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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 | Availability | Quantity |
---|---|---|---|
1 mg | $198 | In Stock | |
2 mg | $268 | In Stock | |
5 mg | $388 | In Stock | |
10 mg | $629 | In Stock | |
25 mg | $1,180 | In Stock | |
50 mg | $1,790 | In Stock | |
100 mg | $2,320 | In Stock | |
1 mL x 10 mM (in DMSO) | $448 | 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (162.44 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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