hUP1-IN-2
hUP1-IN-2 is a Urd-competitive and Pᵢ-noncompetitive hUP1 inhibitor with Ki values of 68 nM and 127 nM, respectively. hUP1-IN-2 reduces the toxicity of 5-fluorouracil (HY-90006) against colon cancer. hUP1-IN-2 can be used in the research of colon cancer.
For research use only. We do not sell to patients.
- CAS No.: 1478121-01-5
- Formula: C10H13N3O3
- Molecular Weight:223.23
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
hUP1-IN-2 (Compound 10a) at a concentration of 1 μM inhibits the catalytic activity of recombinant hUP1 by 80%[1].
hUP1-IN-2 acts as a competitive inhibitor of recombinant hUP1 against Urd (Ki = 68 nM), and a non-competitive inhibitor against Pᵢ (Ki = 127 nM)[1].
hUP1-IN-2 binds to free recombinant hUP1, the hUP1-Pi binary complex, and the hUP1-R1P binary complex via exothermic reactions, with the highest affinity for the hUP1-Pi complex (Kd = 151 nM)[1].
hUP1-IN-2 exhibits negligible inhibitory activity against thymidine phosphorylase, with an IC50 >100 μM[1].
hUP1-IN-2 (1-100 μM; 72 h) exerts no significant in vitro cytotoxicity against HaCat, HT-29 or SW-620 cells when applied at concentrations ranging from 1 to 100 μM for 72 h[1].
hUP1-IN-2 (30 μM; 72 h) does not alter the cytotoxicity of 5-FU in HaCat cells, reduces the cytotoxicity of 5-FU in HT-29 cells, and enhances the cytotoxicity of 5-FU in SW-620 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCat (normal human keratinocyte), HT-29 (human colon cancer), SW-620 (human colon cancer)
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Concentration:1-100 μM
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Incubation Time:72 h
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Result:Did not significantly affect cell viability of any tested cell line.
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Cell Line:HaCat (normal human keratinocyte), HT-29 (human colon cancer), SW-620 (human colon cancer)
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Concentration:30 μM
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Incubation Time:72 h
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Result:Caused no significant change in 5-FU IC50 in HaCat cells compared to control.
Caused 9-fold increase in 5-FU IC50 in HT-29 cells, indicating a protective effect.
Caused 6-fold decrease in 5-FU IC50 in SW-620 cells, indicating increased sensitivity to 5-FU.
Chemical Information
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CAS No. 1478121-01-5
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Molecular Weight 223.23
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Formula C10H13N3O3
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SMILES
OC(NC(C(CNCCO)=C1C)=O)=C1C#N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)