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GSK429286A

Cat. No. M3513
GSK429286A Structure
Synonym:

RHO-15

Size Price Availability Quantity
2mg USD 36  USD40 In stock
5mg USD 54  USD60 In stock
10mg USD 85.5  USD95 In stock
50mg USD 220.5  USD245 In stock
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Quality Control
Biological Activity

GSK429286A is a cell-permeable, selective Rho-associated kinase (ROCK) inhibitor with an IC50 of 14 nM. GSK429286A also possessed exciting selectivity (30-fold) against a panel of 33 kinases, including RSK1 (IC50 = 3.1 μM) and p70S6K (Ic50 = 2.85μM). ROCKs are serine/threonine specific protein kinases which play a crucial role in organization of the actin cytoskeleton. ROCK inhibitors have been found to prevent apoptosis, as well as to enhance the survival and cloning efficiency of dissociated human embryonic stem (ES) cells without affecting their self-renewal properties or pluripotency.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Male spontaneously hypertensive rats (SHRs)
Formulation Formulated in 6% Hydroxypropyl-β-Cyclodextrin (pH4.0) and 5% DMSO solution
Dosages ~30 mg/kg
Administration Oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 432.37
Formula C21H16F4N4O2
CAS Number 864082-47-3
Purity 99.74%
Solubility DMSO 75 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK429286A, RHO-15 supplier, ROCK, inhibitors

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