IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 inhibits IsoT/USP5 with an IC50 of 20 μM. IU1-47 stimulates tau degradation principally via the ubiquitin-proteasome system. IU1-47 (3 μM, 10 and 30 μM; 48 hours) significantly decreases Tau and phosphotau species Ser-202/Thr-205 levels in murine cortical primary neurons. The level of USP14 itself does not change.
| Cell Experiment | |
|---|---|
| Cell lines | Murine cortical primary neurons (DIV5) isolated from APPSwe/P301L transgenic animals |
| Preparation method | Murine cortical primary neurons (DIV5) isolated from APPSwe/P301L transgenic animals were incubated with the indicated doses of IU1-47 for 48 h, then harvested, and processed as above. Immunoblots developed with IRDye-conjugated secondary antibodies show the level of total tau and of several specific phospho (P)-tau species upon IU1-47 treatment. Phosphoepitopes are indicated in parentheses. The top three blots are from one gel; the bottom four blots are from another gel (left). The USP14 blot shows that no change in USP14 protein level was observed upon IU1-47 treatment. Values in the graphs represent an average of two biological replicates representing cortical neurons from littermates. |
| Concentrations | 3 μM, 10 μM and 30 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 330.85 |
| Formula | C19H23ClN2O |
| CAS Number | 670270-31-2 |
| Solubility (25°C) | DMSO 8 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Deubiquitinase Products |
|---|
| TNG348
TNG348 is a novel, oral, potent and selective ubiquitin-specific protease 1 (USP1) inhibitor for studies related to BRCA1/2 mutations and other homologous recombination defect (HRD)+ cancers. |
| FT-3171
FT-3171 is a small molecule ubiquitin-specific protease 1 (USP1) inhibitor targeting a novel DNA damage repair (DDR) pathway for studies related to solid tumors. |
| BAY-728
BAY-728 serves as a negative control for BAY-805, a potent and selective USP21 inhibitor. |
| BAY-805
BAY-805 is a selective inhibitor of the ubiquitin-specific protease USP21 with high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common off-target enzymes. |
| USP1-IN-6
USP1-IN-6 is a USP1 inhibitor (IC50<50 nM). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
