ACA-28 (compound 2a) is a potent modulator of the ERK MAPK signaling pathway that exerts anticancer effects through a unique mechanism involving ERK hyperactivation. Rather than inhibiting ERK activity directly, ACA-28 induces sustained ERK activation, which paradoxically triggers apoptosis in cancer cells.
It demonstrates selective cytotoxicity, inhibiting the growth of melanoma cells (SK-MEL-28) with an IC₅₀ of 5.3 μM, while showing lower toxicity toward normal human melanocytes (NHEM), with an IC₅₀ of 10.1 μM. ACA-28's ability to exploit ERK signaling dysregulation for selective induction of apoptosis makes it a promising candidate for further development in cancer therapy, particularly in ERK-dependent malignancies.
ACA-28 (compound 2a) is a potent modulator of the ERK MAPK signaling pathway that exerts anticancer effects through a unique mechanism involving ERK hyperactivation. Rather than inhibiting ERK activity directly, ACA-28 induces sustained ERK activation, which paradoxically triggers apoptosis in cancer cells.
It demonstrates selective cytotoxicity, inhibiting the growth of melanoma cells (SK-MEL-28) with an IC₅₀ of 5.3 μM, while showing lower toxicity toward normal human melanocytes (NHEM), with an IC₅₀ of 10.1 μM. ACA-28's ability to exploit ERK signaling dysregulation for selective induction of apoptosis makes it a promising candidate for further development in cancer therapy, particularly in ERK-dependent malignancies.
Product Information
Catalog Num
A24158
Formula
C17H16O6
Molecular Weight
316.31
CAS Number
948044-25-5
SMILES
O=C(OC)OC1=CC=C(C(C2=CC=CC=C2)OC(OC)=O)C=C1
Storage
Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 1 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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