Product Description: PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM)[1][2]. PIK-75 induces apoptosis[3].
Applications: Cancer-Kinase/protease
Formula: C16H14BrN5O4S
Citations: Molecules. 2020 Apr 23;25(8):1980./Clin Cancer Res. 2020 Apr 15;26(8):2011-2021. /Research Square Preprint. 2023 Apr 6.
References: [1]Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47./[2]Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58./[3]Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69.
CAS Number: 372196-67-3
Molecular Weight: 452.28
Compound Purity: 98.72
Research Area: Cancer
Solubility: DMSO : 50 mg/mL (ultrasonic;warming;heat to 60°C)
Target: Apoptosis;DNA-PK;PI3K