PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1.
| Molecular Weight | 697.92 |
| Formula | C36H43NO7S3 |
| 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.
[5] Susi Zhu et al. Cancer Lett. Pyruvate kinase M2 (PKM2) in cancer and cancer therapeutics
| Related Pyruvate Kinase Products |
|---|
| ZY-1
ZY-1 is a control molecule of ZY-2. |
| PKR activator 4
PKR activator 4 is a potent pyruvate kinase R (PKR) activator. |
| CIAC001
CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. |
| PKM2-IN-4
Pkm2-in-4 is a selective inhibitor of PKM2 (IC50=0.35 μM), which regulates pyruvate-dependent respiration and induces mitochondrial H202 production rate and electron transport system coupling. |
| TP-1454
TP-1454 is an activator of PKM2 and can be used in studies related to solid tumors. |
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