PKCβ inhibitor is a potent and selective inhibitor of PKCβ isozymes (IC50 = 5 nM and 21 nM for human PKCβII and βI). PKCβ inhibitor displays greater selectivity over PKCα, PKCγ, PKCε with IC50s of 331 nM, > 1 μM, and 2.8 μM, respectively.
| Molecular Weight | 411.46 |
| Formula | C24H21N5O2 |
| CAS Number | 257879-35-9 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| 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.
[1] James D Phelan, et al. A multiprotein supercomplex controlling oncogenic signalling in lymphoma
[2] Ovidiu Musat, et al. DIABETIC MACULAR EDEMA
[3] Heidrun L Deissler, et al. The Protein Kinase C Inhibitor: Ruboxistaurin
[4] Thomas E Witzig, et al. Signal transduction inhibitor therapy for lymphoma
| Related PKC Products |
|---|
| PKC β pseudosubstrate
PKC β pseudosubstrate is a selective cell-permeable inhibitor of PKC. |
| Protein Kinase C (19-31)
Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), is used as protein kinase C substrate peptide for testing the protein kinase C activity. |
| Protein Kinase C (19-36)
Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM. |
| [Ala113]MBP(104-118)
[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM. |
| [Ala107]MBP(104-118)
[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM. |
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