ACA22

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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Biological Activity

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.

Physicochemical Properties

M.Wt	308.34
Formula	C17H16N4O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(2-(1H-indole-2-carbonyl)hydrazineyl)-2-phenylacetamide

References

1. Cynthia V Pagba, et al. ACS Omega. 2023 Aug 18;8(34):31419-31426.

ACA22

Biological Activity

Physicochemical Properties

References

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