K252a is an inhibitor of the BDNF receptor TrkB. K-252a inhibits protein kinase with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
Tianjin Medical Journal. 2023;51(4):387-391.
Study on the mechanism of glial maturation factor-β induced inflammatory response of retinal Müller cells in diabetes rats
K252a purchased from AbMole
Molecular Weight | 467.47 |
Formula | C27H21N3O5 |
CAS Number | 99533-80-9 |
Solubility (25°C) | DMSO 50 mg/mL (Need ultrasonic and warming) |
Storage | -20°C |
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.
[4] Alessandro Morotti, et al. K252a inhibits the oncogenic properties of Met, the HGF receptor
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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.