2. Metabolic Enzyme/Protease Apoptosis
  3. Aminotransferases (Transaminases) Apoptosis
  4. Aspulvinone O

Aspulvinone O is a selective inhibitor of glutamate oxaloacetate aminotransferase GOT1. Aspulvinone O inhibits glutamine metabolism and reduces NADPH production, thereby inducing oxidative stress and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cells. Aspulvinone O inhibits PDAC cell proliferation in vitro and tumor growth in xenograft models.

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Aspulvinone O Chemical Structure

Aspulvinone O Chemical Structure

CAS No. : 914071-54-8

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Aspulvinone O Related Antibodies

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Description

Aspulvinone O is a selective inhibitor of glutamate oxaloacetate aminotransferase GOT1. Aspulvinone O inhibits glutamine metabolism and reduces NADPH production, thereby inducing oxidative stress and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cells. Aspulvinone O inhibits PDAC cell proliferation in vitro and tumor growth in xenograft models[1][2].

IC50 & Target

GOT/AST

 

Cellular Effect
Cell Line Type Value Description References
J774.1 IC50
3 μM
Compound: 11
Anti-inflammatory activity against mouse J774A.1 macrophage assessed as reduction in LPS-induced LDH release incubated for 1 hr in presence of nigericin by LDH assay
Anti-inflammatory activity against mouse J774A.1 macrophage assessed as reduction in LPS-induced LDH release incubated for 1 hr in presence of nigericin by LDH assay
[PMID: 35293744]
In Vitro

Aspulvinone O (0.1-100 μM; 48 h) inhibits the proliferation of pancreatic ductal adenocarcinoma cell lines (SW1990, PANC-1, AsPC-1) with IC50 of 20.54-26.80 μM, showing selectivity for cancer cells over normal cells[1].
Aspulvinone O (10-40 μM; 48 h) arrests the cell cycle of SW1990 cells at the S phase and induces apoptosis[1].
Aspulvinone O (10-40 μM; 24 h) reduces the levels of glutamine metabolic intermediates (OAA, malate) and the NADPH/NADP+ ratio[1] in SW1990 cells[1].

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

Aspulvinone O Related Antibodies

Cell Viability Assay[1]

Cell Line: SW1990, PANC-1, AsPC-1 (human PDAC cells)
Concentration: 0.1-100 μM
Incubation Time: 48 h
Result: Dose-dependent growth inhibition with IC50 of 20.54 μM (SW1990), 26.80 μM (PANC-1), and 23.12 μM (AsPC-1), respectively, while showed no significant cytotoxicity (IC50 >100 μM) against normal HPDE6C7 cells.
In Vivo

Aspulvinone O (2.5 mg/kg, 5 mg/kg; intraperitoneal injection; once daily; 14 days) significantly inhibits tumor growth in the SW1990 PDAC cell xenograft model of CB17/scid mice, reducing tumor weight by 40-60%, without obvious systemic toxicity[1].

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

Animal Model: CB17/scid male mice (8 weeks old, ~20 g), SW1990 cell-derived xenograft model[1]
Dosage: 2.5 mg/kg, 5 mg/kg
Administration: Intraperitoneal injection (i.p.), daily for 14 days, starting when tumors reached ~3 mm diameter
Result: Significantly reduced tumor volume and weight compared to control. Showed a 60% reduction in tumor weight in the 5 mg/kg group, at day 14 and a 55% reduction in tumor volume.
Decreased levels of oxaloacetate (OAA) and malate (~50% reduction), increased aspartate (Asp) and glutamine (Gln) (~30% increase), and a 45% decrease in NADPH/NADP+ ratio compared to control.
No significant changes in body weight or histomorphology, indicating good tolerability.
Molecular Weight

448.51

Formula

C27H28O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=C(C2=CC(C/C=C(C)/C)=C(O)C=C2O)C(O/C1=C/C3=CC(C/C=C(C)/C)=C(O)C=C3)=O
Structure Classification
Initial Source

Aspergillus terreus
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (55.74 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 2.2296 mL 11.1480 mL 22.2960 mL
5 mM 0.4459 mL 2.2296 mL 4.4592 mL
View the 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: ≥96.0%

SDS (251 KB)

COA (247 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2296 mL 11.1480 mL 22.2960 mL 55.7401 mL
5 mM 0.4459 mL 2.2296 mL 4.4592 mL 11.1480 mL
10 mM 0.2230 mL 1.1148 mL 2.2296 mL 5.5740 mL
15 mM 0.1486 mL 0.7432 mL 1.4864 mL 3.7160 mL
20 mM 0.1115 mL 0.5574 mL 1.1148 mL 2.7870 mL
25 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2296 mL
30 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8580 mL
40 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3935 mL
50 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
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Aspulvinone O Related Classifications

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.

Keywords:

Aspulvinone O914071-54-8Aminotransferases (Transaminases)ApoptosisAminotransferases (Transaminases) GOT1ROSenergy metabolismPDACgrowthglutamine metabolismInhibitorinhibitorinhibit

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