Molecular structure of PI-103, CAS Number: 371935-74-9
PI-103 (CAS 371935-74-9)
See product citations (3)
Alternate Names:
PI 3-K Inhibitor V
Application:
PI-103 is an ATP-competitive DNA-PK, PI 3-kinase, and FRAP inhibitor
CAS Number:
371935-74-9
Purity:
99%
Molecular Weight:
348.36
Molecular Formula:
C19H16N4O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
PI-103 is a cell-permeable pyridinylfuranopyrimidine compound that acts as an ATP-competitive inhibitor of DNA-PK and FRAP mTOR(FRAP)complex 1 and 2. Studies suggest that PI-103 can induce apoptosis and an arrest in the cell cycle by inhibition of the aforementioned proteins. When PI-103 is combined with rapamycin, a prototypic mTORC1 inhibitor, synergistic suppression of AKT and ribosomal S6 protein phosphorylation are observed. In addition, PI-103 has been seen to have nominal effects inhibiting basal Na+ transport, but is very effective in abolishing insulin-induced Na+ absorption in the nephron. PI-103 is an inhibitor of PI 3-kinase p110 alpha, PI 3-kinase p110 beta, PI 3-kinase p110 delta and PI 3-kinase p110 gamma.
PI-103 (CAS 371935-74-9) References
- PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML. | Park, S., et al. 2008. Leukemia. 22: 1698-706. PMID: 18548104
- Effects of nominally selective inhibitors of the kinases PI3K, SGK1 and PKB on the insulin-dependent control of epithelial Na+ absorption. | Mansley, MK. and Wilson, SM. 2010. Br J Pharmacol. 161: 571-88. PMID: 20880397
- Vertical inhibition of the mTORC1/mTORC2/PI3K pathway shows synergistic effects against melanoma in vitro and in vivo. | Werzowa, J., et al. 2011. J Invest Dermatol. 131: 495-503. PMID: 21048785
- A dual PI3K/mTOR inhibitor, PI-103, cooperates with stem cell-delivered TRAIL in experimental glioma models. | Bagci-Onder, T., et al. 2011. Cancer Res. 71: 154-63. PMID: 21084267
- Oncostatin M-enhanced vascular endothelial growth factor expression in human vascular smooth muscle cells involves PI3K-, p38 MAPK-, Erk1/2- and STAT1/STAT3-dependent pathways and is attenuated by interferon-γ. | Demyanets, S., et al. 2011. Basic Res Cardiol. 106: 217-31. PMID: 21174212
- PI-103 and sorafenib inhibit hepatocellular carcinoma cell proliferation by blocking Ras/Raf/MAPK and PI3K/AKT/mTOR pathways. | Gedaly, R., et al. 2010. Anticancer Res. 30: 4951-8. PMID: 21187475
- PI-103 sensitizes acute myeloid leukemia stem cells to daunorubicin-induced cytotoxicity. | Ding, Q., et al. 2013. Med Oncol. 30: 395. PMID: 23335068
- PI-103 and Quercetin Attenuate PI3K-AKT Signaling Pathway in T- Cell Lymphoma Exposed to Hydrogen Peroxide. | Maurya, AK. and Vinayak, M. 2016. PLoS One. 11: e0160686. PMID: 27494022
- PI-103 attenuates PI3K-AKT signaling and induces apoptosis in murineT-cell lymphoma. | Maurya, AK. and Vinayak, M. 2017. Leuk Lymphoma. 58: 1153-1161. PMID: 27658642
- Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. | Luo, L., et al. 2020. Bioorg Med Chem Lett. 30: 127258. PMID: 32527558
- Opposite effects of the triple target (DNA-PK/PI3K/mTOR) inhibitor PI-103 on the radiation sensitivity of glioblastoma cell lines proficient and deficient in DNA-PKcs. | Djuzenova, CS., et al. 2021. BMC Cancer. 21: 1201. PMID: 34763650
- An investigation of the metabolic activity, isozyme contribution, species differences and potential drug-drug interactions of PI-103, and the identification of efflux transporters for PI-103-O-glucuronide in HeLa1A9 cells. | Gao, L., et al. 2020. RSC Adv. 10: 9610-9622. PMID: 35497201
- A gene prognostic index from cellular senescence predicting metastasis and radioresistance for prostate cancer. | Feng, D., et al. 2022. J Transl Med. 20: 252. PMID: 35658892
- Two-pore channel blockade by phosphoinositide kinase inhibitors YM201636 and PI-103 determined by a histidine residue near pore-entrance. | Du, C., et al. 2022. Commun Biol. 5: 738. PMID: 35871252
- RIDR-PI-103, ROS-activated prodrug PI3K inhibitor inhibits cell growth and impairs the PI3K/Akt pathway in BRAF and MEK inhibitor-resistant BRAF-mutant melanoma cells. | Patel, H., et al. 2023. Anticancer Drugs. 34: 519-531. PMID: 36847042
Inhibitor of:
β-defensin 133, β-defensin 18, β-defensin 43, β-defensin 50, 1700021F02Rik, 4921510H08Rik, 9430016H08Rik, advillin, AI314180, ALG-4, ANGEL2, BC051070, Bpifa6, C4orf37, C6orf81, C7orf52, CARD 11, CEACAM1, Centaurin β5, Clm3, CRIM2, CSN3, D4Ertd196e, D630037F22Rik, DDX41, DNA-PK, E230008N13Rik, EAT-2B, EG224763, EG225058, EG432879, EG626575, EVT-2, F8A1, F8A2, FAM131C, FAM169A, FAM183A, FAM83B, FAM8A1, FLJ40125, Fus1, Gab 2, GATSL2, GATSL3, GFAP, Ggnbp2, Gm6772, Grap, GRIP-1, GSDMDC1, HMG-14, ILKAP, INSL4, IRS-3, KBTBD2, KIAA1377, KIAA1609, LAMTOR4, LOC100041274, LOC342918, LOC646864, LOC728379, LOC729974, LRRC31, MAGE-A12, MAGE-B10, MICB, mTOR, NG2, NICE4, NKIAMRE, NKR-P1F, Olfr520, OTTMUSG00000012817, OTTMUSG00000019256, p52 S6 kinase, PGBD2, PI 3-kinase C2α, PI 3-kinase C2β, PI 3-kinase p101, PI 3-kinase p110, PI 3-kinase p110 alpha, PI 3-kinase p110 beta, PI 3-kinase p110 delta, PI 3-kinase p110 gamma, PI 3-kinase p55γ, PI 3-kinase p85α, PI 3-kinase p85β, PI 4-kinase α, PIPK I β, PLEKHS1, PRLH, Protor-2, PRR5, PTN, Rae-1α, Rag C, REDD-2, RN-tre, RNF167, RWDD2B, SAC1_Sac1, SPATA17, Sprouty 4, STK33, TAPP1, TESSP5, TMEM232, TMEM55A, TMEM55B, TREML6, TTP-αL, VAC14, VGF, WDR75, and WSCD1.Activator of:
14-3-3 ζ, 4E-BP2, Aex-3, Atg10, C16orf72, C1orf159, C87499, C87977, DIO3, EBV EBNA-3A, eIF4E3, FAM111B, FGF-BP, FOXE2, HSV-1 ICP0, IL-5, KRTAP2, MTMR8, myotubularin, NPRL3, PAK5, PERQ1, PIK3IP1, Rabaptin-5β, RhebL1, Rif1, SGK3, SMG1, SNX3, SNX5, SUSP4, TINAGL1, and UBE3C.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PI-103, 1 mg | sc-203193 | 1 mg | $32.00 | |||
PI-103, 5 mg | sc-203193A | 5 mg | $128.00 |