2. Apoptosis
  3. Apoptosis
  4. GR-891

GR-891 is an acyclic nucleoside 5-Fluorouracil (HY-90006) derivative. GR-891 exerts antiproliferative activity in human cancer cells and inhibits proliferation of human rhabdomyosarcoma cells. GR-891 induces terminal myogenic differentiation in human rhabdomyosarcoma cells, including modulation of desmin and vimentin expression. GR-891 is phosphorylated by kinases, incorporated into RNA, and releases acrolein. GR-891 can be used for the research of cancer and rhabdomyosarcoma.

For research use only. We do not sell to patients.

GR-891

GR-891 Chemical Structure

CAS No. : 138969-77-4

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GR-891 Related Antibodies

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Description

GR-891 is an acyclic nucleoside 5-Fluorouracil (HY-90006) derivative. GR-891 exerts antiproliferative activity in human cancer cells and inhibits proliferation of human rhabdomyosarcoma cells. GR-891 induces terminal myogenic differentiation in human rhabdomyosarcoma cells, including modulation of desmin and vimentin expression. GR-891 is phosphorylated by kinases, incorporated into RNA, and releases acrolein. GR-891 can be used for the research of cancer and rhabdomyosarcoma[1][2].

In Vitro

GR-891 (22.5-90 µM; 6 days) inhibits proliferation of human rhabdomyosarcoma RD cells in a time- and dose-dependent manner, with >90% cell viability maintained across tested concentrations after 6 days of continuous treatment, and irreversible growth suppression following retreatment[2].
GR-891 (22.5-45 µM; 6 days) induces terminal myogenic differentiation in human rhabdomyosarcoma RD cells, characterized by morphological, SEM, and TEM features of mature muscle cells, including formation of myotube-like giant cells that represent up to 65% of the cell population after 6 days of treatment[2].
GR-891 (22.5-90 µM; 6 days) modulates intermediate filament protein expression in human rhabdomyosarcoma RD cells, with 22.5 µM and 45 µM causing significant increases in desmin-positive cells (to 68.8% and 63.0%, respectively) and significant decreases in vimentin-positive cells (to 40.8% and 57.5%, respectively), consistent with myogenic differentiation[2].
GR-891 (22.5-90 µM; 6 days) does not modify mdr1 mRNA expression in human rhabdomyosarcoma RD cells after 6 days of treatment at concentrations of 22.5, 45, or 90 µmol l-1[2].

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

GR-891 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: human rhabdomyosarcoma RD cell line
Concentration: 22.5 μM; 45 μM; 90 μM
Incubation Time: 6 days
Result: Caused substantial inhibition of RD cell proliferation during the first 3 days, with inhibition sustained until day 6.
Maintained cell viability >90% for all concentrations after 6 days of treatment.
Resulted in irreversible complete growth suppression when cells were retreated for 6 days after initial 3-day treatment and recovery.

Cell Differentiation Assay[2]

Cell Line: human rhabdomyosarcoma RD cell line
Concentration: 22.5 μM; 45 μM; 90 μM
Incubation Time: 6 days
Result: Induced elongated morphology, parallel/whorl-like growth patterns, and up to 65% multinucleated myotube-like giant cells in RD cells after 3-6 days of treatment at 22.5 µM or 45 µM.
Revealed increased cytoplasm, stronger substrate adhesion, increased phylopodia/membrane folds, and parallel myofibrils via SEM at 22.5 µM or 45 µM.
Showed multinucleated giant cells with increased cytoplasmic organelles, glycogen deposits, elongated mitochondria, lipid vesicles, organized intermediate filaments, and parallel myofilament bundles with Z-band-like electron-dense zones via TEM at 22.5 µM or 45 µM.
Exhibited prominent differentiation features at 22.5 µM and 45 µM, which were also observed in retreated cultures.

RT-PCR[2]

Cell Line: human rhabdomyosarcoma RD cell line
Concentration: 22.5 μM; 45 μM; 90 μM
Incubation Time: 6 days
Result: Showed no change in the intensity of mdr1 PCR product compared to untreated cells after 6 days of treatment at any concentration.
Produced consistent β2-microglobulin PCR product intensity across all samples, confirming RNA integrity.
In Vivo

GR-891 (compound 2b) (200 mg/kg; i.p.; daily; 7 days) shows no apparent in vivo toxicity in healthy Swiss albino mice at a dose equivalent to the 5-FU LD50 of 200 mg/kg, with no treatment-related morbidity or mortality observed[1].

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

Animal Model: Swiss albino (female, adult, 26-27 g average weight, healthy)[1]
Dosage: 200 mg/kg (5-FU LD50 equivalent)
Administration: i.p.; daily; 7 days
Result: Showed no definite weight change tendency.
Showed no changes in physical appearance (no hair loss, no anal zone irritation).
Showed no reduction in vital activity.
Caused no treatment-related death; animals died only at the end of their natural biological cycle.
Molecular Weight

290.29

Formula

C12H19FN2O5
CAS No.
SMILES

O=C1NC(N(C(CCOCCO)OC(C)C)C=C1F)=O
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
References
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GR-891 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:

GR-891138969-77-4GR891GR 891ApoptosisvimentindesminRNAhuman rhabdomyosarcoma cellsmdr1 genefibronectinkinaseshuman cancer cellsSwiss albino micehuman rhabdomyosarcoma RD cellsInhibitorinhibitorinhibit

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