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MedKoo Cat#: 563878 | Name: SI113
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SI113 is a specific inhibitor of the Sgk1 kinase activity, counteracting cancer cell proliferation.

Chemical Structure

SI113
SI113
CAS#1392816-46-4

Theoretical Analysis

MedKoo Cat#: 563878

Name: SI113

CAS#: 1392816-46-4

Chemical Formula: C23H24N6O

Exact Mass: 400.2012

Molecular Weight: 400.49

Elemental Analysis: C, 68.98; H, 6.04; N, 20.99; O, 3.99

Price and Availability

Size Price Availability Quantity
5mg USD 110.00 Ready to ship
10mg USD 180.00 Ready to ship
25mg USD 350.00 Ready to ship
50mg USD 600.00 Ready to ship
100mg USD 950.00 Ready to ship
200mg USD 1,550.00 Ready to ship
500mg USD 2,950.00 Ready to ship
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Related CAS #
1392816-46-4 1283727-37-6
Synonym
SI113; SI-113; SI 113
IUPAC/Chemical Name
(Z)-2-((4-(Phenethylamino)-1-styryl-1H-pyrazolo[3,4-d]pyrimidin-6-yl)amino)ethan-1-ol
InChi Key
LAOYAWHHLUVMFT-QINSGFPZSA-N
InChi Code
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-
SMILES Code
OCCNC1=NC(NCCC2=CC=CC=C2)=C3C(N(/C=C\C4=CC=CC=C4)N=C3)=N1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
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
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
SI-113 is a SGK1 inhibitor (IC50 = 600 nM).
In vitro activity:
SI113 potential use in clinical trials for combination therapy of glioblastoma multiforme (GBM). In GBM cells, SI113 strongly affected the PI3K/mTOR pathway, prompting a pro-survival autophagic response in neurospheres. Combining SI113 with quinacrine showed a synergistic effect, inhibiting GBM growth in various cell types, including neurospheres. Reference: J Exp Clin Cancer Res. 2019 May 17;38(1):202. https://pubmed.ncbi.nlm.nih.gov/31101126/
In vivo activity:
Direct SGK1 inhibition with SI113 can be effective in hepatic cancer therapy, either alone or in combination with radiotherapy. SI113-dependent SGK1 inhibition determined a dramatic increase in apoptosis/necrosis, inhibited cell proliferation and altered the cell cycle profile of treated cells. No short-term toxicity was observed in treated animals during SI113 administration. Reference: Oncotarget. 2015 Nov 10;6(35):37511-25. https://pubmed.ncbi.nlm.nih.gov/26462020/
Solvent mg/mL mM comments
Solubility
DMF 30.0 74.91
DMSO 15.0 37.45
Ethanol 30.0 74.91
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 400.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Abbruzzese C, Matteoni S, Persico M, Ascione B, Schenone S, Musumeci F, Amato R, Perrotti N, Matarrese P, Paggi MG. The small molecule SI113 hinders epithelial-to-mesenchymal transition and subverts cytoskeletal organization in human cancer cells. J Cell Physiol. 2019 Dec;234(12):22529-22542. doi: 10.1002/jcp.28816. Epub 2019 May 16. PMID: 31099037. 2. Matteoni S, Abbruzzese C, Matarrese P, De Luca G, Mileo AM, Miccadei S, Schenone S, Musumeci F, Haas TL, Sette G, Carapella CM, Amato R, Perrotti N, Signore M, Paggi MG. The kinase inhibitor SI113 induces autophagy and synergizes with quinacrine in hindering the growth of human glioblastoma multiforme cells. J Exp Clin Cancer Res. 2019 May 17;38(1):202. doi: 10.1186/s13046-019-1212-1. PMID: 31101126; PMCID: PMC6525441. 3. Hochstetler A, Smith H, Reed M, Hulme L, Territo P, Bedwell A, Persohn S, Perrotti N, D'Antona L, Musumeci F, Schenone S, Blazer-Yost BL. Inhibition of serum- and glucocorticoid-induced kinase 1 ameliorates hydrocephalus in preclinical models. Fluids Barriers CNS. 2023 Aug 18;20(1):61. doi: 10.1186/s12987-023-00461-0. PMID: 37596666; PMCID: PMC10439616. 4. 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. PMID: 26462020; PMCID: PMC4741945.
In vitro protocol:
1. Abbruzzese C, Matteoni S, Persico M, Ascione B, Schenone S, Musumeci F, Amato R, Perrotti N, Matarrese P, Paggi MG. The small molecule SI113 hinders epithelial-to-mesenchymal transition and subverts cytoskeletal organization in human cancer cells. J Cell Physiol. 2019 Dec;234(12):22529-22542. doi: 10.1002/jcp.28816. Epub 2019 May 16. PMID: 31099037. 2. Matteoni S, Abbruzzese C, Matarrese P, De Luca G, Mileo AM, Miccadei S, Schenone S, Musumeci F, Haas TL, Sette G, Carapella CM, Amato R, Perrotti N, Signore M, Paggi MG. The kinase inhibitor SI113 induces autophagy and synergizes with quinacrine in hindering the growth of human glioblastoma multiforme cells. J Exp Clin Cancer Res. 2019 May 17;38(1):202. doi: 10.1186/s13046-019-1212-1. PMID: 31101126; PMCID: PMC6525441.
In vivo protocol:
1. Hochstetler A, Smith H, Reed M, Hulme L, Territo P, Bedwell A, Persohn S, Perrotti N, D'Antona L, Musumeci F, Schenone S, Blazer-Yost BL. Inhibition of serum- and glucocorticoid-induced kinase 1 ameliorates hydrocephalus in preclinical models. Fluids Barriers CNS. 2023 Aug 18;20(1):61. doi: 10.1186/s12987-023-00461-0. PMID: 37596666; PMCID: PMC10439616. 2. 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. PMID: 26462020; PMCID: PMC4741945.
1: D'Antona L, Dattilo V, Catalogna G, Scumaci D, Fiumara CV, Musumeci F, Perrotti G, Schenone S, Tallerico R, Spoleti CB, Costa N, Iuliano R, Cuda G, Amato R, Perrotti N. In Preclinical Model of Ovarian Cancer, the SGK1 Inhibitor SI113 Counteracts the Development of Paclitaxel Resistance and Restores Drug Sensitivity. Transl Oncol. 2019 Aug;12(8):1045-1055. doi: 10.1016/j.tranon.2019.05.008. Epub 2019 Jun 1. PubMed PMID: 31163384; PubMed Central PMCID: PMC6545392. 2: Matteoni S, Abbruzzese C, Matarrese P, De Luca G, Mileo AM, Miccadei S, Schenone S, Musumeci F, Haas TL, Sette G, Carapella CM, Amato R, Perrotti N, Signore M, Paggi MG. The kinase inhibitor SI113 induces autophagy and synergizes with quinacrine in hindering the growth of human glioblastoma multiforme cells. J Exp Clin Cancer Res. 2019 May 17;38(1):202. doi: 10.1186/s13046-019-1212-1. PubMed PMID: 31101126; PubMed Central PMCID: PMC6525441. 3: Abbruzzese C, Matteoni S, Persico M, Ascione B, Schenone S, Musumeci F, Amato R, Perrotti N, Matarrese P, Paggi MG. The small molecule SI113 hinders epithelial-to-mesenchymal transition and subverts cytoskeletal organization in human cancer cells. J Cell Physiol. 2019 Dec;234(12):22529-22542. doi: 10.1002/jcp.28816. Epub 2019 May 16. PubMed PMID: 31099037. 4: 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. 5: 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. 6: 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. 7: 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. 8: 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. 9: 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.