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GSK429286A - 98%, high purity , CAS No.864082-47-3, Inhibitor of Rho associated coiled-coil containing protein kinase 1;Inhibitor of ribosomal protein S6 kinase A1

  • Moligand™
  • ≥98%
Item Number
G127028
Grouped product items
SKUSizeAvailabilityPrice Qty
G127028-5mg
5mg
In stock
$70.90
G127028-10mg
10mg
In stock
$107.90
G127028-25mg
25mg
In stock
$243.90
G127028-50mg
50mg
In stock
$282.90
G127028-100mg
100mg
In stock
$489.90

Selective ROCK1 and ROCK2 inhibitor

Basic Description

SynonymsGSK429286A|864082-47-3|RHO-15|N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide|N-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamid
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsGSK429286A is a cell-permeable, selective Rho-associated kinase (ROCK) inhibitor with an IC50 of 14 nM.Selective ROCK1 and ROCK2 inhibitor. Demonstrated inhibition of ROCKs at 140 nM. Reduces ROCK2 activity over 20-fold at 1 μM. Active in vitro.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of Rho associated coiled-coil containing protein kinase 1;Inhibitor of ribosomal protein S6 kinase A1
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Toxic, refer to SDS for further information. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

Associated Targets

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ROCK2 Tclin Rho-associated protein kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ROCK1 Tclin Rho-associated protein kinase 1 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

JAK3 Tclin Tyrosine-protein kinase JAK3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKACB Tchem cAMP-dependent protein kinase catalytic subunit beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RPS6KB1 Tchem Ribosomal protein S6 kinase beta-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RPS6KA1 Tchem Ribosomal protein S6 kinase alpha-1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKACA Tchem cAMP-dependent protein kinase catalytic subunit alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide
INCHI InChI=1S/C21H16F4N4O2/c1-10-19(20(31)28-17-6-12-9-26-29-16(12)8-15(17)22)14(7-18(30)27-10)11-2-4-13(5-3-11)21(23,24)25/h2-6,8-9,14H,7H2,1H3,(H,26,29)(H,27,30)(H,28,31)
InChi Key OLIIUAHHAZEXEX-UHFFFAOYSA-N
Canonical SMILES CC1=C(C(CC(=O)N1)C2=CC=C(C=C2)C(F)(F)F)C(=O)NC3=C(C=C4C(=C3)C=NN4)F
Isomeric SMILES CC1=C(C(CC(=O)N1)C2=CC=C(C=C2)C(F)(F)F)C(=O)NC3=C(C=C4C(=C3)C=NN4)F
WGK Germany 3
PubChem CID 11373846
Molecular Weight 432.37

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

5 results found

Lot NumberCertificate TypeDateItem
I2227246Certificate of AnalysisJul 15, 2024 G127028
I2227264Certificate of AnalysisJul 15, 2024 G127028
I2227265Certificate of AnalysisJul 15, 2024 G127028
I2227266Certificate of AnalysisJul 15, 2024 G127028
I2227267Certificate of AnalysisJul 15, 2024 G127028

Chemical and Physical Properties

SolubilityDMSO 87 mg/mL Water <1 mg/mL Ethanol 4 mg/mL

Safety and Hazards(GHS)

Pictogram(s) GHS06
Signal Danger
Hazard Statements

H301:Toxic if swallowed

Precautionary Statements

P321:Specific treatment (see ... on this label).

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P301+P316:IF SWALLOWED: Get emergency medical help immediately.

WGK Germany 3

Related Documents

References

1. Goodman KB, Cui H, Dowdell SE, Gaitanopoulos DE, Ivy RL, Sehon CA, Stavenger RA, Wang GZ, Viet AQ, Xu W et al..  (2007)  Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors..  J Med Chem,  50  (1): (6-9).  [PMID:17201405]

Solution Calculators