2. Cell Cycle/DNA Damage NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. DNA/RNA Synthesis Reactive Oxygen Species (ROS)
  4. YRDC-IN-1

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.

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

YRDC-IN-1

YRDC-IN-1 Chemical Structure

CAS No. : 3120494-74-5

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Description

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[1].

In Vitro

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.

YRDC-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: human TMZ-resistant glioblastoma cells (LN18-R), glioblastoma stem cells (MES28)
Concentration: 70 μM
Incubation Time: 48 h
Result: Did not alter YRDC protein levels.
Significantly reduced FABP7 protein levels in both LN18-R and MES28 cells.

Cell Proliferation Assay[1]

Cell Line: human hepatocellular carcinoma (HuH-7), pancreatic carcinoma (PANC-1), colorectal carcinoma (HCT116), gastric carcinoma (SGC7901) cells
Concentration: 70 μM
Incubation Time: 4 days
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.
In Vivo

YRDC-IN-1 (HY-Q66655) (10 mg/kg; i.p.; every 3-4 days; six administrations) significantly reduces GSC147-derived glioblastoma tumor volume and extends mouse survival[1].
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.

Animal Model: BALB/c-nu (5-week-old female, intracranial injection of 5,000 patient-derived GSC147 cells)[1]
Dosage: 10 mg/kg
Administration: i.p.; every 3-4 days; six administrations
Result: Reduced mean tumor volume to ~20 mm3 compared to vehicle control ~60 mm3.
Extended median survival time significantly.
Animal Model: BALB/c-nu (5-week-old female, intracranial injection of 5,000 patient-derived MES28 cells)[1]
Dosage: 10 mg/kg
Administration: i.p.; every 3-4 days; six administrations
Result: Reduced mean tumor volume to ~10 mm3 compared to vehicle control ~60 mm3.
Extended median survival time significantly.
Animal Model: BALB/c-nu (5-week-old female, tumor-free)[1]
Dosage: 10 mg/kg
Administration: i.p.; twice weekly; three weeks
Result: Did not induce significant body weight loss.
Caused no obvious pathological damage in major parenchymal organs.
Molecular Weight

360.41

Formula

C22H20N2O3
CAS No.
SMILES

O=C(N1CCC2(CC1)OCC3=C2C=CC=C3)C4=CC=C(C5=CC=CN=C5)O4
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YRDC-IN-1 Related Classifications

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  • 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:

YRDC-IN-13120494-74-5DNA/RNA SynthesisReactive Oxygen Species (ROS)blood-brain-barrierlipid dropletsFABP7human glioblastoma stem cellsYRDCreactive oxygen speciestRNA-modifying enzymesLN18-R TMZ-resistant glioblastoma cellsglioblastoma patient-derived orthotopic xenograft modelsglioblastomaInhibitorinhibitorinhibit

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