 KRAS Q61H 단백질에 적당한 결합 친화도로 결합합니다. KRAS 억제제-9는 G2/M 세포 주기 정지를 유발하고 세포자멸사를 유도합니다. KRAS 억제제-9는 KRAS 돌연변이가 있는 NSCLC 세포의 증식을 선택적으로 억제하지만 정상 폐 세포는 그렇지 않습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 300809-71-6
Sample solution is provided at 25 µL, 10mM.
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells[1].
KRAS inhibitor-9 bound to KRASG12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity of -5.38, -5.41, and -3.97 kcal/mol, respectively[1]. KRAS inhibitor-9 (0-100 μM) shows strong inhibition selectivity in NSCLC cells with IC50s ranging from 39.56 to 66.02 μM for H2122, H358 and H460 cells (at 72 hours)[1].KRAS inhibitor-9 (0-100 μM; 24 hours) blocks GTP-KRAS formation in H2122, H358 and H460 cells[1].KRAS inhibitor-9 (25-100 μM; 48 hours) inhibits the activation of KRAS downstream signaling pathway[1].KRAS inhibitor-9 (0-100 μM; 24-72 hours) induces cell cycle arrest and apoptosis in NSCLC[1]. Cell Viability Assay[1] Cell Line: H2122 (KRAS G12C), H358 (KRAS G12C) and H460 (KRAS Q61H) cell lines
[1]. Xie C, et al. Identification of a New Potent Inhibitor Targeting KRAS in Non-small Cell Lung Cancer Cells. Front Pharmacol. 2017;8:823. Published 2017 Nov 14.
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