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SP-1-303

Chemical Structure : SP-1-303

CAS No.: 1997286-03-9

SP-1-303

Catalog No.: PC-22672Not For Human Use, Lab Use Only.

SP-1-303 is a dual-targeting class I HDAC inhibitor and ATM activator with IC50 of 12/14 nM for HDAC1/3, preferentially inhibits ER+ breast cancer growth.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SP-1-303 is a dual-targeting class I HDAC inhibitor and ATM activator with IC50 of 12/14 nM for HDAC1/3, preferentially inhibits ER+ breast cancer growth.
SP-1-303 exhibits specificity in inhibiting C HDAC1 and HDAC3, preferentially to HDAC6.
SP-1-303 (1 uM) significantly enhanced acetylation of histone H3 lysine 9 (H3K9) and phosphorylation of ATM/S1981 within 0.5 h of cell exposure in in both MCF7 and MDA-MB-231 cells.
SP-1-303 exhibits effective cell growth inhibition with EC50 of 0.34 and 0.32 uM against ER+ breast cancer cell lines MCF7 and T47D.
SP-1-303 decreases estrogen receptor alpha (ER-α) expression and increases p53 protein expression, while inducing the phosphorylation of ATM and its substrates, BRCA1 and p53, in a time-dependent manner in ER+ BC cells.

Physicochemical Properties

M.Wt 498.58
Formula C29H30N4O4
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

7-(3,4-bis(2-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-N-hydroxyheptanamide

References

1. Mira Jung, et al. PLoS One. 2024 Jul 15;19(7):e0306168.

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