A-3 Hydrochloride is A potent, cellular permeable, reversible, atP-competitive, non-selective antagonist targeting multiple kinases. A-3 Hydrochloride is an inhibitor of PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM), and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibited PKC and casein kinase I activity with Ki of 47 µM and 80 µM, respectively.
| Molecular Weight | 321.22 |
| Formula | C12H13ClN2O2S · HCl |
| CAS Number | 78957-85-4 |
| Solubility (25°C) | DMSO: 24 mg/mL |
| Storage | 4°C, 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] Hassan Kamran, et al. Oral Antiplatelet Therapy After Acute Coronary Syndrome: A Review
[3] Sang Myung Woo. Chemotherapy for Biliary Tract Cancer
[5] H R Kaplan. Bevantolol hydrochloride--preclinical pharmacologic profile
| 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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