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Chemical Structure : ACA22
Catalog No.: PC-21132Not For Human Use, Lab Use Only.
ACA22 is a small molecule KRAS inhibitor, inhibits KRAS-mediated signal transduction in cells expressing wild type (WT) and G12D mutant KRAS.
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ACA22 is a small molecule KRAS inhibitor, inhibits KRAS-mediated signal transduction in cells expressing wild type (WT) and G12D mutant KRAS.
ACA22 binds to guanosine 5′-β,γ-imidophosphate, GNP (a non-hydrolysable GTP analogue)-bound WT and G12D, G13D, and Q61H KRAS at pocket p1 with KD 3-16 uM.
ACA22 shows affinity for WT GNP-KRAS (KD=3 uM), 75-fold stronger than that for the GDP-bound form (GDP-KRAS WT, Kd=225 uM).
ACA22 inhibits WT KRAS more robustly than mutant KRAS.
ACA22 has no effect on intrinsic or GEF-mediated nucleotide exchange reactions of KRAS, also has no effect on KRAS-effector interactions.
| M.Wt | 308.34 | |
| Formula | C17H16N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Cynthia V Pagba, et al. ACS Omega. 2023 Aug 18;8(34):31419-31426.
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