YRDC-IN-1
Based on 1 publication(s) in Google Scholar
YRDC-IN-1 is a blood-brain barrier-permeable YRDC inhibitor. YRDC is a key enzyme that catalyzes the formation of N6-threonylcarbamoyladenosine at position 37 of tRNA (t6A37). YRDC-IN-1 selectively inhibits the translation of ANN codon-enriched FABP7, thereby reducing lipid droplet formation, increasing ROS, and reversing the acquired resistance of GBM to Temozolomide (TMZ) (HY-17364). YRDC-IN-1 can be used for the research of glioblastoma.
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- CAS No.: 3120494-74-5
- Formule: C22H20N2O3
- Masse moléculaire:360.41
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) YRDC-IN-1
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Activité biologique
YRDC-IN-1 (HY-Q66655) potently inhibits the proliferation of human glioma stem cells (MES28) after 48 h, with an IC50 of 65.96 μM[1].
YRDC-IN-1 (70 μM; 48 h) reduces the expression of FABP7 protein in TMZ-resistant glioblastoma cells LN18-R and glioblastoma stem cells MES28, but does not affect the level of YRDC[1].
YRDC-IN-1 (70 μM; 48 h) preferentially inhibits the translation of ANN codon-enriched FABP7 in 293 T cells, and exerts a stronger inhibitory effect on the ANN-high-content FABP7 reporter gene compared with variants with low ANN content[1].
YRDC-IN-1 (70 μM) sensitizes TMZ-resistant glioblastoma cells LN18-R and glioblastoma stem cells MES28 to TMZ, while overexpression of ANN-low FABP7 reverses this effect; in LN18-R cells, the IC50 of TMZ decreases from 535.6 μM to 239.1 μM, and in MES28 cells, it decreases from 1066.0 μM to 467.8 μM[1].
YRDC-IN-1 (70 μM; 48 h) reduces lipid droplet levels in TMZ-resistant LN18-R glioblastoma cells and MES28 glioblastoma stem cells, and overexpression of ANN-low FABP7 reverses this effect[1].
YRDC-IN-1 (0-50 μM) acts synergistically with TMZ (0-600 μM) to inhibit the proliferation of TMZ-resistant LN18-R glioblastoma cells and MES28 glioblastoma stem cells, with their average ZIP synergy scores being 15.14 and 20.66, respectively[1].
YRDC-IN-1 (70 μM; 4 days) potently inhibits the proliferation of human HuH-7 hepatocellular carcinoma cells, PANC-1 pancreatic cancer cells, HCT116 colorectal cancer cells, and SGC7901 gastric cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human TMZ-resistant glioblastoma cells (LN18-R), glioblastoma stem cells (MES28)
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Concentration:70 μM
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Incubation Time:48 h
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Result:Did not alter YRDC protein levels.
Significantly reduced FABP7 protein levels in both LN18-R and MES28 cells.
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Cell Line:human hepatocellular carcinoma (HuH-7), pancreatic carcinoma (PANC-1), colorectal carcinoma (HCT116), gastric carcinoma (SGC7901) cells
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Concentration:70 μM
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Incubation Time:4 days
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Result:Significantly inhibited cell proliferation in all four cancer cell lines.
Reduced relative cell viability to ~2% in HuH-7 by day 4.
Reduced relative cell viability to ~3% in PANC-1 by day 4.
Reduced relative cell viability to ~3% in HCT116 by day 4.
Reduced relative cell viability to ~3% in SGC7901 by day 4.
YRDC-IN-1 (10 mg/kg; i.p.; every 3-4 days; six administrations) significantly reduces MES28-derived glioblastoma tumor volume and extends mouse survival[1].
YRDC-IN-1 (10 mg/kg; i.p.; twice weekly; three weeks) is well-tolerated in healthy BALB/c-nu mice with no significant toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu (5-week-old female, intracranial injection of 5,000 patient-derived GSC147 cells)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every 3-4 days; six administrations
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Result:Reduced mean tumor volume to ~20 mm3 compared to vehicle control ~60 mm3.
Extended median survival time significantly.
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Animal Model:BALB/c-nu (5-week-old female, intracranial injection of 5,000 patient-derived MES28 cells)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every 3-4 days; six administrations
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Result:Reduced mean tumor volume to ~10 mm3 compared to vehicle control ~60 mm3.
Extended median survival time significantly.
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Animal Model:BALB/c-nu (5-week-old female, tumor-free)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice weekly; three weeks
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Result:Did not induce significant body weight loss.
Caused no obvious pathological damage in major parenchymal organs.
Chemical Information
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CAS No. 3120494-74-5
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Appearance Solid
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Masse moléculaire 360.41
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Formule C22H20N2O3
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SMILES
O=C(N1CCC2(CC1)OCC3=C2C=CC=C3)C4=CC=C(C5=CC=CN=C5)O4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Oncogene
Targeting YRDC blocks codon-biased FABP7 translation and lipid droplet formation to overcome chemoresistance in glioblastoma. [Abstract]2026 Jun;45(22):2155-2170. PMID: 42014887
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YRDC-IN-1 Related Classifications
HY-Q66655 Related Classifications
Powered by Bioz
- YRDC-IN-1
- 3120494-74-5
- DNA/RNA Synthesis
- Reactive Oxygen Species (ROS)
- blood-brain-barrier
- lipid droplets
- FABP7
- human glioblastoma stem cells
- YRDC
- reactive oxygen species
- tRNA-modifying enzymes
- LN18-R TMZ-resistant glioblastoma cells
- glioblastoma patient-derived orthotopic xenograft models
- glioblastoma
- Inhibitor
- inhibitor
- inhibit