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GSK429286A

Catalog No. T2633 CAS 864082-47-3

Synonyms: RHO-15

GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).

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GSK429286A, CAS 864082-47-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 35.00
5 mg	In stock	$ 56.00
10 mg	In stock	$ 85.00
25 mg	In stock	$ 139.00
50 mg	In stock	$ 215.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 98.42%

Purity: 97.68%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
Targets&IC50	ROCK1:14 nM, ROCK2:63 nM
In vitro	GSK429286A (3-30 mg/kg, p.o.) significantly reduces the mean arterial pressure in spontaneous hypertensive rats in a dose-dependent manner, with a maximum reduction of 50 mmHg approximately 2 hours after administering a dose of 30 mg/kg. In male Sprague-Dawley rats, the oral bioavailability of GSK429286A is 61%.
In vivo	GSK429286A at a concentration of 1 μM significantly reduces the activity of ROCK2 by 20-fold, whereas it only reduces MSK1 activity by approximately 5-fold at the same concentration. This compound exhibits higher selectivity as an ROCK2 inhibitor compared to the commonly used inhibitor Y-27632, showing negligible inhibition against LRRK2 even at 30 μM, with an IC50 that is 500 times higher for ROCK2. Similar to GSK269962A, GSK429286A at 10 μM can eliminate phosphorylation at Thr850 of MYPT induced either by the baseline or by the G14V-Rho mutant in HEK-293 cells, demonstrating effects similar to those of H-1152 and Y-27632 and consistent with ROCK-mediated phosphorylation. Regardless of the presence of G14V-Rho, GSK429286A does not affect the phosphorylation of ERM proteins. Additionally, GSK429286A mildly inhibits RSK (IC50: 0.78 μM) and p70S6K (IC50: 1.94 μM). It also significantly inhibits the dilation of rat aortic rings (IC50: 190 nM).
Kinase Assay	Binding affinity assays: TR-FRET-binding affinity assays are performed for BCL-2, BCL-XL, and MCL-1 in 4.52?mM monobasic potassium phosphate, 15.48?mM dibasic potassium phosphate, 1?mM sodium EDTA, 0.05% Pluronic F-68 detergent, 50?mM sodium chloride, and 1?mM DTT (pH 7.5). For MCL-1 assays, GST-tagged MCL-1 (1?nM) is mixed with 100?nM f-Bak, 1?nM Tb-labeled anti-GST antibody, and compound at room temperature (RT) for 60?min. Fluorescence is measured on an Envision plate reader using a 340/35?nm excitation filter and 520/525 (f-Bak) and 495/510?nm (Tb-labeled anti-GST antibody) emission filters.

Synonyms	RHO-15
Molecular Weight	432.37
Formula	C21H16F4N4O2
CAS No.	864082-47-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 4 mg/mL (9.25 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 81 mg/mL (187.3 mM)

References and Literature

1. Goodman KB, et al. J Med Chem, 2007, 50(1), 6-9. 2. Nichols RJ, et al. Biochem J, 2009, 424(1), 47-60.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library TGF-beta/Smad Compound Library Highly Selective Inhibitor Library Cell Cycle Compound Library Neural Regeneration Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Cytoskeletal Signaling Pathway Compound Library Wnt/Hedgehog/Notch Compound Library Reprogramming Compound Library

Related Products

Related compounds with same targets

SB-772077B dihydrochloride GSK269962A GSK180736A RKI-1447 CKI-7 Afuresertib ROCK-IN-9 CMPD101

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Keywords

GSK429286A 864082-47-3 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK RHO15 Inhibitor inhibit RHO 15 GSK-429286A RHO-15 Rho-kinase Rho-associated kinase ROK Rho-associated protein kinase inhibitor

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