NSC756093
Based on 1 Customer Validation
NSC756093 (SU093) is a GBP1:PIM1 interaction inhibitor. NSC756093 binds to GBP1-PIM1 with a Kd of 38 nM. NSC756093 suppresses proliferation, reduces migration, induces G1 phase cell-cycle arrest, and increases apoptotic cell death in ovarian cancer cells. NSC756093 reduces cellular proteasomal activity, induces accumulation of ubiquitinated proteins, and restrains tumor progression and lung metastasis in murine ovarian cancer xenograft models. NSC756093 increases sensitivity of prostate cancer cells to Docetaxel (HY-B0011) and sensitizes GBP1-overexpressing ovarian cancer cells to Paclitaxel (HY-B0015). NSC756093 can be used for the research of prostate cancer and ovarian cancer.
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- Purity: 99.58%
- CAS No.: 1629908-92-4
- 화학식: C20H19NO4
- 분자량:337.37
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보관:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| FaDu | IC50 |
0.496 μM
Compound: SU093
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Synergistic antiproliferative activity against human FADU cells assessed as reduction in colony formation unit followed by irradiation with 5 Gy IR and measured after 10 to 14 days by crystal violet staining based assay
Synergistic antiproliferative activity against human FADU cells assessed as reduction in colony formation unit followed by irradiation with 5 Gy IR and measured after 10 to 14 days by crystal violet staining based assay
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[PMID: 31531203] |
| FaDu | IC50 |
6.5 μM
Compound: SU093
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Inhibition of colony formation in human FADU cells incubated for 10 to 14 days by crystal violet staining based assay
Inhibition of colony formation in human FADU cells incubated for 10 to 14 days by crystal violet staining based assay
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[PMID: 31531203] |
NSC756093 (0.1-100 nM) potently and dose-dependently inhibits the recombinant GBP1:PIM1 protein-protein interaction in an SPR-based assay, achieving 65% inhibition at 100 nM[1].
NSC756093 (100 nM; 3 h) inhibits the endogenous GBP1:PIM1 interaction in SKOV3 ovarian cancer cells[1].
NSC756093 (10 nM-100 μM) inhibits growth of NCI-60 human cancer cell lines, with increased sensitivity in cell lines expressing higher levels of both GBP1 and PIM1[1].
NSC756093 (2-8 μM; up to 144 h) potently inhibits the proliferation of parental DU145 and PC3 prostate cancer cells, but has no effect on GBP1 knockout DU145 and PC3 cells, indicating its anti-proliferative activity is dependent on GBP1 expression[2].
NSC756093 (4 μM; 24 h) potently inhibits the migration of DU145 and PC3 prostate cancer cells[2].
NSC756093 (48 h) inhibits viability of multiple ovarian cancer cell lines, demonstrating IC50 values of 1.18 μM (OVCAR3), 13.69 μM (OVCAR4), 14.96 μM (OVCAR5), 2.03 μM (OVCAR8), 1.9 μM (SKOV3), 6.95 μM (ID8) after 48 h treatment[3].
NSC756093 (0.5-1 μM; 7 days) dose-dependently inhibits colony formation of OVCAR8, SKOV3, and ID8 ovarian cancer cells when treated for 7 days, with significant effects at 0.5 and 1 μM[3].
NSC756093 (1-5 μM; 12 h) causes dose-dependent cell cycle arrest in sub-G1 and G1 phases of OVCAR8, SKOV3, and ID8 ovarian cancer cells after 12 h treatment at 1, 2.5, and 5 μM[3].
NSC756093 (2.5-5 μM; 24 h) dose-dependently induces apoptotic cell death in OVCAR8, SKOV3, and ID8 ovarian cancer cells after 24 h treatment at 2.5 and 5 μM[3].
NSC756093 (1 μM; 12 h pre-treatment, 16 h migration) inhibits migration of OVCAR8, SKOV3, and ID8 ovarian cancer cells by 40-46% in a Boyden chamber assay[3].
NSC756093 (SU093) significantly inhibits proteasomal activity in ovarian cancer cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human prostate cancer DU145 cells, human prostate cancer PC3 cells, GBP1 knockout DU145 cells, GBP1 knockout PC3 cells
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Concentration:2 μM, 4 μM, 8 μM (preliminary dose optimization); 4 μM (growth monitoring)
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Incubation Time:Up to 96 h (DU145 growth monitoring); up to 144 h (PC3 growth monitoring)
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Result:Significantly reduced the growth rate of parental DU145 and PC3 cells.
