PIK-75

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].

Product Specifications

CAS Number

[372196-67-3]

UNSPSC

12352005

Hazard Statement

H302+H312+H332, H315, H319, H335

Target

Apoptosis; DNA-PK; PI3K

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pik-75-1.html

Concentration

10mM

Purity

99.94

Solubility

DMSO : 13 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)/N=C/C2=CN=C3C=CC(Br)=CN32)=O

Molecular Formula

C16H14BrN5O4S

Molecular Weight

452.28

Precautions

H302+H312+H332, H315, H319, H335

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, protect from light)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

PI3KC2α; PI3KC2β; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ; Vps34

Citation 01

Adv Sci (Weinh) . 2024 Jun 3:e2400023.|Cell Rep. 2025 Feb 5;44 (2) :115246.|Molecules. 2020 Apr 23;25 (8) :1980.|Clin Cancer Res. 2020 Apr 15;26 (8) :2011-2021. |Res Sq. 2023 Apr 6:rs.3.rs-2688694.