2. Epigenetics PI3K/Akt/mTOR Apoptosis
  3. AMPK Apoptosis
  4. ASS1 activator 1

ASS1 activator 1 (Compound 10f) is a ASS1 activator with an EC50 of 1.90 μM. ASS1 activator 1 enhances the activity of ASS1 and promotes AMPK phosphorylation. ASS1 activator 1 induces cell Apoptosis. ASS1 activator 1 exhibits anticancer activity against triple-negative breast cancer, colorectal cancer and liver cancer.

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ASS1 activator 1

ASS1 activator 1 Chemical Structure

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ASS1 activator 1 Related Antibodies

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Description

ASS1 activator 1 (Compound 10f) is a ASS1 activator with an EC50 of 1.90 μM. ASS1 activator 1 enhances the activity of ASS1 and promotes AMPK phosphorylation. ASS1 activator 1 induces cell Apoptosis. ASS1 activator 1 exhibits anticancer activity against triple-negative breast cancer, colorectal cancer and liver cancer[1].

In Vitro

ASS1 activator 1 potently activates recombinant ASS1 protein, with an EC50 of 1.90 μM[1].
ASS1 activator 1 (48 h) inhibits the viability of various human cancer cell lines (HT-29, HepG2, MDA-MB-231, T47D, MCF-7, SK-BR-3) with IC50 values ranging from 1.9 to 14.4 μM, while it shows low activity against normal MCF-10A mammary epithelial cells, with an IC50 of 28.5 μM[1].
ASS1 activator 1 (2-8 μM; 24 h) inhibits the migration of MDA-MB-231 triple-negative breast cancer cells in a concentration-dependent manner[1].
ASS1 activator 1 (5 μM; incubated at 37 °C until equilibrium is reached) shows a high plasma protein binding rate, with a binding rate of 98.3% in human plasma and 96.3% in rat plasma at 5 μM[1].

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

ASS1 activator 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231
Concentration: 2 μM, 4 μM, 8 μM
Incubation Time: 18 h
Result: Upregulated p-AMPK levels in a concentration-dependent manner without affecting total AMPK or ASS1 levels.
Decreased SQSTM/p62 levels and increased LC3B-II levels, indicating increased autophagic flux.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-t AUC0-∞ CL Vz Vss MRT0-∞ Bioavailability
Rat[1] 1 mg/kg i.v. 263 ± 34.3 ng/mL 0.10 ± 0.00 h 6.32 ± 0.34 h 619 ± 79.6 ng·h/mL 654 ± 86.3 ng·h/mL 1.55 ± 0.21 L/h/kg 14.1 ± 1.37 L/kg 10.0 ± 1.30 L/kg 6.47 ± 0.25 h /
Rat[1] 5 mg/kg p.o. 53.5 ± 3.61 ng/mL 4.0 ± 0.00 h 5.00 ± 0.69 h 538 ± 30.8 ng·h/mL 562 ± 41.1 ng·h/mL / / / 7.89 ± 0.72 h 17.4 %
In Vivo

ASS1 activator 1 (5 mg/kg; i.p.; every other day) exerts potent antiproliferative activity against MDA-MB-231 triple-negative breast cancer xenografts in nude mice without causing systemic toxicity[1].

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

Animal Model: BALB/c nude (female, 4−6 weeks old)[1]
Dosage: 5 mg/kg
Administration: intraperitoneally; every other day; 23 days
Result: Reduced final tumor weights and tumor volumes significantly compared to vehicle control.
Decreased Ki67-positive cells (cell proliferation marker) significantly in tumor tissue relative to controls.
Increased LC3B levels (autophagy marker) significantly in tumor tissue relative to controls.
Caused no significant changes in mouse body weight.
Showed no pathological changes in major organs (heart, liver, spleen, lung, kidney) via H&E staining, indicating no apparent systemic toxicity.
Molecular Weight

743.97

Formula

C41H65N3O9
SMILES

C[C@@H]1O[C@@H](O[C@@H]2C[C@]3(C=C[C@]4([C@@]([H])(C(C5=O)=C[C@]4([C@@]3(C2)[H])[H])CC(O[C@H](CCC/C([C@H]5C)=N\OCCCCN6CCNCC6)CC)=O)[H])[H])[C@H](OC)[C@H](OC)[C@H]1OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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ASS1 activator 1 Related Classifications

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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.

Keywords:

ASS1 activator 1AMPKApoptosisAMP-activated protein kinaseAMPK/mTOR signaling pathwayMCF-10AHepG2argininosuccinate synthase 1MCF-7MDA-MB-231T47DHT-29tumor cell apoptosistriple-negative breast cancerInhibitorinhibitorinhibit

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