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I-138

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Catalog No. T73560Cas No. 2098211-50-6

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.

I-138

I-138

🥰Excellent
Purity: 99.41%
Catalog No. T73560Cas No. 2098211-50-6
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 SizePriceAvailabilityQuantity
1 mg$198In Stock
2 mg$268In Stock
5 mg$388In Stock
10 mg$629In Stock
25 mg$1,180In Stock
50 mg$1,790In Stock
100 mg$2,320In Stock
1 mL x 10 mM (in DMSO)$448In Stock
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Purity:99.41%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight492.5
FormulaC26H23F3N6O
Cas No.2098211-50-6
SmilesC(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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM2.0305 mL10.1523 mL20.3046 mL101.5228 mL
5 mM0.4061 mL2.0305 mL4.0609 mL20.3046 mL
10 mM0.2030 mL1.0152 mL2.0305 mL10.1523 mL
20 mM0.1015 mL0.5076 mL1.0152 mL5.0761 mL
50 mM0.0406 mL0.2030 mL0.4061 mL2.0305 mL
100 mM0.0203 mL0.1015 mL0.2030 mL1.0152 mL

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