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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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NSC756093

NSC756093 Chemical Structure

CAS No. : 1629908-92-4

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Description

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[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
FaDu IC50
0.496 μM
Compound: SU093
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
[PMID: 31531203]
FaDu IC50
6.5 μM
Compound: SU093
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
[PMID: 31531203]
In Vitro

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.

Cell Proliferation Assay[2]

Cell Line: Human prostate cancer DU145 cells, human prostate cancer PC3 cells, GBP1 knockout DU145 cells, GBP1 knockout PC3 cells
Concentration: 2 μM, 4 μM, 8 μM (preliminary dose optimization); 4 μM (growth monitoring)
Incubation Time: Up to 96 h (DU145 growth monitoring); up to 144 h (PC3 growth monitoring)
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.

Cell Migration Assay[2]

Cell Line: Human prostate cancer DU145 cells, human prostate cancer PC3 cells
Concentration: 4 μM
Incubation Time: 24 h
Result: Significantly reduced the number of migrated DU145 and PC3 cells per field compared to untreated control cells.

Cell Cycle Analysis[3]

Cell Line: OVCAR8, SKOV3, ID8
Concentration: 1 μM, 2.5 μM, 5 μM
Incubation Time: 12 h
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.

Apoptosis Analysis[3]

Cell Line: OVCAR8, SKOV3, ID8
Concentration: 2.5 μM, 5 μM
Incubation Time: 24 h
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.
In Vivo

NSC756093 (SU093) (20 mg/kg; i.p.; daily; 42 days) reduces ovarian cancer tumor weight by 1.5-fold, delays tumor progression, and reduces lung metastasis in female C57BL/6 mice with ID8 xenografts, with no observable liver toxicity[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (female, 6-7 weeks old, syngeneic xenograft model via subcutaneous implantation of luciferase-expressing ID8 cells)[3]
Dosage: 20 mg/kg
Administration: i.p.; daily; 42 days
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).
Molecular Weight

337.37

Formula

C20H19NO4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1OCC(N2CCO)=C1C(C3=CC=CC=C3)C4=C2C=C(OC)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9641 mL 14.8205 mL 29.6410 mL
5 mM 0.5928 mL 2.9641 mL 5.9282 mL
View the 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.

  • Molarity Calculator

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Purity & Documentation
References

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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
NSC756093
Cat. No.:
HY-12929
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