PIK-75 (hydrochloride)
Product Specifications
UNSPSC Description
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].
Target Antigen
Apoptosis; DNA-PK; PI3K
Type
Reference compound
Related Pathways
Apoptosis;Cell Cycle/DNA Damage;PI3K/Akt/mTOR
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/pik-75.html
Purity
99.72
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 Weight
488.74
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. Clin Cancer Res. 2020 Apr 15;26(8):2011-2021. |Research Square Preprint. 2023 Apr 6.|Adv Sci (Weinh). 2024 Jun 3:e2400023.|Molecules. 2020 Apr 23;25(8):1980.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-13281/PIK-75-hydrochloride-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-13281/PIK-75-hydrochloride-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
372196-77-5
Available Sizes
Curated Selection
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