hUP1-IN-2 |
Catalog No.GC79748
One-Click Copy Product Info
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hUP1-IN-2 is a Urd-competitive and Pᵢ-noncompetitive hUP1 inhibitor with K i values of 68 nM and 127 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1478121-01-5
Sample solution is provided at 25 µL, 10mM.
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In Vitro, 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].
References:
[1]. Renck D, et al. Design of novel potent inhibitors of human uridine phosphorylase-1: synthesis, inhibition studies, thermodynamics, and in vitro influence on 5-fluorouracil cytotoxicity. Journal of medicinal chemistry. 2013 Nov 14;56(21):8892-902.
| Cas No. | 1478121-01-5 | SDF | |
| Formula | C10H13N3O3 | M.Wt | 223.23 |
| Solubility | DMSO: 12.5 mg/mL (56.00 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4797 mL | 22.3984 mL | 44.7968 mL |
| 5 mM | 895.9 μL | 4.4797 mL | 8.9594 mL |
| 10 mM | 448 μL | 2.2398 mL | 4.4797 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)