UNBS5162
Based on 7 publication(s) in Google Scholar
UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.07%
- CAS. Nr.: 956590-23-1
- Formel: C17H18N4O3
- Molecular Weight:326.35
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) UNBS5162
More- Mol Med Rep. 2018 Jan;17(1):549-555. [Abstract]
- Drug Dev Ind Pharm. 2019 Aug;45(8):1306-1312. [Abstract]
- Cancer Manag Res. 2019 Mar 22:11:2339-2348. [Abstract]
- Thorac Cancer. 2018 Jan;9(1):105-111. [Abstract]
- Onco Targets Ther. 2017 Nov 6:10:5303-5309. [Abstract]
- Exp Ther Med. 2018 Nov;16(5):3921-3928. [Abstract]
- Med Sci (Paris). 2018 Oct:34 Focus issue F1:99-104. [Abstract]
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Biologische Aktivität
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CXCL |
UNBS5162 is a pan-antagonist of CXCL chemokine expression and exhibits weak antiproliferative activity against human cancer cell lines with mean IC50 of 17.9 μM. UNBS5162 markedly impairs PC-3 tumor cell growth kinetics, without inducing senescence, whereas the reverse feature is observed with respect to DU-145 cells[1]. UNBS5162 is cytotoxic to a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7), with IC50s of 0.5-5 μM. UNBS5162 also markedly increases the levels of expression of LC3-I and LC3-II in human cancer cells. UNBS5162 displays no anti-topoisomerase II activity. Moreover, UNBS5162 induces cancer cell death through lysosomal membrane permeabilization (LMP) in PC3 prostate cancer cells but not in U373 glioblastoma cells, with this LMP process occurring as an UNBS5162-induced decrease in Hsp70 expression[2]. UNBS5162 inhibits the proliferation of esophageal cancer squamous cells via the PI3K/AKT signaling pathway. UNBS5162 downregulates the protein expression of proteins associated with the PI3K/AKT signaling pathway, including the levels of phosphorylated (p)-AKT, p-mechanistic target of rapamycin kinase, ribosomal protein S6 kinase β1 and cyclin D1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 956590-23-1
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Appearance Solid
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Molecular Weight 326.35
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Formel C17H18N4O3
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Color Light yellow to yellow
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SMILES
O=C(N)NC1=CC2=CC=CC(C(N(CCN(C)C)C3=O)=O)=C2C3=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Mol Med Rep
UNBS5162 inhibits the proliferation of esophageal cancer squamous cells via the PI3K/AKT signaling pathway. [Abstract]2018 Jan;17(1):549-555. PMID: 29115622 -
Drug Dev Ind Pharm
UNBS5162 as a novel naphthalimide holds efficacy in human gastric carcinoma cell behaviors mediated by AKT/ERK signaling pathway. [Abstract]2019 Aug;45(8):1306-1312. PMID: 30995142 -
Cancer Manag Res
UNBS5162 and amonafide inhibits tumor progression in human melanoma by the AKT/mTOR pathway. [Abstract]2019 Mar 22:11:2339-2348. PMID: 30962721 -
Thorac Cancer
UNBS5162 inhibits the proliferation of human A549 non-small-cell lung cancer cells by promoting apoptosis. [Abstract]2018 Jan;9(1):105-111. PMID: 29130641
UNBS5162 purchased from MedChemExpress. Usage Cited in: Thorac Cancer. 2018 Jan;9(1):105-111. [Abstract]
Apoptosis is induced by UNBS5162 (24 h) treatment in human A549 non-small cell lung cancer (NSCLC) cells. Western blot analysis of apoptosis protein expression in human A549 NSCLC cells.
UNBS5162 purchased from MedChemExpress. Usage Cited in: Thorac Cancer. 2018 Jan;9(1):105-111. [Abstract]
UNBS5162 (10 μM; 24-72 h) inhibited the proliferation and growth of human A549 non‐small cell lung cancer (NSCLC) cells, as shown by (a) cell counting kit‐8 and (b) colony formation assays. *Indicates P < 0.05. Data was expressed as means ± standard deviations. NC, normal control; OD, optical density. (Inline graphic) NC and (Inline graphic) UNBS5162.
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Onco Targets Ther
UNBS5162 inhibits proliferation of human retinoblastoma cells by promoting cell apoptosis. [Abstract]2017 Nov 6:10:5303-5309. PMID: 29158682
UNBS5162 purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2017 Nov 6:10:5303-5309. [Abstract]
UNBS5162 inhibits proliferation of human retinoblastoma cells through the Akt–mTOR pathway. Following Western blot, expression of Akt-pathway and key proliferation-related genes- those for p-Akt, p-mTOR, p70, and cyclin D1-is found to be downregulated significantly in the UNBS5162-treated group compared with the negative-control (NC) group in WERIRb1 cells.
