I-138
Based on 1 publication(s) in Google Scholar
I-138 is an orally active, reversible inhibitor of USP1-UAF1 (IC50: 4.1 nM; Ki: 5.4 nM), structurally related to ML323 (HY-17543). I-138 induces monoubiquitination of FANCD2 and PCNA in cells and eliminates USP1 autocleavage in cells.
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- Pureté : 99.75%
- CAS No.: 2098211-50-6
- Formule: C26H23F3N6O
- Masse moléculaire:492.50
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Stockage: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
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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HY-17543
ML-323USP1-UAF1 Inhibitor -
HY-138794
XL177AUSP7 Inhibitor -
HY-117043
GRL0617PLpro Inhibitor -
HY-148482
USP7-IN-11USP7 Inhibitor -
HY-149230
USP28-IN-4USP28 Inhibitor -
HY-50737A
DUB-IN-2Deubiquitinase Inhibitor -
HY-80012
SJB3-019AUSP1 Inhibitor -
HY-112438
MF-094USP30 Inhibitor -
HY-13814
PR-619DUB Inhibitor -
HY-100900
ML364USP2 Inhibitor -
HY-122885
IU1-248USP14 Inhibitor -
HY-141659
CMPD-39USP30 Inhibitor
Publications Citing Use of MedChemExpress (MCE) I-138
More
Activité biologique
Description
In Vitro
I-138 (0.5 μM; 4 h) eliminates USP1 self-lysis in HAP-1 USP1 WT and knockout cells[1].
I-138 (0.5 μM; 4 h) induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells[1].
(0.01-10 μM; 10 days) dose-dependently inhibits MDA-MB-436 cells viability and don't affect HCC1954 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2098211-50-6
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Appearance Solid
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Masse moléculaire 492.50
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Formule C26H23F3N6O
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Color White to light yellow
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SMILES
O=C1NC2=CN=C(C3=CC=CC=C3C(C)C)N=C2N1CC4=CC=C(C5=NC(C(F)(F)F)=CN5C)C=C4
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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
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (203.05 mM; Need ultrasonic; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 2.5 mg/mL (5.08 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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PCNA Immunodetection Proliferation Assay
PCNA immunodetection measures proliferative activity by detecting proliferating cell nuclear antigen, a nuclear protein associated with DNA polymerase δ function and DNA replication. The assay readout is the proportion of PCNA-positive nuclei among total counted cells, but PCNA labeling is not identical to BrdU labeling because PCNA can mark late G1/early S-associated replication competence and may persist beyond active DNA synthesis depending on fixation and extraction conditions.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.0305 mL | 10.1523 mL | 20.3046 mL | 50.7614 mL |
| 5 mM | 0.4061 mL | 2.0305 mL | 4.0609 mL | 10.1523 mL | |
| 10 mM | 0.2030 mL | 1.0152 mL | 2.0305 mL | 5.0761 mL | |
| 15 mM | 0.1354 mL | 0.6768 mL | 1.3536 mL | 3.3841 mL | |
| 20 mM | 0.1015 mL | 0.5076 mL | 1.0152 mL | 2.5381 mL | |
| 25 mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 2.0305 mL | |
| 30 mM | 0.0677 mL | 0.3384 mL | 0.6768 mL | 1.6920 mL | |
| 40 mM | 0.0508 mL | 0.2538 mL | 0.5076 mL | 1.2690 mL | |
| 50 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 60 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8460 mL | |
| 80 mM | 0.0254 mL | 0.1269 mL | 0.2538 mL | 0.6345 mL | |
| 100 mM | 0.0203 mL | 0.1015 mL | 0.2030 mL | 0.5076 mL |
I-138 Related Classifications
HY-153365 Related Classifications
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