Molecular structure of PIK-75, hydrochloride, CAS Number: 372196-77-5
PIK-75, hydrochloride (CAS 372196-77-5)
Alternate Names:
2-methyl-5-nitro-2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide-benzenesulfonic acid, monohydrochloride
Application:
PIK-75, hydrochloride is a selective inhibitor of PI 3-kinase isoform p110α
CAS Number:
372196-77-5
Purity:
≥98%
Molecular Weight:
488.74
Molecular Formula:
C16H14BrN5O4S•HCl
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 3-Kα Inhibitor VIII is a cell-permeable imidazopyridine compound that acts as a highly potent and ATP-competitive DNA-PK and p110α-selective PI 3-kinase inhibitor (IC50 = 0.3, 40, 100, and 850 nM for p110α, p110γ, PI 3-K C2β, and p110β, respectively). PI 3-Kα Inhibitor VIII may act to effectively block cellular PI 3-kinase/Akt signaling and inhibit tumor growth both in vitro (IC50 ≤58 nM in MCF7, MCF7 ADR-res, HeLa, A375, and A549 cultures) and in mice in vivo (62% inhibition of HeLa xenograft in 2 weeks, 50 mg/kg/day, i.p.).
PIK-75, hydrochloride (CAS 372196-77-5) References
- Development of PIK-75 nanosuspension formulation with enhanced delivery efficiency and cytotoxicity for targeted anti-cancer therapy. | Talekar, M., et al. 2013. Int J Pharm. 450: 278-89. PMID: 23632263
- Targeting acute myeloid leukemia by dual inhibition of PI3K signaling and Cdk9-mediated Mcl-1 transcription. | Thomas, D., et al. 2013. Blood. 122: 738-48. PMID: 23775716
- Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. | Duong, HQ., et al. 2014. Int J Oncol. 44: 959-69. PMID: 24366069
- Suppression of CD4+ T lymphocyte activation in vitro and experimental encephalomyelitis in vivo by the phosphatidyl inositol 3-kinase inhibitor PIK-75. | Acosta, YY., et al. 2014. Int J Immunopathol Pharmacol. 27: 53-67. PMID: 24674679
- The inhibitory effect of PIK-75 on inflammatory mediator response induced by hydrogen peroxide in feline esophageal epithelial cells. | Jeong, JY., et al. 2014. Mediators Inflamm. 2014: 178049. PMID: 25276052
- Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9. | Phillipson, LJ., et al. 2015. Bioorg Med Chem. 23: 6280-96. PMID: 26349627
- Phosphoinositide 3-Kinase Is Involved in Mediating the Anti-inflammation Effects of Vasopressin. | Jan, WC., et al. 2017. Inflammation. 40: 435-441. PMID: 27943011
- Identification of Hsp90 Inhibitors with Anti-Plasmodium Activity. | Posfai, D., et al. 2018. Antimicrob Agents Chemother. 62: PMID: 29339390
- An Unusual Intramolecular Halogen Bond Guides Conformational Selection. | Tesch, R., et al. 2018. Angew Chem Int Ed Engl. 57: 9970-9975. PMID: 29873877
- PIK-75 promotes homology-directed DNA repair. | Li, G., et al. 2019. J Genet Genomics. 46: 141-144. PMID: 30935856
- Joint action of miR-126 and MAPK/PI3K inhibitors against metastatic melanoma. | Pedini, F., et al. 2019. Mol Oncol. 13: 1836-1854. PMID: 31115969
- Role of PI3K/Akt and MEK/ERK Signalling in cAMP/Epac-Mediated Endothelial Barrier Stabilisation. | Gündüz, D., et al. 2019. Front Physiol. 10: 1387. PMID: 31787905
- Context dependent isoform specific PI3K inhibition confers drug resistance in hepatocellular carcinoma cells. | Narci, K., et al. 2022. BMC Cancer. 22: 320. PMID: 35331184
- Reciprocal regulation of Daxx and PIK3CA promotes colorectal cancer cell growth. | Huang, YS., et al. 2022. Cell Mol Life Sci. 79: 367. PMID: 35718818
Inhibitor of:
ARX, C030037F17Rik, C11orf24, C22orf34, C2orf18, C2orf74_1700093K21Rik, Centaurin α2, DNA-PK, EDEM3, EG626456, ESC, IF3, IRP-2, KRBA2, Lambda 5, LOC100041343, LOC283904, LOC439950, LOC645188, LRRC2, MafF, MrgA1, Olfr478, Olfr479, Olfr830, OTTMUSG00000010327, PI 3-kinase C2y, PI 3-kinase p110 alpha, PI 3-kinase p110 gamma, PI 4-kinase α, PLC ε, PLEKHM2, PRIC285, Rbx1, Reticulum Cell, RNF11, SAV1, SerpinB1a, SgK269, SH3D19, SKAP55, SP140, SPATA19, Speedy E4, STS-1, TPIP, UFSP2, USP10, XTP3-B, and ZNF216.Activator of:
Clm3, eyes absent, Kex2, KLHL18, MLL5, NO66, NYAP2, PFAAP5, PI 3-kinase p110, Ral A, RYBP, STK33, and Tctex5.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PIK-75, hydrochloride, 1 mg | sc-296089 | 1 mg | $29.00 | |||
PIK-75, hydrochloride, 5 mg | sc-296089A | 5 mg | $124.00 |