hUP1-IN-2
Based on 1 Customer Validation
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.24%
- CAS. Nr.: 1478121-01-5
- Formel: C10H13N3O3
- Molecular Weight:223.23
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
Beschreibung
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
-
Cell Line:HaCat (normal human keratinocyte), HT-29 (human colon cancer), SW-620 (human colon cancer)
-
Concentration:1-100 μM
-
Incubation Time:72 h
-
Result:Did not significantly affect cell viability of any tested cell line.
-
Cell Line:HaCat (normal human keratinocyte), HT-29 (human colon cancer), SW-620 (human colon cancer)
-
Concentration:30 μM
-
Incubation Time:72 h
-
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
-
CAS. Nr. 1478121-01-5
-
Appearance Solid
-
Molecular Weight 223.23
-
Formel C10H13N3O3
-
Color Off-white to light yellow
-
SMILES
OC(NC(C(CNCCO)=C1C)=O)=C1C#N
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 12.5 mg/mL (56.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (5.60 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (5.60 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
-
Data Sheet (272 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.4797 mL | 22.3984 mL | 44.7968 mL | 111.9921 mL |
| 5 mM | 0.8959 mL | 4.4797 mL | 8.9594 mL | 22.3984 mL | |
| 10 mM | 0.4480 mL | 2.2398 mL | 4.4797 mL | 11.1992 mL | |
| 15 mM | 0.2986 mL | 1.4932 mL | 2.9865 mL | 7.4661 mL | |
| 20 mM | 0.2240 mL | 1.1199 mL | 2.2398 mL | 5.5996 mL | |
| 25 mM | 0.1792 mL | 0.8959 mL | 1.7919 mL | 4.4797 mL | |
| 30 mM | 0.1493 mL | 0.7466 mL | 1.4932 mL | 3.7331 mL | |
| 40 mM | 0.1120 mL | 0.5600 mL | 1.1199 mL | 2.7998 mL | |
| 50 mM | 0.0896 mL | 0.4480 mL | 0.8959 mL | 2.2398 mL |
hUP1-IN-2 Related Classifications
HY-185840 Related Classifications
Powered by Bioz