NVS-ZP7-4 is a potent ZIP7 Inhibitor, which inhibits Notch signaling with IC50 of 0.13 uM in HES-Luc reporter gene assays, selectively induces apoptosis and ER stress. NVS-ZP7-4 altered zinc in the ER, and an analog of the compound photoaffinity labeled ZIP7 in cells. NVS-ZP7-4 can probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
| Molecular Weight | 501.62 |
| Formula | C28H28FN5OS |
| CAS Number | 2349367-89-9 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage | -20°C, protect from light, dry, sealed |
| 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.
[1] Erin Nolin, et al. Nat Chem Biol. Discovery of a ZIP7 inhibitor from a Notch pathway screen
| Related Notch Products |
|---|
| Jagged-1 (188-204)
Jagged-1 (188-204) is a fragment of the Jagged-1 (JAG-1) protein with Notch agonist activity. |
| DAPM
DAPM is a Notch pathway inhibitor with anticancer activity and antiproliferative effects. |
| Procyanidin B2 3,3'-di-O-gallate
Procyanidin B2, 3,3'-di-O-gallate is an active constituent. Procyanidin B2, 3,3'-di-O-gallate strongly suppresses the constitutive as well as Jagged1 (Notch1 ligand)-induced activated Notch1 pathway. |
| SAHM1 TFA
SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly. |
| JI051
JI051 is a stabilizer for the Hes1-PHB2 interaction. JI051 interacts with a cancer-associated protein chaperone prohibitin 2 (PHB2), induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1. Anti-cancer activity. |
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