PIK-75

• 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].

• 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.

• CAS Number:

  [372196-67-3]