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I-138 is an orally active and potent reversible inhibitor of USP1-UAF1.I-138 induces mono-ubiquitination of FANCD2 and PCNA and inhibits USP1 auto-cleavage in cells.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $189 | - | In Stock | |
| 5 mg | $388 | - | In Stock | |
| 10 mg | $546 | - | In Stock | |
| 25 mg | $786 | - | In Stock | |
| 50 mg | $1,090 | - | In Stock | |
| 100 mg | $1,630 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $427 | - | In Stock |
| Description | I-138 is an orally active and potent reversible inhibitor of USP1-UAF1.I-138 induces mono-ubiquitination of FANCD2 and PCNA and inhibits USP1 auto-cleavage in cells. |
| In vitro | I-138 (0.5 μM; 4 hours) eliminates USP1 autodeubiquitination in HAP-1 USP1 WT and knockout cells, induces monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells, and dose-dependently (0.01-10 μM; 10 days) inhibits the viability of MDA-MB-436 cells without affecting HCC1954 cells[1]. |
| In vivo | I-138 (50 mg/kg/day; oral administration; for 41 days) shows USP1 inhibition and moderate antitumor activity in mice with MDA-MB-436 tumors. However, combining I-138 with the PARP inhibitor Niraparib is more effective at inhibiting BRCA1/2 mutant tumors in vivo[1]. |
| Molecular Weight | 492.5 |
| Formula | C26H23F3N6O |
| Cas No. | 2098211-50-6 |
| Smiles | C(N1C=2C(NC1=O)=CN=C(N2)C3=C(C(C)C)C=CC=C3)C4=CC=C(C=C4)C5=NC(C(F)(F)F)=CN5C |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (162.44 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.7 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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