KT5823 is a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 inhibits guanosine monophosphate (GMP)-dependent protein kinase activity (cGK). It is a staurosporine compound, which promotes the thyroid-stimulating hormone and regulates Na+/I− symporter (NIS) expression.
| Molecular Weight | 495.53 |
| Formula | C29H25N3O5 |
| CAS Number | 126643-37-6 |
| Form | Solid |
| Solubility (25°C) | ethyl acetate: 5 mg/mL DMSO 1 mg/mL |
| Storage | -20°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.
[3] Jianzhen Li, et al. The role of PKG in oocyte maturation of zebrafish
[5] Diego A Golombek, et al. Signaling in the mammalian circadian clock: the NO/cGMP pathway
| Related PKA Products |
|---|
| Malantide
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. |
| PKI (14-24)amide TFA
PKI (14-24)amide TFA is a potent PKA inhibitor. |
| PKA Inhibitor Fragment (6-22) amide
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. |
| PKI (14-24)amide
PKI (14-24)amide is a potent PKA inhibitor. |
| H1-7 (histone H1 phosphorylation site), PKA Substrate
H1-7 (histone H1 phosphorylation site), PKA Substrate, a synthetic polypeptide, can be used as PKA substrate. |
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