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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

COA COA
In stock
Item Number
G127028
Grouped product items
SKU Size
Availability
 Price Qty
G127028-5mg
5mg
3
$70.90
G127028-10mg
10mg
2
$107.90
G127028-25mg
25mg
2
$243.90
G127028-50mg
50mg
2
$282.90
G127028-100mg
100mg
1
$489.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet

Selective ROCK1 and ROCK2 inhibitor

View related series
Cell Cycle (2830) Cell Cycle/DNA Damage (2602) Cytoskeleton (498) Rho associated coiled-coil containing protein kinase 1 Inhibitor (17) ribosomal protein S6 kinase A1 Inhibitor (8) ROCK (71) Stem Cell/Wnt (1019) TGF-beta/Smad (303)

Basic Description

Synonyms HMS3244C08 | HMS3654N12 | N6-ethanimidoyl-L-lysine dihydrochloride | dihydropyridone indazole amide 15 | HY-11000 | N-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydropyridine-3-carboxamide | N-(6-Fluoro-1H-indazol
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms GSK429286A 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 Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of Rho associated coiled-coil containing protein kinase 1;Inhibitor of ribosomal protein S6 kinase A1
Note Wherever 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.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Class Benzene and substituted derivatives
Subclass Trifluoromethylbenzenes
Intermediate Tree Nodes Not available
Direct Parent Trifluoromethylbenzenes
Alternative Parents Indazoles  N-arylamides  Tetrahydropyridines  Aryl fluorides  Vinylogous amides  Heteroaromatic compounds  Pyrazoles  Lactams  Secondary carboxylic acid amides  Azacyclic compounds  Hydrocarbon derivatives  Alkyl fluorides  Carbonyl compounds  Organic oxides  Organofluorides  Organopnictogen compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Trifluoromethylbenzene - Indazole - Benzopyrazole - N-arylamide - Tetrahydropyridine - Aryl fluoride - Aryl halide - Hydropyridine - Azole - Pyrazole - Heteroaromatic compound - Vinylogous amide - Secondary carboxylic acid amide - Lactam - Carboxamide group - Azacycle - Carboxylic acid derivative - Organoheterocyclic compound - Alkyl fluoride - Organohalogen compound - Organofluoride - Organonitrogen compound - Organooxygen compound - Hydrocarbon derivative - Carbonyl group - Organic oxide - Organopnictogen compound - Organic oxygen compound - Organic nitrogen compound - Alkyl halide - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as trifluoromethylbenzenes. These are organofluorine compounds that contain a benzene ring substituted with one or more trifluoromethyl groups.
External Descriptors Not available

Associated Targets(Human)

ROCK1 Tclin Rho-associated protein kinase 1 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha-1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKACB Tchem cAMP-dependent protein kinase beta-1 catalytic subunit (589 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK2 Tclin Rho-associated protein kinase 2 (6206 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKACA Tchem cAMP-dependent protein kinase alpha-catalytic subunit (3475 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KB1 Tchem Ribosomal protein S6 kinase 1 (4456 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Thoracic aorta (838 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504766351
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504766351
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)
InChIKey OLIIUAHHAZEXEX-UHFFFAOYSA-N
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
Molecular Weight 432.37
Reaxy-Rn 10732416
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10732416&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot Number Certificate Type Date Item
I2227264 Certificate of Analysis Jul 15, 2024 G127028
I2227246 Certificate of Analysis Jul 15, 2024 G127028
I2227265 Certificate of Analysis Jul 15, 2024 G127028
I2227266 Certificate of Analysis Jul 15, 2024 G127028
I2227267 Certificate of Analysis Jul 15, 2024 G127028

Chemical and Physical Properties

Solubility DMSO 87 mg/mL Water <1 mg/mL Ethanol 4 mg/mL
Molecular Weight 432.400 g/mol
XLogP3 2.900
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 3
Exact Mass 432.121 Da
Monoisotopic Mass 432.121 Da
Topological Polar Surface Area 86.900 Ų
Heavy Atom Count 31
Formal Charge 0
Complexity 748.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 1
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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