Description
Key facts
CAS number:130964-39-5,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:519.3 Da,
Molecular formula:C20H22BrCl2N3O2S,
PubChem:5702541,
Nature:Synthetic,
Biochemical name:H-89 Dihydrochloride,
Biological description:Kinase inhibitor, commonly used as a protein kinase A inhibitor (IC50 = 135 nM). Also inhibits other kinases, including MSK1 , S6K1 and ROCKII (IC50 values are 120, 80 and 270 nM, respectively).,
Canonical smiles:C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNCC=CC3=CC=C(C=C3)Br.Cl.Cl,
Isomeric smiles:C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNC/C=C/C3=CC=C(C=C3)Br.Cl.Cl,
InChi:InChI=1S/C20H20BrN3O2S.2ClH/c21-18-8-6-16(7-9-18)3-2-11-22-13-14-24-27(25,26)20-5-1-4-17-15-23-12-10-19(17)20;;/h1-10,12,15,22,24H,11,13-14H2;2*1H/b3-2+;;,
InChiKey:GELOGQJVGPIKAM-WTVBWJGASA-N,
IUPAC Name:N-[2-[[(E)-3-(4-bromophenyl)prop-2-enyl]amino]ethyl]isoquinoline-5-sulfonamide;dihydrochloride
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
S6K1 AKT1 AKT2 and AKT3 are part of a group of serine/threonine kinases that play roles in cellular signaling. ROCK2 or Rho Kinase alpha is another serine/threonine kinase involved in regulating cytoskeletal dynamics. The cAMP Protein Kinase Catalytic subunit which includes PKA beta is important for many cellular processes through cAMP-dependent pathways. PRKACG is a catalytic subunit of PKA and has a molecular weight of about 40 kDa. These targets express widely in many tissues including muscle brain and liver where they have specific roles in diverse cellular activities.
Biological function summary
These kinases are essential in regulating proliferation survival and cell growth. S6K1 is critical in protein synthesis often linked with the mTOR complex. AKT isoforms (AKT1 AKT2 AKT3) control apoptosis and metabolism often in response to growth factors. ROCK2 influences smooth muscle contraction and cell motility. The cAMP Protein Kinase Catalytic subunit (including PKA) mediates responses to hormonal stimuli. They are often part of larger protein complexes impacting cellular reactions and maintaining homeostasis.
Pathways
These proteins are involved in important cellular signaling pathways like the PI3K/AKT/mTOR and RhoA/ROCK pathways. AKT1 AKT2 and AKT3 facilitate intracellular signaling impacting protein synthesis and glucose metabolism. S6K1 acts downstream of mTOR and works with these proteins to regulate cell growth and metabolism. ROCK2 functions in the regulation of actin cytoskeleton dynamics and interacts with other proteins like RhoA influencing cell shape and motility.
These targets relate to various pathological conditions like cancer and diabetes. Aberrant AKT signaling which includes AKT1 AKT2 and AKT3 is implicated in oncogenesis and tumor progression. The overactivity or dysregulation of mTOR/S6K1 signaling is pivotal in many cancers and metabolic disorders. ROCK2 dysregulation plays a role in hypertension and cardiac diseases influencing vascular tone and function. These kinases form potential therapeutic targets with inhibitors developed to modulate their activities in disease states.
