PIK-75 (hydrochloride)

PIK-75 hydrochloride 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 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) [1][2]. PIK-75 hydrochloride induces apoptosis[3].

Product Specifications

CAS Number

[372196-77-5]

UNSPSC

12352005

Hazard Statement

H302

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.html

Purity

99.66

Solubility

DMSO : 11 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

BrC(C=C1)=CN2C1=NC=C2/C=N/N(S(=O)(C3=C(C=CC([N+]([O-])=O)=C3)C)=O)C.[H]Cl

Molecular Formula

C16H15BrClN5O4S

Molecular Weight

488.74

Precautions

H302

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.|[4]Hayakawa M, Kawaguchi K, Kaizawa H, et al. Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007;15 (17) :5837-5844.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

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

Citation 01

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