UNBS5162 purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2017 Nov 6:10:5303-5309. [Abstract]
UNBS5162 inhibits proliferation of human retinoblastoma cells through the Akt–mTOR pathway. Following Western blot, expression of Akt-pathway and key proliferation-related genes- those for p-Akt, p-mTOR, p70, and cyclin D1-is found to be downregulated significantly in the UNBS5162-treated group compared with the negative-control (NC) group in Y79 cells.
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Exp Ther Med
UNBS5162 induces growth inhibition and apoptosis via inhibiting PI3K/AKT/mTOR pathway in triple negative breast cancer MDA-MB-231 cells. [Abstract]2018 Nov;16(5):3921-3928. PMID: 30344670
UNBS5162 purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2018 Nov;16(5):3921-3928. [Abstract]
The effect of UNBS5162 on MDA-MB-231 cell apoptosis detected using western blot. Western blot assay is utilized to determine BCL-2, BAX and active caspase-3 protein expression levels in MDA MB 231 cells extracts.
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Med Sci (Paris)
2018 Oct:34 Focus issue F1:99-104. PMID: 30403183
UNBS5162 purchased from MedChemExpress. Usage Cited in: Med Sci (Paris). 2018 Oct:34 Focus issue F1:99-104. [Abstract]
The expression levels of Bcl-2, Bax and active caspase-3 proteins are measured using Western-blot analyses after incubation with UNBS5162 or DMSO for 24 h.
UNBS5162 purchased from MedChemExpress. Usage Cited in: Med Sci (Paris). 2018 Oct:34 Focus issue F1:99-104. [Abstract]
Western-blot analysis of proteins involved in the PI3K/Akt signaling pathway in HCT116 cells cultured in presence of UNBS5162 or DMSO (NC).
Lösungsmittel & Löslichkeit
DMSO : 21.5 mg/mL (65.88 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
Mice[1]
Orthotopic xenografts are obtained by injecting 2.5 × 106 human PC-3 or DU-145 cells into the prostate of 6-week-old male nu/nu mice (n = 9 animals per treatment group). All grafts are performed under anesthesia [saline/Rompun/Imalgene; 5:1:1 by volume]. The end point in these orthotopic experiments is the survival period of the tumor-bearing mice after the administration of UNBS3157, UNBS5162, or reference anticancer agents (taxol, mitoxantrone, and amonafide). However, for ethical reasons, animals are killed when 20% of body weight have been lost compared to that determined at the time of tumor grafting. All animals are weighed three times a week. Autopsies and histologic diagnoses are performed on each mouse to confirm the presence of tumor development; 100% is achieved. In the case of UNBS5162 experiments in the PC-3 model, after the sacrifice of animals, tumors are removed from both drug-treated [10 mg/kg, intravenous (i.v.)] and vehicle-treated mice, fixed in buffered formalin, embedded in paraffin, and 5-µm-thick sections taken. These histologic slides are then stained with hematoxylin and eosin for blood vessel counts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Mijatovic T, et al. UNBS5162, a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers. Neoplasia. 2008 Jun;10(6):573-86. [Content Brief]
[3]. He D, et al. UNBS5162 inhibits the proliferation of esophageal cancer squamous cells via the PI3K/AKT signaling pathway. Mol Med Rep. 2018 Jan;17(1):549-555. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0642 mL | 15.3210 mL | 30.6419 mL | 76.6049 mL |
| 5 mM | 0.6128 mL | 3.0642 mL | 6.1284 mL | 15.3210 mL | |
| 10 mM | 0.3064 mL | 1.5321 mL | 3.0642 mL | 7.6605 mL | |
| 15 mM | 0.2043 mL | 1.0214 mL | 2.0428 mL | 5.1070 mL | |
| 20 mM | 0.1532 mL | 0.7660 mL | 1.5321 mL | 3.8302 mL | |
| 25 mM | 0.1226 mL | 0.6128 mL | 1.2257 mL | 3.0642 mL | |
| 30 mM | 0.1021 mL | 0.5107 mL | 1.0214 mL | 2.5535 mL | |
| 40 mM | 0.0766 mL | 0.3830 mL | 0.7660 mL | 1.9151 mL | |
| 50 mM | 0.0613 mL | 0.3064 mL | 0.6128 mL | 1.5321 mL | |
| 60 mM | 0.0511 mL | 0.2553 mL | 0.5107 mL | 1.2767 mL |
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