SI113 is a specific inhibitor of the Sgk1 kinase activity, counteracting cancer cell proliferation.
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Name | SI113 |
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Iupac Chemical Name | (Z)-2-((4-(Phenethylamino)-1-styryl-1H-pyrazolo[3,4-d]pyrimidin-6-yl)amino)ethan-1-ol |
Synonyms | SI113; SI-113; SI 113 |
Molecular Formula | C23H24N6O |
Molecular Weight | 400.48 |
Smile | C(CC1=CC=CC=C1)NC1=C2C(=NC(=N1)NCCO)N(N=C2)\C=C/C2=CC=CC=C2 |
InChiKey | LAOYAWHHLUVMFT-QINSGFPZSA-N |
InChi | InChI=1S/C23H24N6O/c30-16-14-25-23-27-21(24-13-11-18-7-3-1-4-8-18)20-17-26-29(22(20)28-23)15-12-19-9-5-2-6-10-19/h1-10,12,15,17,30H,11,13-14,16H2,(H2,24,25,27,28)/b15-12- |
CAS Number | 1392816-46-4 |
Related CAS |
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Formulation | crystalline solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO, not in water |
Handling | |
Shipping Condition | Shipped under ambient temperature |
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1: Abbruzzese C, Catalogna G, Gallo E, di Martino S, Mileo AM, Carosi M, Dattilo V, Schenone S, Musumeci F, Lavia P, Perrotti N, Amato R, Paggi MG. The small molecule SI113 synergizes with mitotic spindle poisons in arresting the growth of human glioblastoma multiforme. Oncotarget. 2017 Nov 18;8(67):110743-110755. doi: 10.18632/oncotarget.22500. eCollection 2017 Dec 19. PubMed PMID: 29340013; PubMed Central PMCID: PMC5762281.
2: Catalogna G, Talarico C, Dattilo V, Gangemi V, Calabria F, D'Antona L, Schenone S, Musumeci F, Bianco C, Perrotti N, Amato R, Cascini GL. The SGK1 Kinase Inhibitor SI113 Sensitizes Theranostic Effects of the 64CuCl2 in Human Glioblastoma Multiforme Cells. Cell Physiol Biochem. 2017;43(1):108-119. doi: 10.1159/000480328. Epub 2017 Aug 25. PubMed PMID: 28848088.
3: Conza D, Mirra P, Calì G, Tortora T, Insabato L, Fiory F, Schenone S, Amato R, Beguinot F, Perrotti N, Ulianich L. The SGK1 inhibitor SI113 induces autophagy, apoptosis, and endoplasmic reticulum stress in endometrial cancer cells. J Cell Physiol. 2017 Dec;232(12):3735-3743. doi: 10.1002/jcp.25850. Epub 2017 Apr 27. PubMed PMID: 28177128.
4: Talarico C, Dattilo V, D'Antona L, Barone A, Amodio N, Belviso S, Musumeci F, Abbruzzese C, Bianco C, Trapasso F, Schenone S, Alcaro S, Ortuso F, Florio T, Paggi MG, Perrotti N, Amato R. SI113, a SGK1 inhibitor, potentiates the effects of radiotherapy, modulates the response to oxidative stress and induces cytotoxic autophagy in human glioblastoma multiforme cells. Oncotarget. 2016 Mar 29;7(13):15868-84. doi: 10.18632/oncotarget.7520. PubMed PMID: 26908461; PubMed Central PMCID: PMC4941283.
5: Talarico C, D'Antona L, Scumaci D, Barone A, Gigliotti F, Fiumara CV, Dattilo V, Gallo E, Visca P, Ortuso F, Abbruzzese C, Botta L, Schenone S, Cuda G, Alcaro S, Bianco C, Lavia P, Paggi MG, Perrotti N, Amato R. Preclinical model in HCC: the SGK1 kinase inhibitor SI113 blocks tumor progression in vitro and in vivo and synergizes with radiotherapy. Oncotarget. 2015 Nov 10;6(35):37511-25. doi: 10.18632/oncotarget.5527. PubMed PMID: 26462020; PubMed Central PMCID: PMC4741945.
6: D'Antona L, Amato R, Talarico C, Ortuso F, Menniti M, Dattilo V, Iuliano R, Gigliotti F, Artese A, Costa G, Schenone S, Musumeci F, Abbruzzese C, Botta L, Trapasso F, Alcaro S, Paggi MG, Perrotti N. SI113, a specific inhibitor of the Sgk1 kinase activity that counteracts cancer cell proliferation. Cell Physiol Biochem. 2015;35(5):2006-18. doi: 10.1159/000374008. Epub 2015 Mar 27. PubMed PMID: 25871776.