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PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. PTP1B-IN-9 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. PTP1B-IN-9 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. PTP1B-IN-9 (0-30 µM; 48 hours) treatment produces a dose dependent reduction in the viability of HPV16-positive SiHa and Caski cells and HPV-39-positive ME180 cervical cancer cell lines respectively. PTP1B-IN-9 reduces the cell viability of exponentially growing HeLa cervical cancer cells in a dose-dependent fashion with an IC50 value of 2 µM.
| 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.
| Molecular Weight | 413.12 |
| Formula | C19H13Cl4NO |
| CAS Number | 145888-79-5 |
| Purity | >98% |
| Solubility | |
| Storage | at -20°C |
| Related Proteasome Products |
|---|
| RA190 hydrochloride
RA190 HCl is a potent RPN13 and ADRM1 Inhibitor, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13. |
| MDL 28170
MDL 28170 is a potent cell permeable calpain I and II inhibitor, it reduces capsaicin-mediated cell death in cultured dorsal root ganglion neurons. |
| Sivelestat sodium tetrahydrate
Sivelestat sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse. |
| MG-101
MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM). IC50 value: 150 nM (Ki) |
| VR23
VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM). |
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