δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research.
| Molecular Weight | 220.23 |
| Formula | C10H12N4O2 |
| CAS Number | 842964-18-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (ultrasonic) |
| Storage | 4°C, protect from light |
| 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.
[5] Kazumi Ishidoh, et al. Biol Chem. Processing and activation of lysosomal proteinases
| Related Caspase Products |
|---|
| TC11
TC11 is a phenylphthalimide derivative and an activator of caspase-9 and CDK1, as well as a degrader of MCL1.TC11 is structurally related to immunomodulatory active molecules. During prolonged mitotic blockade, TC11 induces MCL1 degradation and leads to apoptotic death. |
| Ac-Ile-Glu-Thr-Asp-pNA
Ac-Ile-Glu-Thr-Asp-pNA is a substrate for caspase-8. |
| Z-DEVD-AFC
Z-DEVD-AFC is a cell-permeant substrate for caspase-3, which causes a shift in fluorescence uponcleavage of the AFC fluorophore. |
| Ac-IETD-AFC
Ac-IETD-AFC is a fluorogenic substrate of caspase-8, caspase-3, caspase-10, and granzyme B. |
| Z-VDVAD-FMK
Z-VDVAD-FMK is a special inhibitor of caspase-2. |
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