Had no apparent growth-inhibitory effect on GBP1 knockout DU145 and PC3 cells.
Caused more severe growth inhibition of parental cells at 8 μM, while induced milder effect at 2 μM.
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Cell Line:Human prostate cancer DU145 cells, human prostate cancer PC3 cells
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Concentration:4 μM
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Incubation Time:24 h
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Result:Significantly reduced the number of migrated DU145 and PC3 cells per field compared to untreated control cells.
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Cell Line:OVCAR8, SKOV3, ID8
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Concentration:1 μM, 2.5 μM, 5 μM
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Incubation Time:12 h
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Result:Induced significant, dose-dependent arrest in sub-G1 and G1 phases, with concomitant decreases in S or G2/M phase cells across all three cell lines.
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Cell Line:OVCAR8, SKOV3, ID8
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Concentration:2.5 μM, 5 μM
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Incubation Time:24 h
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Result:Significantly increased the proportion of apoptotic cells at both doses in all three cell lines.
Showed higher apoptosis observed at 5 μM compared to 2.5 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6-7 weeks old, syngeneic xenograft model via subcutaneous implantation of luciferase-expressing ID8 cells)[3]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 42 days
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Result:Significantly delayed tumor progression compared to vehicle control.
Reduced tumor weight by 1.5-fold relative to vehicle controls at study termination.
Reduced the number of lung metastatic nodules relative to vehicle controls.
Caused no significant changes in liver toxicity parameters (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase).
Chemical Information
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CAS No. 1629908-92-4
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Appearance Solid
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분자량 337.37
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화학식 C20H19NO4
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Color White to off-white
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SMILES
O=C1OCC(N2CCO)=C1C(C3=CC=CC=C3)C4=C2C=C(OC)C=C4
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Synonyms
SU093
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
용액&용해도
DMSO : 62.5 mg/mL (185.26 mM; Need ultrasonic; 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. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (284 KB)
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SDS (536 KB)
- English - EN (536 KB)
- Français - FR (536 KB)
- Deutsch - DE (536 KB)
- Norwegian - NO (536 KB)
- Español - ES (536 KB)
- Swedish - SV (536 KB)
- Italian - IT (536 KB)
- Portuguese - PT (536 KB)
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Handling Instructions (2659 KB)
References
[1]. Andreoli M, et al. Identification of the first inhibitor of the GBP1:PIM1 interaction. Implications for the development of a new class of anticancer agents against paclitaxel resistant cancer cells. J Med Chem. 2014;57(19):7916-7932. [Content Brief]
[2]. Zhao J, et al. Oncogenic Role of Guanylate Binding Protein 1 in Human Prostate Cancer. Front Oncol. 2020 Jan 10;9:1494. [Content Brief]
[3]. Tailor D, et al. Y box binding protein 1 inhibition as a targeted therapy for ovarian cancer. Cell Chem Biol. 2021;28(8):1206-1220.e6. [Content Brief]
[4]. Tailor D, et al. Guanylate-binding protein 1 modulates proteasomal machinery in ovarian cancer. iScience. 2023;26(11):108292. Published 2023 Oct 24. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9641 mL | 14.8205 mL | 29.6410 mL | 74.1026 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL | 14.8205 mL | |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL | 7.4103 mL | |
| 15 mM | 0.1976 mL | 0.9880 mL | 1.9761 mL | 4.9402 mL | |
| 20 mM | 0.1482 mL | 0.7410 mL | 1.4821 mL | 3.7051 mL | |
| 25 mM | 0.1186 mL | 0.5928 mL | 1.1856 mL | 2.9641 mL | |
| 30 mM | 0.0988 mL | 0.4940 mL | 0.9880 mL | 2.4701 mL | |
| 40 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | 1.8526 mL | |
| 50 mM | 0.0593 mL | 0.2964 mL | 0.5928 mL | 1.4821 mL | |
| 60 mM | 0.0494 mL | 0.2470 mL | 0.4940 mL | 1.2350 mL | |
| 80 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9263 mL | |
| 100 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7410 mL |
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